Roland E. Dolle, Ph.D.

Research

Inventing new medicines is the overarching theme of my laboratory. It is an integral part of the Center for Drug Discovery. We design and synthesize novel molecular probes and small molecule ligands to aid in the understanding of the mechanistic pathophysiology of human diseases. Drug leads are identified through classical high-throughput screening or one of many other alternative strategies. A drug lead may be defined as a chemical that triggers a specific biological action. It serves as a chemical starting point for a preclinical discovery project. Using medicinal and computational chemistry, drug leads are optimized for potency, molecular target selectivity, pharmacokinetics, in vivo pharmacology, pharmacodynamics, and safety to yield proprietary development candidates for potential clinical evaluation in patients. Lead optimization creates variations of the original chemical and tests their performance against a range of biological endpoints. In this process, structure-activity relationships are established informing the design of increasingly robust drug-like molecules. Because the principles of drug design are applicable to virtually any molecular target, our projects tackle drugs for enzymes, proteases, kinases, receptors, transporters, ion channels, transcription factors, and RNA, transcending anti-infective, cardiovascular, gastroenterology, neurology (CNS), oncology, and allied therapeutic areas.

Our laboratory’s expertise and capability to identify and optimize drug leads provides a strong basis for collaboration with Washington University researchers.

Representative WUSTL collaborators:

J Cho   •    G Dorn  •   L Shan   •    J Heemstra  •   P Kotzbauer  •   K Lavine  •   M Greenberg  •   K Mahajan  •   N Mahajan  •   S Mennerick  •   J Milbrandt  •   A DiAntonio  •   R Pachynski  •   D Pagliarini  •   T Peterson  •   D Piston  •   L Ratner  •   M Rutherford  •   R Sah  •   D Spitzer  •   A Stegh  •   B Van Tine  •   D Perlmutter  •   L Adamo  •   G Amarasinghe  •   J Arbeit  •   M Artyomov  •   R Bateman  •   A Bonni  •   G Bowman  •   A Cashikar  •   G Challen  •   Z Chen  •   J Cui  •   J Dougherty  •   J Guo  •   D Hallahan  •   S Haroutounian  •   P Hruz  •   D Hunstad  •   P Kung  •   W Li  •   L Ma  •   G Longmore  •   B Major  •   D Mann  •   B Maybruck  •   J Miner  •   K Moley  •   M Montana  •   A Morhardt  •   A Orevdahl  •   T Papouin  •   J Petroff  •   J Phillips  •   B Racette  •   B Razani  •   D Rosen  •   K Seibert  •   T Stappenbeck  •   J Wambach  •   T Wencewicz  •   B Wiss  •   B Yue  •   Q Zhang  •   S England  •   D Covey  •   J Henderson  •   M Chheda  •   H Yano  •   D Fremont  •   S Pak  •   D Curiel  •   B DeBosch  •   G Silverman  •   A Kim  •   C Stallings  •   M Colonna  •   M Bambouskova  •   J Huettner  •   B Kim  •   M Chen  •   B Humphreys  •   S Markovina  •   H Adhikari  •   R Fowle Grider  •   F Asadi Jomnani  •   J Schwartz  •   R Gereau  •   J Lodge  •   J Millman  •   D Sibley  •   R Galletto  •   A Yoo  •   K Azab  •   G Dantas  •   S Achilefu  •   B Garcia  •   W Barnes  •   J Janetka  •   C Luke  •   M Ilagan  •   M Zayed  •   J Boon  •   I Singh  •   G Grant  •   A Evers  •   S Djuranovic

Select Publications

A novel dual NLRP1 and NLRP3 inflammasome inhibitor for the treatment of inflammatory diseases. Docherty, C. A., Fernando, A. J., Rosli, S., Lam, M., Dolle, R. E., Navia, M. A., Farquhar, R., La France, D., Tate, M. D., Murphy, C. K., Rossi, A. G., Mansell, A. Clin. Transl. Immunology, 2023, 12, e1455.

Development of ADS051, an oral, gut-restricted, small molecule neutrophil modulator for the treatment of neutrophil-mediated inflammatory diseases. Murphy, C. K., Dixit, B., Oleson, F. B., Dolle, R. E., Farquhar, R., McCormick, B. A. Development of ADS051, an oral, gut-restricted, small molecule neutrophil modulator for the treatment of neutrophil-mediated inflammatory diseases. FEBS Open Bio, 2023, 13, 1434–1446.

Age-related Huntington’s disease progression modeled in directly reprogrammed patient-derived striatal neurons highlights impaired autophagy. Oh, Y. M., Lee, S. W., Kim, W. K., Chen, S., Church, V. A., Cates, K., Li, T., Zhang, B., Dolle, R. E., Dahiya, S., Pak, S. C., Silverman, G. A., Perlmutter, D. H., & Yoo, A. S. Nature Neurosci. 2022, 25, 1420–1433.

Reducing auditory nerve excitability by acute antagonism of Ca2+-permeable AMPA receptors. Walia, A.; Lee, C.; Hartsock, J.; Goodman, S. S.; Dolle, R. E.; Salt, A. N.; Lichtenhan, J. T.; Rutherford, M. A. Front. Synaptic Neurosci. 2021, 13, 1-19.

Discovery of 6-phenylhexanamide derivatives as potent stereoselective mitofusin activators for the treatment of mitochondrial diseases. Dang, X.; Zhang, L.; Franco, A.; Li, Jiajia; R., Agostinho G.; Devanathan, S.; Dolle, R. E.; Bernstein, P. R.; Dorn, G. W. J. Med. Chem. 2020, 63, 7033-7051.

Discovery of pyrazolopyridones as a novel class of gyrase B inhibitors using structure guided design. Cross, J. B.; Zhang, J.; Yang, Q.; Mesleh, M. F.; Romero, J. A. C.; Wang, B.; Bevan, D.; Poutsiaka, K. M.; Epie, F.; Moy, T.; Daniel, A.; Shotwell, J.; Chamberlain, B.; Carter, N.; Andersen, O.; Barker, J.; Ryan, M. D.; Metcalf, C. A., III; Silverman, J.; Nguyen, K.; Lippa, B.; Dolle, R. E. ACS Med. Chem. Lett. 2016, 7, 374-378.

Fragment-based discovery of DNA gyrase inhibitors targeting the ATPase subunit of gyrase B. Mesleh, M. F.; Cross, J. B.; Zhang, J.; Kahmann, J.; Andersen, O. A.; Barker, J.; Cheng, R. K.; Felicetti, B.; Wood, M.; Hadfield, A. T.; Scheich, C.; Moy, T. I.; Yang, Q.; Shotwell, J.; Nguyen, K.; Lippa, B.; Dolle, R. E.; Ryan, M. D. Bioorg. Med. Chem. Lett. 2016, 26, 1314-1318.

Discovery of azaindole ureas as a novel class of bacterial gyrase B inhibitors. Zhang, J.; Yang, Q.; Cross, J.; Romero, J. A. C.; Poutsiaka, K. M.; Epie, F.; Bevan, D.; Wang, B.; Zhang, Y.; Chavan, A.; Zhang, X.; Moy, T.; Daniel, A.; Nguyen, K.; Chamberlain, B.; Carter, N.; Shotwell, J.; Silverman, J.; Metcalf, III, C. A.; Ryan, D., Lippa, B.; Dolle, R. E. J. Med. Chem. 2016, 58, 8503-8512.

Discovery of indazole derivatives as a novel class of bacterial gyrase B inhibitors. Zhang, J.; Yang, Q.; Romero, A. J. C.; Cross, J.; Wang, B.; Poutsiaka, K. M.; Epie, F.; Bevan, D.; Wu, Y.; Moy, T.; Daniel, A.; Chamberlain, B.; Carter, N.; Shotwell, J.; Arya, A.; Kumar, V.; Silverman, J.; Nguyen, K.; Metcalf, C. A.; Ryan, D.; Lippa, B.; Dolle, R. E. ACS Med. Chem. Lett. 2016, 6, 1080-1085.

The discovery and development of the N-substituted trans-3,4-dimethyl-4-(3′-hydroxyphenyl)piperidine class of pure opioid receptor antagonists. Carroll, F. I.; Dolle, R. E. ChemMedChem. 2014, 9, 1638-1654.

δ-Opioid mechanisms for ADL5747 and ADL5859 effects in mice: analgesics, locomotion, and receptor internalization. Chihiro, N.; Le Bourdonnec, B.; Reiss, D.; Windh, R. T.; Little, P. J.; Dolle, R. E.; Kieffer, B. L.; Gaveriaux-Ruff, D. J. Pharmacol. Exp. Ther. 2012, 342, 799-807.

The selective mu-opioid receptor antagonist ADL5510 reduces levodopa-induced dyskinesia without affecting antiparkinsonian action in MPTP-lesioned macaque model of Parkinson’s disease. Koprich J. B.; Fox S. H.; Johnston T. H.; Goodman A.; Le Bourdonnec B.; Dolle R. E.; DeHaven R. N.; DeHaven-Hudkins D. L.; Little P. J; Brotchie J. M. Movement Disorders 2011, 26, 1225-33.

Opioid receptor antagonists for gastrointestinal dysfunction. Hipkin, R. W.; Dolle, R. E. Ann. Reports Med Chem. 2010, 45, 143-155.

A facile synthesis of novel 2-amino-6-arylmethyl-7-carboxamido-7,8-dihyropyrimido[5,4-f][1,4]thiazepin-5-ones. Qin, L.-Y.; Cole, A. G.; Metzger, A.; Brescia, M.-R.; Salonz, K. W.; Zhang, J. J.; Rogollier. P.; Wareing, J. R.; Gstach, H.; Zimmerman, J.; Dolle, R. E. Tetrahedron Lett. 2010, 51, 4486-4489.

Comprehensive survey of chemical libraries for drug discovery and chemical biology: 2009. Dolle, R. E.; Le Bourdonnec, B.; Worm, K.; Morales, G. A.; Thomas, C. J.; Zhang, W. J. Combin. Chem. 2010, 12, 765-806.

Novel sulfamoyl benzamides as selective CB2 agonists with improved in vitro metabolic stability. Sellitto, I.; Le Bourdonnec, B.; Worm, K.; Goodman, A.; Salvolainen, M. A.; Chu, C.-H.; Ajello, C. W.; Saeui, C. T.; Leister, L. K.; Cassel, J. A.; DeHaven, R. N.; Labuda, C. J.; Koblish, M.; Little, P. J.; Brogdon, B. L.; Smith, S. A.; Dolle, R. E. Bioorg. Med. Chem. Lett. 2010, 20, 387-391.

Discovery of N-(3-morpholinomethyl)phenyl)amides as potent and selective CB2 agonists. Worm, K.; Weaver, D. G.; Green, R. C.; Saeui, C. T.; Dulay, D.-M. S.; Baker, W. M.; Cassel, J. A.; Stabley, G. J.; DeHaven, R. N.; LaBuda, C. J.; Koblish, M.; Brogdon, B. L.; Smith, S. A.; Dolle, R. E. Bioorg. Med. Chem. Lett. 2009, 19, 5004-5008.

Nascent structure-activity relationship study of a diastereomeric series of kappa opioid receptor antagonists derived from CJ-15,208. Dolle, R. E.; Michaut, M.; Martinez-Teipel, B.; Seida, P. R.; Ajello, C. W.; Muller, A. L.; DeHaven, R. N.; Carroll, P. J. Bioorg. Med. Chem. Lett. 2009, 19, 3647-3650.

Design and synthesis of imidazopyrimidine derivatives as potent iNOS dimerization inhibitors. Chu, G.-H.; Le Bourdonnec, B.; Gu, M.; Ajello, C. W.; Leister, L. K.; Sellitto, I.; Cassel, J. A.; Tuthill, P. A.; O’Hare, H.; DeHaven, R. N.; Dolle, R. E. Open Med. Chem. J. 2009, 3, 8-13.

N-Alkylation-intramolecular Michael addition: new reaction manifold for high throughput annulation of amines. MacLeod, C.; Tuthill, P. A.; Dolle, R. E. Synlett 2009, 2857-2861.

Combined solution-phase and solid-phase synthesis of 2-amino-7,8-dihydropteridin-6(5H)-ones. Metzger, A.; Qin, L.-Y.; Cole, A. G.; Saionz, K. W.; Brescia, M.-R.; Gstach, H.; Wareing, J. R.; Zimmermann, J.; Brill, W. K.-D.; Baldwin, J. J.; Dolle, R. E.; Henderson, I. Tetrahedron Lett. 2009, 50, 7082-7085.

High-performance liquid chromatographic enantioseparation of methanobenzazocines. Barker, W. M.; Worm, K.; Dolle, R. E. J. Chromatog. A 2009, 1216, 7708-7714.

Novel pyridine derivatives as potent and selective CB2 cannabinoid receptor antagonists. Chu, G.-H.; Saeui, C. T.; Worm, K.; Weaver, D. G.; Goodman, A. J.; Broadrup, R. L.; Cassel, J. A.; DeHaven, R. N.; LaBuda, C. J.; Koblish, M.; Brogdon, B.; Smith, S. A.; Le Bourdonnec, B.; Dolle, R. E. Bioorg. Med. Chem. Lett. 2009, 19, 5931-5935.

CB2 selective sulfamoyl benzamides: optimization of the amide functionality. Goodman, A. J.; Ajello, C. W.; Worm, K.; Le Bourdonnec, B.; Savolainen, M. A.; O’Hare, H.; Cassel, J. A.; Stabley, G. J.; DeHaven, R. N.; LaBuda, C. J.; Koblish, M.; Little, P. J.; Brogdon, B. L.; Smith, S. A.; Dolle, R. E. Bioorg. Med. Chem. Lett. 2009, 19, 309-313.

Sulfonamido-aryl ethers as bradykinin B1 receptor antagonists. Cole, A. G.; Metzger, A.; Brescia, M.-R.; Qin, L.-Y.; Appell, K. C.; Brian, C. T.; Hallett, A.; Ganju, P.; Denholm, A. A.; Wareing, J. R.; Richie, T. J.; Drake, G. M.; Bevan, S. J.; MacGloinn, A.; McBryde, A.; Patel, V.; Oakly, P. J.; Nunez, X.; Gstach, H.; Schneider, P.; Baldwin, J. J.; Dolle, R. E.; McDonald, E.; Henderson, I. Bioorg. Med. Chem. Lett. 2009, 19, 119-122.

General and efficient synthetic approach to novel tricyclic spiroketones. Chu, G.-H.; Le Bourdonnec, B.; Gu, M.; Saeui, C. T.; Dolle, R. E. Tetrahedron 2009, 65, 5161-5167.

Spirocyclic delta opioid receptor agonists for the treatment of pain: discovery of N,N-diethyl-3-4(spiro[chromene-2,4′-piperidine]-4-yl)benzamide (ADL5747). Le Bourdonnec, B.; Windh, R. T.; Leister, L. K. Zhou, Q. J.; Ajello, C. W.; Gu. M.; Chu, G.-H.; Tuthill, P. A.; Barker, W. M.; Koblish, M.; Wiant, D. D.; Graczyk, T. M.; Belanger, S.; Cassel, J. A.; Feschenko, M. S.; Brogdon, B. L.; Smith, S. A.; Derelanko, M. J.; Kutz, S.; Little, P. J.; DeHaven, R. N.; DeHaven-Hudkins, D. L.; Dolle, R. E. J. Med. Chem. 2009, 52, 5685-5702.

Comprehensive survey of chemical libraries for drug discovery and chemical biology: 2008. Dolle, R. E.; Le Bourdonnec, B.; Goodman, A. J.; Morales, G. A.; Thomas, C. J.; Zhang, W. J. Combin. Chem. 2009, 11, 739-790.

Simultaneous optimization of potency, selectivity and physicochemical properties for cannabinoid CB2 ligands. Worm, K.; Dolle, R. E. Curr. Pharm. Design 2009, 15, 3345-3366.

Sulfamoyl benzamides as novel CB2 cannabinoid receptor ligands. Worm, K.; Zhou, Q. J.; Saeui, C. T.; Green, R. C.; Cassel, J. A.; Stabley, G. J.; DeHaven, R. N.; Conway-James, N.; LaBuda, C. J.; Koblish, M.; Little, P. J.; Dolle, R. E. Bioorg. Med. Chem. Lett. 2008, 18, 2830-2835.

Novel trans-3,4-dimethyl-4-(3-hydroxyphenyl)piperidines as mu opioid receptor antagonists with improved opioid receptor selectivity profiles. Le Bourdonnec, B.; Barker, W. M.; Belanger, S.; Wiant, D. D.; Conway-James, N. C.; Cassel, J. A.; O’Neill, T. J.; Little, P. J.; DeHaven, R. N.; DeHaven-Hudkins, D. L.; Dolle, R. E. Bioorg. Med. Chem. Lett. 2008, 18, 2006-2012.

Potent, orally bioavailable delta opioid receptor agonists for the treatment of pain: discovery of N,N-diethyl-4-(5-hydroxyspiro[chromene-2,4′-piperidine]-4-yl)benzamide (ADL5859). Le Bourdonnec, B.; Windh, R. T.; Ajello, C. W.; Leister, L. K.; Gu. M.; Chu, G.-H.; Tuthill, P. A.; Barker, W. M.; Koblish, M.; Wiant, D. D.; Graczyk, T. M.; Belanger, S.; Cassel, J. A.; Feschenko, M. S.; Brogdon, B. L.; Smith, S. A.; Christ, D. D.; Derelanko, M. J.; Kutz, S.; Little, P. J.; DeHaven, R. N.; DeHaven-Hudkins, D. L.; Dolle, R. E. J. Med. Chem. 2008, 51, 5893-5896.

Comprehensive survey of chemical libraries for drug discovery and chemical biology: 2007. Dolle, R. E.; Le Bourdonnec, B.; Goodman, A. J.; Morales, G. A.; Thomas, C. J.; Zhang, W. J. Combin. Chem. 2008, 10, 739-790.

Discovery of a series of aminopiperidines as novel iNOS inhibitors. Le Bourdonnec, B.; Leister, L. K.; Ajello, C. A.; Cassel, J. A.; Seida, P. R.; O’Hare, H.; Gu, M.; Chu, G.-H.; Tuthill, P. A.; DeHaven, R. N.; Dolle, R. E. Bioorg. Med. Chem. Lett. 2008, 18, 336-343.

Biaryl cannabinoid mimetics: synthesis and structure-activity relationship. Worm, K.; Zhou, Q. J.; Stabley, G. J.; DeHaven, R. N.; Dolle, R. E. Bioorg. Med. Chem. Lett. 2007, 17, 3652-3656.

Further studies of tyrosine surrogates in opioid receptor peptide ligands. Dolle, R. E.; Michaut, M.; Martinez-Teipel, B.; Belenger, S.; Graczyk, T. M.; DeHaven, R. N. Bioorg. Med. Chem. Lett. 2007, 17, 2656-2660.

Novel malonamide derivatives as potent kappa opioid receptor agonists. Chu, G.-H.; Gu. M.; Cassel, J. A.; Belander, S.; Graczyk, T. M.; DeHaven, R. N. Conway-James, N.; Koblish, M.; Little, P. J.; DeHaven-Hudkins, D. L.; Dolle, R. E. Bioorg. Med. Chem. Lett. 2007, 17, 1951-1955.

Comprehensive survey of chemical libraries for drug discovery and chemical biology: 2006. Dolle, R. E.; Le Bourdonnec, B.; Goodman, A. J.; Morales, G. A.; Salvino, J. M.; Zhang, W. J. Combin. Chem. 2007, 9, 739-790.

Mu opioid receptor antagonists: recent developments. Goodman, A. J.; Le Bourdonnec, B.; Dolle, R. E. ChemMedChem 2007, 2, 1552-1570.

Annulation of primary amines to piperazines and diazaspirocycles utilizing alpha-methyl benzyl resin. MacLeod C.; Martinez-Teipel, B. I.; Barker, W. M.; Dolle, R. E. J. Combin. Chem. 2006, 8, 132-140.

Synthesis and structure-activity relationships of a new series of 2alpha-substituted trans-4,5-dimethyl-4-(3-hydroxyphenyl)piperidine as mu-selective antagonists. Le Bourdonnec, B.; Goodman, A. J.; Michaut, M.; Ye, H. F.; Graczyk, T. M.; Belanger, S.; DeHaven, R. N.; Dolle, R. E. Bioorg. Med. Chem. Lett. 2006, 16, 864-868.

Novel phenylamino acetamide derivatives as potent and selective kappa opioid receptor ligands. Chu, G.-H.; Gu, M.; Cassel, J. A.; Belanger, S.; Stabley, G. J.; DeHaven, R. N.; Conway-James, N.; Koblish, M.; Little, P. J.; DeHaven-Hudkins, D. L.; Dolle, R. E. Bioorg. Med. Chem. Lett. 2006, 16, 645-648.

Antinociceptive activity of the selective iNOS inhibitor ARC-102222 in rodent models of inflammatory, neuropathic and post-operative pain. LaBuda, C. J.; Koblish, M.; Tuthill, P.; Dolle, R. E.; Little, P. J. Eur. J. Pain 2006, 10, 505-512.

Comprehensive survey of combinatorial library synthesis: 2005. Dolle, R. E.; Le Bourdonnec, B.; Morales, G. A.; Moriarty, K. J.; Salvino, J. M. J. Combin. Chem. 2006, 8, 597-635.

Elucidation of the bioactive conformation of the N-substituted trans-3,4-dimethyl-4-(3-hydroxyphenyl)piperidine class of mu opioid receptor antagonists. Le Bourdonnec, B.; Goodman, A. J.; Michaut, M.; Ye, H. F.; Graczyk, T. M.; Belanger, S.; Herbertz, T.; Yap, G. P. A.; DeHaven, R. N.; Dolle, R. E. J. Med. Chem. 2006, 49, 7278-7289.

Synthesis and pharmacological evaluation of novel octahydro-1H-pyrido[1,2-a]pyrazine as mu opioid receptor antagonists. Le Bourdonnec, B.; Goodman, A. J.; Graczyk, T. M.; Belanger, S.; Seida, P. R.; DeHaven, R. N.; Dolle, R. E. J. Med. Chem. 2006, 49, 7290-7306.

Potent and highly selective kappa opioid receptor agonists incorporating chroman- and 2,3-dihydrobenzofuran-based constraints. Chu, G.-H.; Gu, M.; Cassel, J. A.; Belanger, S.; Graczyk, T. M.; DeHaven, R. N.; Conway-James. N.; Koblish, M.; Little, P. J.; DeHaven-Hudkins. D. L.; Dolle, R. E. Bioorg. Med. Chem. Lett. 2005, 15, 5114-5119.

Arylacetamide kappa opioid receptor agonists with reduced cytochrome P450 2D6 inhibitory activity. Le Bourdonnec, B.; Ajello, C. W.; Seida, P. R.; Susnow, R. G.; Cassel, J. A.; Belanger, S.; Stabley, G. J.; DeHaven, R. N.; DeHaven-Hudkins, D. L.; Dolle, R. E. Bioorg. Med. Chem. Lett. 2005, 15, 2647-2652.

Solid/solution-phase annulation reagents: single-step synthesis of cyclic amine derivatives. Dolle, R. E.; MacLeod, C.; Martinez-Teipel, B. I.; Barker, W. M.; Seida, P.; Herbetz, T. Angew. Chem., Int. Ed. 2005, 44, 5830-5833.

Comprehensive survey of combinatorial library synthesis: 2004. Dolle, R. E. J. Combin. Chem. 2005, 7, 739-798.

10-Hydroxy-10,9-boroxarophenenthrenes: versatile synthetic intermediates to 3,4-benzocoumarins and triaryls. Zhou, Q. J.; Worm, K.; Dolle, R. E. J. Org. Chem. 2004, 69, 5147-5149.

Development of a new alpha-aminonitrile synthesis. Chu, G.-H.; Gu, M.; Gerard, B.; Dolle, R. E. Syn. Commun. 2004, 34, 4583-4590.

Peripherally restricted opioid agonists as novel analgesic agents. DeHaven-Hudkins, D. L.; Dolle, R. E. Curr. Pharm. Design 2004,10, 743-757.

Small molecule biaryl FSH receptor agonists. Part 1. Lead discovery via encoded combinatorial synthesis. Guo, T.; Adang, A. E. P.; Dolle, R. E.; Dong, G.; Fitzpatrick, D.; Geng, P.; Ho, K. K.; Kultgen, S. G.; Liu, R.; McDonald, E.; McGuinness, B. F.; Saionz, K. W.; Valenzano, K. J.; van Straten, N. C. R.; Xie, D.; Webb, M. L. Bioorg. Med. Chem. Lett. 2004, 14, 1713-1716.

(4-Carboxamido)phenylalanine is a surrogate for tyrosine in opioid receptor peptide ligands. Dolle, R. E.; Machaut, M.; Martinez-Teipel, B.; Belanger, S.; Cassel, J. A.; Stabley, G. J.; Graczyk, T. M.; DeHaven, R. N. Bioorg. Med. Chem. Lett. 2004, 14, 3545-3548.

Azepinone as a conformational constraint in the design of kappa receptor agonists. Tuthill, P. A.; Seida, P. R.; Barker, W.; Cassel, J. A.; Belanger, S.; DeHaven, R. N.; Koblish, M.; Gorrshall, S. L.; Little, P. J.; DeHaven-Hudkins, D. L.; Dolle, R. E. Bioorg. Med. Chem. Lett. 2004, 14, 5693-5697.

Comprehensive survey of combinatorial library synthesis: 2003. Dolle, R. E. J. Combin. Chem. 2003, 6, 623-679.

trans-3,4-Dimethyl-4-(3-carboxamidophenyl)piperidines: a novel class of mu-selective opioid antagonists. Le Bourdonnec, B.; Belanger, S.; Cassel, J. A.; Stabley, G. J.; DeHaven, R. N.; Dolle, R. E. Bioorg. Med. Chem. Lett. 2003, 13, 4459-4462.

Comprehensive survey of combinatorial library synthesis: 2002. Dolle, R. E. J. Combin. Chem. 2003, 5, 693-753.

The solid-phase synthesis and use of N-monosubstituted piperazines in chemical library synthesis. Salvino, J. M.; Baudouin, G.; Fen, Y. H.; Berengere, S.; Dolle, R. E. J. Combin. Chem. 2003, 5, 260-266.

Comprehensive survey of combinatorial library synthesis: 2001. Dolle, R. E. J. Combin. Chem. 2002, 4, 369-418.

Solid-phase synthesis of -hydroxy phosphonates and hydroxystatine amides. Transition-state isosteres derived from resin-bound amino acid aldehydes. Dolle, R. E.; Herpin, T. F.; Shimshock, Y. C. Tetrahedron Lett. 2001, 42, 1855-1858.

Comprehensive survey of combinatorial library synthesis: 2000. Dolle, R. E. J. Combin. Chem. 2001, 3, 477-517.

Allosteric inhibitors of inducible nitric oxide synthase dimerization discovered via combinatorial chemistry. McMillan, K.; Adler, M.; Auld, D. S.; Baldwin, J. J.; Blasko, E.; Browne, L. J.; Chelsky, D.; Davey, D.; Dolle, R. E.; Eagen, K. A.; Erickson, S.; Feldman, R. I.; Glaser, C. B.; Mallari, C.; Morrissey, M. M.; Ohlmeyer, M. H. J.; Pan, G.; Parkinson, J. F.; Phillips, G. B.; Polokoff, M. A.; Sigal, N. H.; Vergona, R.; Whitlow, M.; Young, T. A.; Devlin, J. J. Proc. Natl. Acad. Sci. U.S.A. 2000, 97, 1506-1529.

Comprehensive survey of combinatorial library synthesis: 1999. Dolle, R. E. J. Combin. Chem. 2000, 2, 383-433.

A statistical-based approach to assessing the fidelity of combinatorial libraries encoded with electrophoric molecular tags. Development and application of tag decode-assisted single bead LC/MS analysis. Dolle, R. E.; Guo, J.; O’Brien, L.; Jin, Y.; Piznik, M.; Bowman, K. J.; Li, W.; Egan, W. J.; Cavallaro, C. L.; Roughton, A. L.; Zhao, Q.; Reader, J. C.; Orlowski, M.; Jacob-Samuel, B.; Dilanni-Carroll, C. J. Comb. Chem. 2000, 2, 716-731.

Comprehensive survey of combinatorial library with undisclosed biological activity: 1992-1997. Dolle, R. E. Mol. Diversity 2000, 4, 233-256.

Analysis of libraries encoded with GC tags: compound elution, tag decode analysis, and statistical sampling analysis. Dolle, R. E.; Li, W.; Guo, J.; Zhao, N.; Connelly, J. A. Mol. Diversity 2000, 5, 35-49.

Allylindium and allylboronic acid pinacolate: mild reagents for the allylation of resin-bound aldehydes. Application to the solid-phase synthesis of hydroxypropylamines. Cavallaro, C. L.; Herpin, T.; McGuinness, B. F.; Shimshock, Y. C.; Dolle, R. E. Tetrahedron Lett. 1999, 40, 2711-2714.

Application of the intramolecular azomethine imine cycloaddition to the construction of a novel, orthogonally protected spirodiamino acid scaffold. Dolle, R. E.; Barden M. C.; Brennan, P. E.; Ahmed, G.; Tran, V.; Ho, D. M. Tetrahedron Lett. 1999, 40, 2907-2908.

Small molecule antagonists of the bradykinin B1 receptor. Horlick, R. A.; Ohlmeyer, M. H.; Stroke, I. L.; Strohl, B.; Pan, G.; Schilling, A.; Paradkar, V.; Quintero, J. G.; You, M.; Riviello, C.; Thorn, M. B.; Damaj, B.; Fitzpatrick, V. D.; Dolle, R. E.; Webb, M. L.; Baldwin, J. J.; Sigal, N. H. Immunopharm. 1999, 43, 169-177.

Comprehensive survey of combinatorial library synthesis: 1998. Dolle, R. E.; Nelson, K. H., Jr. J. Combin. Chem. 1999, 1, 235-282.

Comprehensive survey of chemical libraries yielding enzyme inhibitors, receptor agonists and antagonists, and other biologically active agents. Dolle, R. E. Mol. Diversity 1998, 3, 199-233.

Identification of potent inhibitors of Plasmodium falciparum plasmepsin II from an encoded statine combinatorial library. Carroll, C. D.; Patel, H.; Johnson, T. O.; Guo, T.; Orlowski, M.; He, Z. M.; Cavallaro, C. L.; Guo, J.; Oksman, A.; Gluzman, I. Y.; Connelly, J.; Chelsky, D.; Goldberg, D. E.; Dolle, R. E. Bioorg. Med. Chem. Lett. 1998, 8, 2315-2320.

Evaluation of a structure-based statine cyclic diamino amide encoded combinatorial library against plasmepsin II and cathepsin D. Carroll, C. D.; Johnson, T. O.; Tao, S.; Lauri, G.; Orlowski, M.; Gluzman, I. Y.; Goldberg, D. E.; Dolle, R. E. Bioorg. Med. Chem. Lett. 1998, 8, 3203-3206.

ATP-citrate lyase as a target for hypolipidemic intervention. 2. Synthesis and evaluation of (3R*,5S*)--substituted-3-carboxy-3,5-dihydroxyalkanoic acids and their -lactone prodrugs as inhibitors of the enzyme in vitro and in vivo. Gribble, A. D.; Ife, R. J.; Shaw, A.; McNair, D.; Novelli, C.E.; Bakewell, S.; Shaw, V. P.; Dolle, R. E.; Groot, P. H.; Pearce, N.; Yates, J.; Tew, D.; Boyd, H.; Ashman, S.; Eggleston, D. S.; Haltiwanger, R. C.; Okafo, G. J. Med. Chem. 1998, 41, 3582-3595.

-((Tetronoyl)oxy) and -((tetramoyl)oxy)methyl ketone inhibitors of the interleukin-1converting enzyme (ICE). Graybill, T. L.; Prouty, C. P.; Speier, G. J.; Hoyer, D.; Dolle, R. E.; Helaszek, C. T.; Ator, M. A.; Uhl, J.; Straster, J. Bioorg. Med. Chem. Lett. 1997, 7, 41-46.

Pyridazinodiazepines as a high-affinity, P2-P3 peptidomimetic class of interleukin-1 converting enzyme inhibitor. Dolle, R. E.; Prasad, C. V. C.; Prouty, C. P.; Salvino, J. M.; Awad, M. M. A.; Schmidt, S. J.; Hoyer, D.; Ross, T. M.; Graybill, T. L.; Speier, G.; Uhl, J.; Miller, R.; Helaszek, C. T.; Ator, M. A. J. Med. Chem. 1997, 40, 1941-1946.

3-Chloro-4-carboxamido-6-arylpyridazines as a nonpeptide class of interleukin-1 converting enzyme inhibitor. Dolle, R. E.; Hoyer, D.; Rinker, J. M.; Ross, T. M.; Schmidt, S. J.; Helaszek, C.; Ator, M. A. Bioorg. Med. Chem. 1997, 7, 1003-1006.

Discovery of enzyme inhibitors through combinatorial chemistry. Dolle, R. E. Mol. Diversity 1997, 2, 223-236.

First examples of peptidomimetic inhibitors of interleukin-1 converting enzyme. Dolle, R. E.; Prouty, C. P.; Prasad, C. V. C.; Cook, E.; Saha, A.; Ross, T. M.; Salvino, J. M.; Helaszek, C. T.; Ator, M. A. J. Med. Chem. 1996, 39, 2438-2440.

ATP-citrate lyase as a target for hypolipidemic intervention. 1. Design and synthesis of 2-substituted butane-1,4-dioic acids as novel, potent inhibitors of the enzyme. Gribble, A. D.; Dolle, R. E.; Shaw, A.; McNair, D.; Novelli, R.; Novelli, C. E.; Slingsby, B. P.; Shah, V. P.; Tew, D.; Saxty, B. A.; Allen, M.; Groot, P. H.; Pearce, N.; Yates, J. J. Med. Chem. 1996, 39, 3569-3584.

Synthesis of novel thiol-containing citric acid analogs. Kinetic evaluation of these and other potential active-site-directed and mechanism-based inhibitors of ATP-citrate lyase. Dolle, R. E.; Gribble, A.; Wilkes, T. K.; Kruse, L. I.; Eggelston, D.; Saxty, B. A.; Wells, T. N. C.; Groot, P. H. E. J. Med. Chem. 1995, 38, 537-543.

Structural and stereochemical requirements of time-dependent inactivators of the interleukin-1β converting enzyme. Prasad, C. V. C.; Prouty, C. P.; Hoyer, D.; Ross,. T. M.; Salvino, J. M.; Awad, M.; Graybill, T. L.; Schmidt, S. J.; Osifo, K. I.; Dolle, R. E.; Helaszek, C. T.; Miller, R. E..; Ator, M. A. Bioorg. Med. Chem. Lett. 1995, 5, 315-318.

Pharmacology and structure-activity relationships of the nonpeptide bradykinin receptor antagonist WIN 64338. Sawutz, D. G.; Salvino, J. M.; Dolle, R. E.; Seoane, P. R.; Farmer, S. G. Can. J. Physiol. Pharmacol. 1995, 73, 805-811.

Aspartyl -((diphenylphosphinyl)oxy)methyl ketones as novel inhibitors of interleukin-1 converting enzyme. Utility of the diphenylphosphinic acid leaving group for the inhibition of cysteine proteases. Dolle, R. E.; Singh, J.; Whipple D.; Osifo, I. K.; Speier, G.; Graybill, T. L.; Gregory, J. S.; Harris A. L.; Helaszek, C. T.; Miller, R. E.; Ator, M. A. J. Med. Chem. 1995, 28, 220-222.

Inhibition of mature IL-1 production in murine macrophages and a murine model of inflammation by WIN 67694, an inhibitor of IL-1 converting enzyme. Miller, B. E.; Krasney, P. A.; Gauvin, B. M.; Holbrook, K. B.; Koonz, D. J.; Abruzzese, R. V.; Miller, R. E.; Pagani, K. A.; Dolle, R. E. J. Immunol. 1995, 154, 1331-1338.

CD45 protein tyrosine phosphatase: determination of minimal peptide length for substrate recognition and synthesis of some tyrosine-based electrophiles as potential active-site directed irreversible inhibitors. Bobko, M.; Wolfe, H. R.; Saha, A.; Dolle, R. E.; Fisher, D. K.; Higgins, T. J. Bioorg. Med. Chem. Lett. 1995, 5, 353-356.

Characterization of a continuous fluorogenic assay for calpain 1. Kinetic evaluation of peptide aldehydes, halomethyl ketones and (acyloxy)methyl ketones as inhibitors of the enzyme. Harris, A. L.; Gregory, J. S.; Maycock, A. L.; Graybill, T. L.; Osifo, I. K.; Schmidt, S. J.; Dolle, R. E. Bioorg. Med. Chem. Lett. 1995, 5, 393-398.

Synthesis of nonpeptide bradykinin B2 receptor antagonists. Douty, B. D.; Salvino, J. M.; Seoane, P. R.; Dolle. R. E. Bioorg. Med. Chem. Lett. 1995, 5, 363-366.

Inhibition of human erythrocyte calpain 1 by novel quinolinecarboxamides. Graybill, T. L.; Dolle, R. E.; Osifo, I. K.; Schmidt, S. J.; Gregory, J. S.; Harris, A. L.; Miller, M. S. Bioorg. Med. Chem. Lett. 1995, 5, 387-392.

ACE inhibitors as a template for the design of bradykinin B2 receptor antagonists. Hoyer, D.; Awad, M. M. A.; Salvino, J. M.; Seoane, P. R.; Dolle. R. E.; Houck, W. T.; Sawutz, D. G. Bioorg. Med. Chem. Lett. 1995, 5, 367-370.

Structure-activity relationships of nonpeptide bradykinin B2 receptor antagonists. Salvino, J. M.; Seoane, P. R.; Douty, B. D.; Awad, M. M. A.; Hoyer, D.; Ross, T. M.; Dolle, R. E.; Houck, W. T.; Faunce, D. M.; Sawutz, D. G. Bioorg. Med. Chem. Lett. 1995, 5, 357-362.

Secretion of human monocyte mature IL-1: optimization of culture conditions and inhibition by ICE inhibitors. Uhl, J.; Krasney, P.; Brophy, L.; Arnold, R.; Dolle, R. E.; Helaszek, C.; Miller, R.; Gilman, S.; Ator, M. Inflammation Res. 1995, 44 (suppl. 2), S211-S212.

Approach to the discovery of novel, selective inhibitors of p56lck tyrosine kinase: Identification of non-hydroxylated chromones as p56lck inhibitors. Miller, D.; Wang, S.; Reid, J.; Xie, W.; Gauvin, B.; Kelley, M.; Sarup, J.; Sawutz, D. G.; Miski, M.; Dolle, R. E.; Faltynek, C. R. Drug Dev. Res. 1995, 34, 344-352.

Synthesis and evaluation of diacylhydrazines as inhibitors of the interleukin-1 converting enzyme (ICE). Graybill, T. L.; Dolle, R. E.; Helaszek, C. T.; Ator, M. A.; Strasters, J. Bioorg. Med. Chem. Lett. 1995, 5, 1197-1202.

Interleukin-1 converting enzyme: biology and the chemistry of inhibitors. Ator, M. A.; Dolle. R. E. Curr. Pharm. Res. 1995, 1, 191-210.

Preparation and evaluation of peptidic aspartyl hemiacetals as reversible inhibitors of interleukin-1 converting enzyme. Graybill, T. L.; Dolle, R. E.; Helaszek, C. T.; Miller, R. E.; Ator, M. A. Int. J. Pept. Protein Res. 1994, 44, 173-182.

P1 aspartate-based peptide -((2,6-dichlorobenzoy)oxy)methyl ketones as potent time-dependent inhibitors of interleukin-1 converting enzyme. Dolle, R. E.; Hoyer, D.; Ross, T. M.; Prasad, C. V. C.; Schmidt, S. J.; Helaszed, C. T.; Miller, R. E.; Ator, M. A. J. Med. Chem. 1994, 37, 563-564.

Synthesis, characterization, and conformational analysis of the [D/L-Tic7] stereoisomers of bradykinin receptor antagonist D-Arg0[Hyp3, Thi5, D-Tic7, Oic8]bradykinin. Sawutz, D. G.; Salvino, J. M.; Seaone, P. R.; Douty, B. D.; Houck, W. T.; Bobko, M. A.; Doleman, M. S.; Dolle, R. E.; Wolfe, H. R. Biochemistry 1994, 33, 2373-2379.

The nonpeptide WIN 64338 is a bradykinin B2 receptor antagonist. Sawutz, D. G.; Salvino, J. M.; Dolle, R. E.; Casiano, F.; Ward, S. J.; Houck, W. T.; Faunce, D. M.; Douty, B. D.; Baizman, E. Proc. Natl. Acad. Sci. 1994, 91, 4693-4697.

5,7-Dimethoxy-3-(pyridinyl)quinoline is a potent and selective inhibitor of human vascular beta-type platelet-derived growth factor receptor tyrosine kinase. Dolle, R. E.; Dunn, J. A.; Bobko, M.; Singh, B.; Kuster, J. E.; Baizman, E.; Harris, A. L.; Sawutz, D. G.; Miller, D.; Wang, S.; Faltynek, C. R.; Xie, W.; Sarup, J.; Bode, D. C.; Pagani, E. D.; Silver, P. J. J. Med. Chem. 1994, 37, 2627-2629.

Aspartyl -((1-phenyl-3-trifluoromethyl)pyrazol-5-yl)oxy)methyl ketones as interleukin-1 converting enzyme inhibitors. Significance of the P1 and P3 amido nitrogens for enzyme-peptide inhibitor binding. Dolle, R. E.; Singh, J.; Rinker, J.; Hoyer, D.; Prasas, C. V. C.; Graybill T. L.; Salvino, J. M.; Helaszek, C. T.; Miller, R. E.; Ator, M. A. J. Med. Chem. 1994, 37, 3863-3866.

9-(Sulfoximinoalkyl)guanine nucleosides as potential antiherpetic agents. Dolle, R. E.; McNair, D. Tetrahedron Lett. 1993, 34, 133-136.

Design of potent nonpeptide competitive antagonists of the human bradykinin B2 receptor. Salvino, J. M.; Seoane, P. R.; Douty, B. D.; Awad, M. M. A.; Dolle. R. E.; Houck, W. T.; Faunce, D. M.; Sawutz, D. G. J. Med. Chem. 1993, 36, 2583-2584.

Synthesis, specificity, and antifungal activity of inhibitors of the Candida albicans ∆24-sterol methyltransferase. Ator, M. A.; Schmidt, S. J.; Adams, J. L.; Dolle, R. E.; Kruse, L. I.; Frey, C. L.; Barone, J. M. J. Med. Chem. 1992, 35, 100-106.

Enantiospecific synthesis of (-)-tabtoxinine -lactam. Dolle, R. E.; Li, C.-S.; Novelli, R.; Kruse, L. I.; Eggleston, D. J Org. Chem. 1992, 57, 128-132.

Synthesis and evaluation of (+)- and (-)-2,2-difluorocitrate as inhibitors of rat-liver ATP-citrate lyase and porcine-heart aconitase. Saxty, B. A.; Novelli, R.; Dolle. R. E.; Kruse, L. I.; Reid, D. G.; Camilleri, P.; Wells T. N. C. Eur. J. Biochem. 1992, 202, 889-896.

ATP-citrate lyase as a target for hypolipidemic intervention. Sulfoximine and 3-hydroxy--lactam-containing analogues of citric acid as potential tight-binding inhibitors. Dolle, R. E.; McNair, D.; Houghes, M. J.; Kruse, L. I.; Eggelston, D.; Saxty, B. A.; Wells, T. N. C.; Groot, P. H. E. J. Med. Chem. 1992, 35, 4875-4884.

Synthesis and evaluation of azapeptide-derived inhibitors of serine and cysteine proteases. Graybill, T. L.; Ross, M. J.; Gauvin, B. R.; Gregory, J. S.; Harris, A. L.; Ator, M. A.; Rinker, J. M.; Dolle, R. E. Bioorg. Med. Chem. Lett. 1992, 2, 1375-1380.

Conformational analysis of bradykinin by annealed molecular dynamics and comparison to NMR derived conformations. Salvino, J. S.; Seoane, P. R.; Dolle, R. E. J. Comp. Chem. 1992, 14, 438-444.

Synthesis of saclophen: a putative GABAB antagonist. Li, C.-S.; Howson, W.; Dolle. R. E. Synthesis 1991, 244.

Enantioselective synthesis of (+)-pinidine. Dolle, R. E.; Osifo, K. I.; Li, C-S. Tetrahedron Lett. 1991, 32, 5029-5030.

Design and synthesis of 14-methyl-14-D-homo-azasterols as novel antimycotics. Dolle, R. E.; Allaudeen, H. S.; Kruse, L. I. J. Med. Chem. 1990, 33, 877-880.

Design and synthesis of a series of glycerol-derived receptor mediated calcium entry (RMCE) blockers. Howson, W.; Armstrong, W. P.; Cassidy, K.; Novelli, R.; Tchorzewska, M. A.; Jaxa-Chamiec, A.; Dolle, R. E.; Hallam, T. J.; Leigh, B. K.; Merritt, J. E.; Moores, K. E.; Rink, T. J. Eur. J. Med. Chem. 1990, 25, 595-602.

Enantioselective synthesis of (+)-(2S,3S)-3-ethynyltyrosine. Shaw, A. N.; Dolle, R. E.; Kruse, L. I. Tetrahedron Lett. 1990, 31, 5081-5081.

Preparation of (+)-(erythro)-and (+)-(threo)-2-vinyl citric acids as potential mechanism-based inhibitors of ATP-citrate lyase. Dolle, R. E.; Novelli, R.; Saxty, B. A.; Wells, T. N. C.; Kruse, L. I.; Camilleri, P.; Eggleston, D. Tetrahedron Lett. 1990, 32, 4587-4590.

Synthesis of zymosterol, fecosterol and related biosynthetic sterol intermediates. Dolle, R. E.; Schmidt, S. J.; Erhard, K. F.; Kruse, L. I. J. Am. Chem. Soc. 1989, 111, 278-284.

3-Aminopropylphosphinic acid: a potent selective GABAB receptor agonist in the guinea pig ileum and rat anococcygeus. Hills, J. M.; Dingsdale, R. A.; Parsons, M. E.; Howson, W.; Dolle, R. E. Br. J. Pharmacol. 1989, 97, 1292-1296.

Concomitant [2,3]-sigmatropic rearrangement of allylic sulfilimines and intramolecular N-alkylation. Synthesis of 2-vinyl substituted cyclic amines. Dolle, R. E.; Li, C-S.; Shaw, A. N. Tetrahedron Lett. 1989, 30, 4723-4726.

Preparation and alkylation of N-tert-butyldimethylsilyl-3-trimethylsilyloxyazetidin-2-one. Dolle, R. E.; Hughes, M. J.; Li, C.-S.; Kruse, L. I. J. Chem. Soc., Chem. Commun. 1989, 1448-1449.

Mechanisms and inhibition of ∆24-sterol methyltransferase from Candida albicans and Candida tropicalis. Ator, A.; Schmidt, J.; Adams, J.; Dolle, R. E. Biochemistry 1989, 28, 9633-9640.

Separation of the enantiomers of difluorocitrate. Camilleri, P.; Novelli, R.; Dolle, R. E.; Sulter, S. J. Chromatogr. B 1989, 482, 258-261.

Synthesis of zymosterol: salient intermediate fungal and mammalian sterol biosynthesis. Dolle, R. E.; Schmidt, S. J.; Kruse, L. I. J. Chem. Soc., Chem. Commun. 1988, 19-21.

Synthesis of antifungal antibiotic A25822 Factor A. Dolle, R. E.; Kruse, L. I. J. Chem. Soc., Chem. Commun. 1988, 133-135.

Studies on the acid-catalyzed homonuclear steroidal diene isomerization. Schmidt, S. J.; Dolle, R. E.; Eggleston, E.; Kruse, L. I. J. Org. Chem. 1988, 53, 1563-1566.

Regiocontrolled synthesis of the ergosterol -isomers. Dolle, R. E.; Schmidt, S. J.; Kruse, L. I. Tetrahedron Lett. 1988, 29, 1581-1582.

The copper sites of dopamine β-hydroxylase: an X-ray absorption spectroscopic study. Scott, R. A.; Sullivan, R. J.; DeWolf, Jr., W. E.; Dolle, R. E.; Kruse, L. I. Biochemistry 1988, 27, 5411-5417.

Intramolecular [4+2] cycloaddition of α,β-unsaturated hydrazones as a route to annulated pyridines. Dolle, R. E.; Armstrong, W. P.; Shaw, A. N.; Novelli, R. Tetrahedron Lett. 1988, 29, 6349-6352.

Inactivation of dopamine β-hydroxylase by p-cresol: Isolation and characterization of covalently modified active site peptides. DeWolf, Jr., W. E.; Carr, S. A.; Varrichio, A.; Goodhardt, J. P.; Mentzer, M. A.; Roberts, G. D.; Southan, C. D.; Dolle, R. E.; Kruse, L. I. Biochemistry 1988, 27, 9093-9101.

Palladium-catalyzed alkoxycarbonylation of phenols to benzoate esters. Dolle, R. E.; Schmidt, S. J.; Kruse, L. I. J. Chem. Soc., Chem. Commun. 1987, 904-905.

Improved preparation of (3β,5α,14α)-3-hydroxy-14-methylcholest-7-en-15-one. Synthesis of ergostenone and 20α-(hydroxymethyl)pregnenone analogs. Dolle, R. E.; Kruse, L. I. J. Org. Chem. 1986, 51, 4047-4053.

New technologies for the synthesis of complex natural products. I. Total synthesis of elfamycins: aurodox and efrotomycin. II. Glycosyl fluorides: preparation, reactions and oligosaccharide synthesis. Partial synthesis of avermectin B1a. Dolle, R. E. Univ. Microfilms Int., Order No. DA8515364 Diss. Abstr. Int. B, 1986, 46, 1-623.

Total synthesis of ionophore antibiotic X-14547A. Nicolaou, K. C.; Papahatjis, D. P.; Claremon, D. A.; Magolda, R. L.; Dolle, R. E. J. Org. Chem. 1985, 50, 1440-1456.

Total synthesis of elfamycins: aurodox and efrotomycin. 2. Coupling of key intermediates and completion of the synthesis. Dolle, R. E.; Nicolaou, K. C. J. Am. Chem. Soc. 1985, 107, 1695-1698.

Total synthesis of elfamycins: aurodox and efrotomycin. 1. Strategy and construction of key intermediates. Dolle, R. E.; Nicolaou, K. C. J. Am. Chem. Soc. 1985, 107, 1691-1694.

Carbohydrate-based syntheses of the goldinonolactone and the tetrahydrofuran fragments of aurodox and efrotomycin. Dolle, R. E.; Nicolaou, K. C. J. Chem. Soc., Chem. Commun. 1985, 1016-1018.

A practical synthesis of oligosaccharides. Partial synthesis of avermectin B1a. Nicolaou, K. C.; Dolle, R. E.; Papahatjis, D. P. J. Am. Chem. Soc. 1984, 106, 4189-4192.

A general and stereocontrolled total synthesis of LTB4 and analogs. Nicolaou, K. C.; Zipkin, R. E.; Dolle, R. E.; Harris, B. D. J. Am. Chem. Soc. 1984, 106, 3748-3751.

Reactions of glycosyl fluorides 2. Synthesis of O-, S-, N-, and P-glycosides. Nicolaou, K. C.; Dolle, R. E.; Chucholowski, A.; Randall, J. L. J. Chem. Soc., Chem. Commun. 1984, 1155-1156.

Reactions of glycosyl fluorides 1. Synthesis of C-glycosides. Nicolaou, K. C.; Dolle, R. E.; Chucholowski, A. J. Chem. Soc., Chem. Commun. 1984, 1153-1154.

Total synthesis of ionophore antibiotic X-14547A. Enantioselective synthesis of the tetrahydropyran and tetrahydroindan building blocks. Nicolaou, K. C.; Papahatjis, D. P.; Claremon, D. A.; Dolle, R. E. J. Am. Chem. Soc. 1981, 103, 6967-6969.

Separation of Darvon and APC. Stall, W. J.; Dolle, R. E. Microgram 1978, 11, 204.

Tilidone and mepirizole – two foreign analgesics. Stall, W. J.; Dolle, R. E. Microgram 1978, 11, 197.