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Optimization of a potent class of arylamide colony-stimulating factor-1 receptor inhibitors leading to anti-inflammatory clinical candidate 4-cyano-N-[2-(1-cyclohexen-1-yl)-4-[1-[(dimethylamino)acetyl]-4-piperidinyl]phenyl]-1H-imidazole-2-carboxamide (JNJ-28312141).
Illig CR, Manthey CL, Wall MJ, Meegalla SK, Chen J, Wilson KJ, Ballentine SK, Desjarlais RL, Schubert C, Crysler CS, Chen Y, Molloy CJ, Chaikin MA, Donatelli RR, Yurkow E, Zhou Z, Player MR, Tomczuk BE. Illig CR, et al. Among authors: desjarlais rl. J Med Chem. 2011 Nov 24;54(22):7860-83. doi: 10.1021/jm200900q. Epub 2011 Oct 31. J Med Chem. 2011. PMID: 22039836
Discovery of novel FMS kinase inhibitors as anti-inflammatory agents.
Illig CR, Chen J, Wall MJ, Wilson KJ, Ballentine SK, Rudolph MJ, DesJarlais RL, Chen Y, Schubert C, Petrounia I, Crysler CS, Molloy CJ, Chaikin MA, Manthey CL, Player MR, Tomczuk BE, Meegalla SK. Illig CR, et al. Among authors: desjarlais rl. Bioorg Med Chem Lett. 2008 Mar 1;18(5):1642-8. doi: 10.1016/j.bmcl.2008.01.059. Epub 2008 Jan 19. Bioorg Med Chem Lett. 2008. PMID: 18242992
Synthesis and evaluation of novel 3,4,6-substituted 2-quinolones as FMS kinase inhibitors.
Wall MJ, Chen J, Meegalla S, Ballentine SK, Wilson KJ, DesJarlais RL, Schubert C, Chaikin MA, Crysler C, Petrounia IP, Donatelli RR, Yurkow EJ, Boczon L, Mazzulla M, Player MR, Patch RJ, Manthey CL, Molloy C, Tomczuk B, Illig CR. Wall MJ, et al. Among authors: desjarlais rl. Bioorg Med Chem Lett. 2008 Mar 15;18(6):2097-102. doi: 10.1016/j.bmcl.2008.01.088. Epub 2008 Jan 30. Bioorg Med Chem Lett. 2008. PMID: 18289848
Structure-based optimization of a potent class of arylamide FMS inhibitors.
Meegalla SK, Wall MJ, Chen J, Wilson KJ, Ballentine SK, Desjarlais RL, Schubert C, Crysler CS, Chen Y, Molloy CJ, Chaikin MA, Manthey CL, Player MR, Tomczuk BE, Illig CR. Meegalla SK, et al. Among authors: desjarlais rl. Bioorg Med Chem Lett. 2008 Jun 15;18(12):3632-7. doi: 10.1016/j.bmcl.2008.04.059. Epub 2008 Apr 26. Bioorg Med Chem Lett. 2008. PMID: 18495479
Reducing ion channel activity in a series of 4-heterocyclic arylamide FMS inhibitors.
Wilson KJ, Illig CR, Chen J, Wall MJ, Ballentine SK, DesJarlais RL, Chen Y, Schubert C, Donatelli R, Petrounia I, Crysler CS, Molloy CJ, Chaikin MA, Manthey CL, Player MR, Tomczuk BE, Meegalla SK. Wilson KJ, et al. Among authors: desjarlais rl. Bioorg Med Chem Lett. 2010 Jul 1;20(13):3925-9. doi: 10.1016/j.bmcl.2010.05.013. Epub 2010 May 12. Bioorg Med Chem Lett. 2010. PMID: 20570147
Enhancement of kinase selectivity in a potent class of arylamide FMS inhibitors.
Illig CR, Manthey CL, Meegalla SK, Wall MJ, Chen J, Wilson KJ, DesJarlais RL, Ballentine SK, Schubert C, Crysler CS, Chen Y, Molloy CJ, Chaikin MA, Donatelli RR, Yurkow E, Zhou Z, Player MR, Tomczuk BE. Illig CR, et al. Among authors: desjarlais rl. Bioorg Med Chem Lett. 2013 Dec 1;23(23):6363-9. doi: 10.1016/j.bmcl.2013.09.061. Epub 2013 Oct 1. Bioorg Med Chem Lett. 2013. PMID: 24138939
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: desjarlais rl. 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
64 results