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Page 1
Discovery of BMS-641988, a Novel Androgen Receptor Antagonist for the Treatment of Prostate Cancer.
Balog A, Rampulla R, Martin GS, Krystek SR, Attar R, Dell-John J, DiMarco JD, Fairfax D, Gougoutas J, Holst CL, Nation A, Rizzo C, Rossiter LM, Schweizer L, Shan W, Spergel S, Spires T, Cornelius G, Gottardis M, Trainor G, Vite GD, Salvati ME. Balog A, et al. Among authors: spergel s. ACS Med Chem Lett. 2015 Jun 19;6(8):908-12. doi: 10.1021/acsmedchemlett.5b00173. eCollection 2015 Aug 13. ACS Med Chem Lett. 2015. PMID: 26288692 Free PMC article.
Potent and Selective Agonists of Sphingosine 1-Phosphate 1 (S1P1): Discovery and SAR of a Novel Isoxazole Based Series.
Watterson SH, Guo J, Spergel SH, Langevine CM, Moquin RV, Shen DR, Yarde M, Cvijic ME, Banas D, Liu R, Suchard SJ, Gillooly K, Taylor T, Rex-Rabe S, Shuster DJ, McIntyre KW, Cornelius G, D'Arienzo C, Marino A, Balimane P, Warrack B, Salter-Cid L, McKinnon M, Barrish JC, Carter PH, Pitts WJ, Xie J, Dyckman AJ. Watterson SH, et al. Among authors: spergel sh. J Med Chem. 2016 Mar 24;59(6):2820-40. doi: 10.1021/acs.jmedchem.6b00089. Epub 2016 Mar 10. J Med Chem. 2016. PMID: 26924461
Identification and synthesis of potent and selective pyridyl-isoxazole based agonists of sphingosine-1-phosphate 1 (S1P1).
Guo J, Watterson SH, Spergel SH, Kempson J, Langevine CM, Shen DR, Yarde M, Cvijic ME, Banas D, Liu R, Suchard SJ, Gillooly K, Taylor T, Rex-Rabe S, Shuster DJ, McIntyre KW, Cornelius G, D'Arienzo C, Marino A, Balimane P, Salter-Cid L, McKinnon M, Barrish JC, Carter PH, Pitts WJ, Xie J, Dyckman AJ. Guo J, et al. Among authors: spergel sh. Bioorg Med Chem Lett. 2016 May 15;26(10):2470-2474. doi: 10.1016/j.bmcl.2016.03.105. Epub 2016 Apr 1. Bioorg Med Chem Lett. 2016. PMID: 27055941
Biphenylsulfonamide endothelin receptor antagonists. 4. Discovery of N-[[2'-[[(4,5-dimethyl-3-isoxazolyl)amino]sulfonyl]-4-(2-oxazolyl)[1,1'-biphenyl]- 2-yl]methyl]-N,3,3-trimethylbutanamide (BMS-207940), a highly potent and orally active ET(A) selective antagonist.
Murugesan N, Gu Z, Spergel S, Young M, Chen P, Mathur A, Leith L, Hermsmeier M, Liu EC, Zhang R, Bird E, Waldron T, Marino A, Koplowitz B, Humphreys WG, Chong S, Morrison RA, Webb ML, Moreland S, Trippodo N, Barrish JC. Murugesan N, et al. Among authors: spergel s. J Med Chem. 2003 Jan 2;46(1):125-37. doi: 10.1021/jm020289q. J Med Chem. 2003. PMID: 12502366
Imidazoquinoxaline Src-family kinase p56Lck inhibitors: SAR, QSAR, and the discovery of (S)-N-(2-chloro-6-methylphenyl)-2-(3-methyl-1-piperazinyl)imidazo- [1,5-a]pyrido[3,2-e]pyrazin-6-amine (BMS-279700) as a potent and orally active inhibitor with excellent in vivo antiinflammatory activity.
Chen P, Doweyko AM, Norris D, Gu HH, Spergel SH, Das J, Moquin RV, Lin J, Wityak J, Iwanowicz EJ, McIntyre KW, Shuster DJ, Behnia K, Chong S, de Fex H, Pang S, Pitt S, Shen DR, Thrall S, Stanley P, Kocy OR, Witmer MR, Kanner SB, Schieven GL, Barrish JC. Chen P, et al. Among authors: spergel sh. J Med Chem. 2004 Aug 26;47(18):4517-29. doi: 10.1021/jm030217e. J Med Chem. 2004. PMID: 15317463
Discovery of a JAK1/3 Inhibitor and Use of a Prodrug To Demonstrate Efficacy in a Model of Rheumatoid Arthritis.
Spergel SH, Mertzman ME, Kempson J, Guo J, Stachura S, Haque L, Lippy JS, Zhang RF, Galella M, Pitt S, Shen G, Fura A, Gillooly K, McIntyre KW, Tang V, Tokarski J, Sack JS, Khan J, Carter PH, Barrish JC, Nadler SG, Salter-Cid LM, Schieven GL, Wrobleski ST, Pitts WJ. Spergel SH, et al. ACS Med Chem Lett. 2019 Feb 13;10(3):306-311. doi: 10.1021/acsmedchemlett.8b00508. eCollection 2019 Mar 14. ACS Med Chem Lett. 2019. PMID: 30891131 Free PMC article.
Aminodiol HIV protease inhibitors. Synthesis and structure-activity relationships of P1/P1' compounds: correlation between lipophilicity and cytotoxicity.
Chen P, Cheng PT, Alam M, Beyer BD, Bisacchi GS, Dejneka T, Evans AJ, Greytok JA, Hermsmeier MA, Humphreys WG, Jacobs GA, Kocy O, Lin PF, Lis KA, Marella MA, Ryono DE, Sheaffer AK, Spergel SH, Sun CQ, Tino JA, Vite G, Colonno RJ, Zahler R, Barrish JC. Chen P, et al. Among authors: spergel sh. J Med Chem. 1996 May 10;39(10):1991-2007. doi: 10.1021/jm950717a. J Med Chem. 1996. PMID: 8642558
Novel tricyclic inhibitors of IKK2: discovery and SAR leading to the identification of 2-methoxy-N-((6-(1-methyl-4-(methylamino)-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-7-yl)pyridin-2-yl)methyl)acetamide (BMS-066).
Watterson SH, Langevine CM, Van Kirk K, Kempson J, Guo J, Spergel SH, Das J, Moquin RV, Dyckman AJ, Nirschl D, Gregor K, Pattoli MA, Yang X, McIntyre KW, Yang G, Galella MA, Booth-Lute H, Chen L, Yang Z, Wang-Iverson D, McKinnon M, Dodd JH, Barrish JC, Burke JR, Pitts WJ. Watterson SH, et al. Bioorg Med Chem Lett. 2011 Dec 1;21(23):7006-12. doi: 10.1016/j.bmcl.2011.09.111. Epub 2011 Oct 5. Bioorg Med Chem Lett. 2011. PMID: 22018461
Biphenylsulfonamide endothelin antagonists: structure-activity relationships of a series of mono- and disubstituted analogues and pharmacology of the orally active endothelin antagonist 2'-amino-N- (3,4-dimethyl-5-isoxazolyl)-4'-(2-methylpropyl)[1, 1'-biphenyl]-2-sulfonamide (BMS-187308).
Murugesan N, Gu Z, Stein PD, Bisaha S, Spergel S, Girotra R, Lee VG, Lloyd J, Misra RN, Schmidt J, Mathur A, Stratton L, Kelly YF, Bird E, Waldron T, Liu EC, Zhang R, Lee H, Serafino R, Abboa-Offei B, Mathers P, Giancarli M, Seymour AA, Webb ML, Hunt JT, et al. Murugesan N, et al. Among authors: spergel s. J Med Chem. 1998 Dec 17;41(26):5198-218. doi: 10.1021/jm970872k. J Med Chem. 1998. PMID: 9857090
32 results