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Page 1
2-(2-Aminothiazol-4-yl)pyrrolidine-based tartrate diamides as potent, selective and orally bioavailable TACE inhibitors.
Dai C, Li D, Popovici-Muller J, Zhao L, Girijavallabhan VM, Rosner KE, Lavey BJ, Rizvi R, Shankar BB, Wong MK, Guo Z, Orth P, Strickland CO, Sun J, Niu X, Chen S, Kozlowski JA, Lundell DJ, Piwinski JJ, Shih NY, Siddiqui MA. Dai C, et al. Among authors: rosner ke. Bioorg Med Chem Lett. 2011 May 15;21(10):3172-6. doi: 10.1016/j.bmcl.2011.01.002. Epub 2011 Jan 6. Bioorg Med Chem Lett. 2011. PMID: 21458257
Fused bi-heteroaryl substituted hydantoin compounds as TACE inhibitors.
Tong L, Kim SH, Rosner K, Yu W, Shankar BB, Chen L, Li D, Dai C, Girijavallabhan V, Popovici-Muller J, Yang L, Zhou G, Kosinski A, Siddiqui MA, Shih NY, Guo Z, Orth P, Chen S, Lundell D, Niu X, Umland S, Kozlowski JA. Tong L, et al. Bioorg Med Chem Lett. 2017 Jul 15;27(14):3037-3042. doi: 10.1016/j.bmcl.2017.05.062. Epub 2017 May 22. Bioorg Med Chem Lett. 2017. PMID: 28558971
The discovery of novel tartrate-based TNF-alpha converting enzyme (TACE) inhibitors.
Rosner KE, Guo Z, Orth P, Shipps GW Jr, Belanger DB, Chan TY, Curran PJ, Dai C, Deng Y, Girijavallabhan VM, Hong L, Lavey BJ, Lee JF, Li D, Liu Z, Popovici-Muller J, Ting PC, Vaccaro H, Wang L, Wang T, Yu W, Zhou G, Niu X, Sun J, Kozlowski JA, Lundell DJ, Madison V, McKittrick B, Piwinski JJ, Shih NY, Arshad Siddiqui M, Strickland CO. Rosner KE, et al. Bioorg Med Chem Lett. 2010 Feb 1;20(3):1189-93. doi: 10.1016/j.bmcl.2009.12.004. Epub 2009 Dec 5. Bioorg Med Chem Lett. 2010. PMID: 20022498
Discovery and SAR of hydantoin TACE inhibitors.
Yu W, Guo Z, Orth P, Madison V, Chen L, Dai C, Feltz RJ, Girijavallabhan VM, Kim SH, Kozlowski JA, Lavey BJ, Li D, Lundell D, Niu X, Piwinski JJ, Popovici-Muller J, Rizvi R, Rosner KE, Shankar BB, Shih NY, Siddiqui MA, Sun J, Tong L, Umland S, Wong MK, Yang DY, Zhou G. Yu W, et al. Among authors: rosner ke. Bioorg Med Chem Lett. 2010 Mar 15;20(6):1877-80. doi: 10.1016/j.bmcl.2010.01.148. Epub 2010 Feb 4. Bioorg Med Chem Lett. 2010. PMID: 20172725
Structure and activity relationships of tartrate-based TACE inhibitors.
Li D, Popovici-Muller J, Belanger DB, Caldwell J, Dai C, David M, Girijavallabhan VM, Lavey BJ, Lee JF, Liu Z, Mazzola R, Rizvi R, Rosner KE, Shankar B, Spitler J, Ting PC, Vaccaro H, Yu W, Zhou G, Zhu Z, Niu X, Sun J, Guo Z, Orth P, Chen S, Kozlowski JA, Lundell DJ, Madison V, McKittrick B, Piwinski JJ, Shih NY, Shipps GW Jr, Siddiqui MA, Strickland CO. Li D, et al. Among authors: rosner ke. Bioorg Med Chem Lett. 2010 Aug 15;20(16):4812-5. doi: 10.1016/j.bmcl.2010.06.104. Epub 2010 Jun 25. Bioorg Med Chem Lett. 2010. PMID: 20638281
Biaryl substituted hydantoin compounds as TACE inhibitors.
Yu W, Tong L, Kim SH, Wong MK, Chen L, Yang DY, Shankar BB, Lavey BJ, Zhou G, Kosinski A, Rizvi R, Li D, Feltz RJ, Piwinski JJ, Rosner KE, Shih NY, Siddiqui MA, Guo Z, Orth P, Shah H, Sun J, Umland S, Lundell DJ, Niu X, Kozlowski JA. Yu W, et al. Among authors: rosner ke. Bioorg Med Chem Lett. 2010 Sep 1;20(17):5286-9. doi: 10.1016/j.bmcl.2010.06.134. Epub 2010 Jul 1. Bioorg Med Chem Lett. 2010. PMID: 20663669
Novel TNF-α converting enzyme (TACE) inhibitors as potential treatment for inflammatory diseases.
Girijavallabhan VM, Chen L, Dai C, Feltz RJ, Firmansjah L, Li D, Kim SH, Kozlowski JA, Lavey BJ, Kosinski A, Piwinski JJ, Popovici-Muller J, Rizvi R, Rosner KE, Shankar BB, Shih NY, Siddiqui MA, Tong L, Wong MK, Yang DY, Yang L, Yu W, Zhou G, Guo Z, Orth P, Madison V, Bian H, Lundell D, Niu X, Shah H, Sun J, Umland S. Girijavallabhan VM, et al. Among authors: rosner ke. Bioorg Med Chem Lett. 2010 Dec 15;20(24):7283-7. doi: 10.1016/j.bmcl.2010.10.081. Epub 2010 Oct 23. Bioorg Med Chem Lett. 2010. PMID: 21106451
Aminothiazole inhibitors of HCV RNA polymerase.
Shipps GW Jr, Deng Y, Wang T, Popovici-Muller J, Curran PJ, Rosner KE, Cooper AB, Girijavallabhan V, Butkiewicz N, Cable M. Shipps GW Jr, et al. Among authors: rosner ke. Bioorg Med Chem Lett. 2005 Jan 3;15(1):115-9. doi: 10.1016/j.bmcl.2004.10.024. Bioorg Med Chem Lett. 2005. PMID: 15582422
Pyrazolo[1,5-a]pyrimidine-based inhibitors of HCV polymerase.
Popovici-Muller J, Shipps GW Jr, Rosner KE, Deng Y, Wang T, Curran PJ, Brown MA, Siddiqui MA, Cooper AB, Duca J, Cable M, Girijavallabhan V. Popovici-Muller J, et al. Among authors: rosner ke. Bioorg Med Chem Lett. 2009 Nov 15;19(22):6331-6. doi: 10.1016/j.bmcl.2009.09.087. Epub 2009 Sep 25. Bioorg Med Chem Lett. 2009. PMID: 19819138