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Page 1
Potency variation of small-molecule chymase inhibitors across species.
Kervinen J, Crysler C, Bayoumy S, Abad MC, Spurlino J, Deckman I, Greco MN, Maryanoff BE, de Garavilla L. Kervinen J, et al. Among authors: crysler c. Biochem Pharmacol. 2010 Oct 1;80(7):1033-41. doi: 10.1016/j.bcp.2010.06.014. Epub 2010 Jun 23. Biochem Pharmacol. 2010. PMID: 20599788
Discovery, SAR, and X-ray structure of novel biaryl-based dipeptidyl peptidase IV inhibitors.
Qiao L, Baumann CA, Crysler CS, Ninan NS, Abad MC, Spurlino JC, Desjarlais RL, Kervinen J, Neeper MP, Bayoumy SS, Williams R, Deckman IC, Dasgupta M, Reed RL, Huebert ND, Tomczuk BE, Moriarty KJ. Qiao L, et al. Among authors: crysler cs. Bioorg Med Chem Lett. 2006 Jan 1;16(1):123-8. doi: 10.1016/j.bmcl.2005.09.037. Epub 2005 Oct 19. Bioorg Med Chem Lett. 2006. PMID: 16236500
Structural basis for elastolytic substrate specificity in rodent alpha-chymases.
Kervinen J, Abad M, Crysler C, Kolpak M, Mahan AD, Masucci JA, Bayoumy S, Cummings MD, Yao X, Olson M, de Garavilla L, Kuo L, Deckman I, Spurlino J. Kervinen J, et al. Among authors: crysler c. J Biol Chem. 2008 Jan 4;283(1):427-436. doi: 10.1074/jbc.M707157200. Epub 2007 Oct 31. J Biol Chem. 2008. PMID: 17981788 Free article.
7-fluoroindazoles as potent and selective inhibitors of factor Xa.
Lee YK, Parks DJ, Lu T, Thieu TV, Markotan T, Pan W, McComsey DF, Milkiewicz KL, Crysler CS, Ninan N, Abad MC, Giardino EC, Maryanoff BE, Damiano BP, Player MR. Lee YK, et al. Among authors: crysler cs. J Med Chem. 2008 Jan 24;51(2):282-97. doi: 10.1021/jm701217r. Epub 2007 Dec 27. J Med Chem. 2008. PMID: 18159923
Discovery and clinical evaluation of 1-{N-[2-(amidinoaminooxy)ethyl]amino}carbonylmethyl-6-methyl-3-[2,2-difluoro-2-phenylethylamino]pyrazinone (RWJ-671818), a thrombin inhibitor with an oxyguanidine P1 motif.
Lu T, Markotan T, Ballentine SK, Giardino EC, Spurlino J, Crysler CS, Brown K, Maryanoff BE, Tomczuk BE, Damiano BP, Shukla U, End D, Andrade-Gordon P, Bone RF, Player MR. Lu T, et al. Among authors: crysler cs. J Med Chem. 2010 Feb 25;53(4):1843-56. doi: 10.1021/jm901802n. J Med Chem. 2010. PMID: 20102150 Clinical Trial.
Orally efficacious thrombin inhibitors with cyanofluorophenylacetamide as the P2 motif.
Kreutter KD, Lu T, Lee L, Giardino EC, Patel S, Huang H, Xu G, Fitzgerald M, Haertlein BJ, Mohan V, Crysler C, Eisennagel S, Dasgupta M, McMillan M, Spurlino JC, Huebert ND, Maryanoff BE, Tomczuk BE, Damiano BP, Player MR. Kreutter KD, et al. Among authors: crysler c. Bioorg Med Chem Lett. 2008 May 1;18(9):2865-70. doi: 10.1016/j.bmcl.2008.03.087. Epub 2008 Apr 8. Bioorg Med Chem Lett. 2008. PMID: 18420408
2-(2-Chloro-6-fluorophenyl)acetamides as potent thrombin inhibitors.
Lee L, Kreutter KD, Pan W, Crysler C, Spurlino J, Player MR, Tomczuk B, Lu T. Lee L, et al. Among authors: crysler c. Bioorg Med Chem Lett. 2007 Nov 15;17(22):6266-9. doi: 10.1016/j.bmcl.2007.09.013. Epub 2007 Sep 8. Bioorg Med Chem Lett. 2007. PMID: 17889527
Structure-based design, synthesis and SAR of a novel series of thiopheneamidine urokinase plasminogen activator inhibitors.
Subasinghe NL, Illig C, Hoffman J, Rudolph MJ, Wilson KJ, Soll R, Randle T, Green D, Lewandowski F, Zhang M, Bone R, Spurlino J, DesJarlais R, Deckman I, Molloy CJ, Manthey C, Zhou Z, Sharp C, Maguire D, Crysler C, Grasberger B. Subasinghe NL, et al. Among authors: crysler c. Bioorg Med Chem Lett. 2001 Jun 4;11(11):1379-82. doi: 10.1016/s0960-894x(01)00247-5. Bioorg Med Chem Lett. 2001. PMID: 11378359
A novel series of potent and selective small molecule inhibitors of the complement component C1s.
Subasinghe NL, Ali F, Illig CR, Jonathan Rudolph M, Klein S, Khalil E, Soll RM, Bone RF, Spurlino JC, DesJarlais RL, Crysler CS, Cummings MD, Morris PE Jr, Kilpatrick JM, Sudhakara Babu Y. Subasinghe NL, et al. Among authors: crysler cs. Bioorg Med Chem Lett. 2004 Jun 21;14(12):3043-7. doi: 10.1016/j.bmcl.2004.04.034. Bioorg Med Chem Lett. 2004. PMID: 15149641
Oxyguanidines: application to non-peptidic phenyl-based thrombin inhibitors.
Tomczuk B, Lu T, Soll RM, Fedde C, Wang A, Murphy L, Crysler C, Dasgupta M, Eisennagel S, Spurlino J, Bone R. Tomczuk B, et al. Among authors: crysler c. Bioorg Med Chem Lett. 2003 Apr 17;13(8):1495-8. doi: 10.1016/s0960-894x(03)00125-2. Bioorg Med Chem Lett. 2003. PMID: 12668020
40 results