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Page 1
Arylsulfonamidopiperidone derivatives as a novel class of factor Xa inhibitors.
Shi Y, O'Connor SP, Sitkoff D, Zhang J, Shi M, Bisaha SN, Wang Y, Li C, Ruan Z, Lawrence RM, Klei HE, Kish K, Liu EC, Seiler SM, Schweizer L, Steinbacher TE, Schumacher WA, Robl JA, Macor JE, Atwal KS, Stein PD. Shi Y, et al. Among authors: sitkoff d. Bioorg Med Chem Lett. 2011 Dec 15;21(24):7516-21. doi: 10.1016/j.bmcl.2011.06.098. Epub 2011 Jun 28. Bioorg Med Chem Lett. 2011. PMID: 22041058
Synthesis of novel potent dipeptidyl peptidase IV inhibitors with enhanced chemical stability: interplay between the N-terminal amino acid alkyl side chain and the cyclopropyl group of alpha-aminoacyl-l-cis-4,5-methanoprolinenitrile-based inhibitors.
Magnin DR, Robl JA, Sulsky RB, Augeri DJ, Huang Y, Simpkins LM, Taunk PC, Betebenner DA, Robertson JG, Abboa-Offei BE, Wang A, Cap M, Xin L, Tao L, Sitkoff DF, Malley MF, Gougoutas JZ, Khanna A, Huang Q, Han SP, Parker RA, Hamann LG. Magnin DR, et al. J Med Chem. 2004 May 6;47(10):2587-98. doi: 10.1021/jm049924d. J Med Chem. 2004. PMID: 15115400
Diprolyl nitriles as potent dipeptidyl peptidase IV inhibitors.
Zhao G, Taunk PC, Magnin DR, Simpkins LM, Robl JA, Wang A, Robertson JG, Marcinkeviciene J, Sitkoff DF, Parker RA, Kirby MS, Hamann LG. Zhao G, et al. Bioorg Med Chem Lett. 2005 Sep 15;15(18):3992-5. doi: 10.1016/j.bmcl.2005.06.043. Bioorg Med Chem Lett. 2005. PMID: 16046120
Ketene aminal-based lactam derivatives as a novel class of orally active FXa inhibitors.
Shi Y, Zhang J, Stein PD, Shi M, O'Connor SP, Bisaha SN, Li C, Atwal KS, Bisacchi GS, Sitkoff D, Pudzianowski AT, Liu EC, Hartl KS, Seiler SM, Youssef S, Steinbacher TE, Schumacher WA, Rendina AR, Bozarth JM, Peterson TL, Zhang G, Zahler R. Shi Y, et al. Among authors: sitkoff d. Bioorg Med Chem Lett. 2005 Dec 15;15(24):5453-8. doi: 10.1016/j.bmcl.2005.08.107. Epub 2005 Oct 5. Bioorg Med Chem Lett. 2005. PMID: 16213711
Amino(methyl) pyrrolidines as novel scaffolds for factor Xa inhibitors.
Shi Y, Sitkoff D, Zhang J, Han W, Hu Z, Stein PD, Wang Y, Kennedy LJ, O'Connor SP, Ahmad S, Liu EC, Seiler SM, Lam PY, Robl JA, Macor JE, Atwal KS, Zahler R. Shi Y, et al. Among authors: sitkoff d. Bioorg Med Chem Lett. 2007 Nov 1;17(21):5952-8. doi: 10.1016/j.bmcl.2007.07.063. Epub 2007 Aug 21. Bioorg Med Chem Lett. 2007. PMID: 17855089
(3R,5S,E)-7-(4-(4-fluorophenyl)-6-isopropyl-2-(methyl(1-methyl-1h-1,2,4-triazol-5-yl)amino)pyrimidin-5-yl)-3,5-dihydroxyhept-6-enoic acid (BMS-644950): a rationally designed orally efficacious 3-hydroxy-3-methylglutaryl coenzyme-a reductase inhibitor with reduced myotoxicity potential.
Ahmad S, Madsen CS, Stein PD, Janovitz E, Huang C, Ngu K, Bisaha S, Kennedy LJ, Chen BC, Zhao R, Sitkoff D, Monshizadegan H, Yin X, Ryan CS, Zhang R, Giancarli M, Bird E, Chang M, Chen X, Setters R, Search D, Zhuang S, Nguyen-Tran V, Cuff CA, Harrity T, Darienzo CJ, Li T, Reeves RA, Blanar MA, Barrish JC, Zahler R, Robl JA. Ahmad S, et al. Among authors: sitkoff d. J Med Chem. 2008 May 8;51(9):2722-33. doi: 10.1021/jm800001n. Epub 2008 Apr 15. J Med Chem. 2008. PMID: 18412317
Design, structure-activity relationships, X-ray crystal structure, and energetic contributions of a critical P1 pharmacophore: 3-chloroindole-7-yl-based factor Xa inhibitors.
Shi Y, Sitkoff D, Zhang J, Klei HE, Kish K, Liu EC, Hartl KS, Seiler SM, Chang M, Huang C, Youssef S, Steinbacher TE, Schumacher WA, Grazier N, Pudzianowski A, Apedo A, Discenza L, Yanchunas J, Stein PD, Atwal KS. Shi Y, et al. Among authors: sitkoff d. J Med Chem. 2008 Dec 11;51(23):7541-51. doi: 10.1021/jm800855x. J Med Chem. 2008. PMID: 18998662
Cyanoguanidine-based lactam derivatives as a novel class of orally bioavailable factor Xa inhibitors.
Shi Y, Zhang J, Shi M, O'Connor SP, Bisaha SN, Li C, Sitkoff D, Pudzianowski AT, Chong S, Klei HE, Kish K, Yanchunas J Jr, Liu EC, Hartl KS, Seiler SM, Steinbacher TE, Schumacher WA, Atwal KS, Stein PD. Shi Y, et al. Among authors: sitkoff d. Bioorg Med Chem Lett. 2009 Aug 1;19(15):4034-41. doi: 10.1016/j.bmcl.2009.06.014. Epub 2009 Jun 13. Bioorg Med Chem Lett. 2009. PMID: 19541481
Aroylguanidine-based factor Xa inhibitors: the discovery of BMS-344577.
Shi Y, Li C, O'Connor SP, Zhang J, Shi M, Bisaha SN, Wang Y, Sitkoff D, Pudzianowski AT, Huang C, Klei HE, Kish K, Yanchunas J Jr, Liu EC, Hartl KS, Seiler SM, Steinbacher TE, Schumacher WA, Atwal KS, Stein PD. Shi Y, et al. Among authors: sitkoff d. Bioorg Med Chem Lett. 2009 Dec 15;19(24):6882-9. doi: 10.1016/j.bmcl.2009.10.084. Epub 2009 Oct 23. Bioorg Med Chem Lett. 2009. PMID: 19896847
28 results