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Page 1
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
3,4-Diamino-2,5-thiadiazole-1-oxides as potent CXCR2/CXCR1 antagonists.
Biju P, Taveras A, Yu Y, Zheng J, Chao J, Rindgen D, Jakway J, Hipkin RW, Fossetta J, Fan X, Fine J, Qiu H, Merritt JR, Baldwin JJ. Biju P, et al. Among authors: fossetta j. Bioorg Med Chem Lett. 2008 Jan 1;18(1):228-31. doi: 10.1016/j.bmcl.2007.10.094. Epub 2007 Oct 30. Bioorg Med Chem Lett. 2008. PMID: 18006311
Synthesis and structure-activity relationships of heteroaryl substituted-3,4-diamino-3-cyclobut-3-ene-1,2-dione CXCR2/CXCR1 receptor antagonists.
Yu Y, Dwyer MP, Chao J, Aki C, Chao J, Purakkattle B, Rindgen D, Bond R, Mayer-Ezel R, Jakway J, Qiu H, Hipkin RW, Fossetta J, Gonsiorek W, Bian H, Fan X, Terminelli C, Fine J, Lundell D, Merritt JR, He Z, Lai G, Wu M, Taveras A. Yu Y, et al. Among authors: fossetta j. Bioorg Med Chem Lett. 2008 Feb 15;18(4):1318-22. doi: 10.1016/j.bmcl.2008.01.024. Epub 2008 Jan 11. Bioorg Med Chem Lett. 2008. PMID: 18242983
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
Characterization of peripheral human cannabinoid receptor (hCB2) expression and pharmacology using a novel radioligand, [35S]Sch225336.
Gonsiorek W, Hesk D, Chen SC, Kinsley D, Fine JS, Jackson JV, Bober LA, Deno G, Bian H, Fossetta J, Lunn CA, Kozlowski JA, Lavey B, Piwinski J, Narula SK, Lundell DJ, Hipkin RW. Gonsiorek W, et al. Among authors: fossetta j. J Biol Chem. 2006 Sep 22;281(38):28143-51. doi: 10.1074/jbc.M602364200. Epub 2006 Jun 5. J Biol Chem. 2006. PMID: 16754676 Free article.
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
26 results