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Discovery and Structure Enabled Synthesis of 2,6-Diaminopyrimidin-4-one IRAK4 Inhibitors.
Seganish WM, Fischmann TO, Sherborne B, Matasi J, Lavey B, McElroy WT, Tulshian D, Tata J, Sondey C, Garlisi CG, Devito K, Fossetta J, Lundell D, Niu X. Seganish WM, et al. Among authors: fossetta j. ACS Med Chem Lett. 2015 Jul 12;6(8):942-7. doi: 10.1021/acsmedchemlett.5b00279. eCollection 2015 Aug 13. ACS Med Chem Lett. 2015. PMID: 26288698 Free PMC article.
Potent and Selective Amidopyrazole Inhibitors of IRAK4 That Are Efficacious in a Rodent Model of Inflammation.
McElroy WT, Tan Z, Ho G, Paliwal S, Li G, Seganish WM, Tulshian D, Tata J, Fischmann TO, Sondey C, Bian H, Bober L, Jackson J, Garlisi CG, Devito K, Fossetta J, Lundell D, Niu X. McElroy WT, et al. Among authors: fossetta j. ACS Med Chem Lett. 2015 May 12;6(6):677-82. doi: 10.1021/acsmedchemlett.5b00106. eCollection 2015 Jun 11. ACS Med Chem Lett. 2015. PMID: 26101573 Free PMC article.
Initial optimization and series evolution of diaminopyrimidine inhibitors of interleukin-1 receptor associated kinase 4.
Seganish WM, McElroy WT, Herr RJ, Brumfield S, Greenlee WJ, Harding J, Komanduri V, Matasi J, Prakash KC, Tulshian D, Yang J, Yet L, Devito K, Fossetta J, Garlisi CG, Lundell D, Niu X, Sondey C. Seganish WM, et al. Among authors: fossetta j. Bioorg Med Chem Lett. 2015 Aug 15;25(16):3203-7. doi: 10.1016/j.bmcl.2015.05.097. Epub 2015 Jun 6. Bioorg Med Chem Lett. 2015. PMID: 26115573
Efforts towards the optimization of a bi-aryl class of potent IRAK4 inhibitors.
Hanisak J, Seganish WM, McElroy WT, Tang H, Zhang R, Tsui HC, Fischmann T, Tulshian D, Tata J, Sondey C, Devito K, Fossetta J, Garlisi CG, Lundell D, Niu X. Hanisak J, et al. Among authors: fossetta j. Bioorg Med Chem Lett. 2016 Sep 1;26(17):4250-5. doi: 10.1016/j.bmcl.2016.07.048. Epub 2016 Jul 22. Bioorg Med Chem Lett. 2016. PMID: 27476420
3,4-Diamino-1,2,5-thiadiazole as potent and selective CXCR2 antagonists.
Biju P, Taveras AG, Yu Y, Zheng J, Hipkin RW, Fossetta J, Fan X, Fine J, Lundell D. Biju P, et al. Among authors: fossetta j. Bioorg Med Chem Lett. 2009 Mar 1;19(5):1434-7. doi: 10.1016/j.bmcl.2009.01.027. Epub 2009 Jan 15. Bioorg Med Chem Lett. 2009. PMID: 19200721
A three-step protocol for lead optimization: quick identification of key conformational features and functional groups in the SAR studies of non-ATP competitive MK2 (MAPKAPK2) inhibitors.
Huang X, Zhu X, Chen X, Zhou W, Xiao D, Degrado S, Aslanian R, Fossetta J, Lundell D, Tian F, Trivedi P, Palani A. Huang X, et al. Among authors: fossetta j. Bioorg Med Chem Lett. 2012 Jan 1;22(1):65-70. doi: 10.1016/j.bmcl.2011.11.074. Epub 2011 Nov 23. Bioorg Med Chem Lett. 2012. PMID: 22169260
Conformation constraint of anilides enabling the discovery of tricyclic lactams as potent MK2 non-ATP competitive inhibitors.
Xiao D, Palani A, Huang X, Sofolarides M, Zhou W, Chen X, Aslanian R, Guo Z, Fossetta J, Tian F, Trivedi P, Spacciapoli P, Whitehurst CE, Lundell D. Xiao D, et al. Among authors: fossetta j. Bioorg Med Chem Lett. 2013 Jun 1;23(11):3262-6. doi: 10.1016/j.bmcl.2013.03.109. Epub 2013 Apr 4. Bioorg Med Chem Lett. 2013. PMID: 23602398
Discovery of 2-hydroxy-N,N-dimethyl-3-{2-[[(R)-1-(5- methylfuran-2-yl)propyl]amino]-3,4-dioxocyclobut-1-enylamino}benzamide (SCH 527123): a potent, orally bioavailable CXCR2/CXCR1 receptor antagonist.
Dwyer MP, Yu Y, Chao J, Aki C, Chao J, Biju P, Girijavallabhan V, Rindgen D, Bond R, Mayer-Ezel R, Jakway J, Hipkin RW, Fossetta J, Gonsiorek W, Bian H, Fan X, Terminelli C, Fine J, Lundell D, Merritt JR, Rokosz LL, Kaiser B, Li G, Wang W, Stauffer T, Ozgur L, Baldwin J, Taveras AG. Dwyer MP, et al. Among authors: fossetta j. J Med Chem. 2006 Dec 28;49(26):7603-6. doi: 10.1021/jm0609622. J Med Chem. 2006. PMID: 17181143
26 results