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Page 1
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: girijavallabhan vm. 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
5-Benzothiazole substituted pyrimidine derivatives as HCV replication (replicase) inhibitors.
Arasappan A, Bennett F, Girijavallabhan V, Huang Y, Huelgas R, Alvarez C, Chen L, Gavalas S, Kim SH, Kosinski A, Pinto P, Rizvi R, Rossman R, Shankar B, Tong L, Velazquez F, Venkatraman S, Verma VA, Kozlowski J, Shih NY, Piwinski JJ, MacCoss M, Kwong CD, Clark JL, Fowler AT, Geng F, Kezar HS 3rd, Roychowdhury A, Reynolds RC, Maddry JA, Ananthan S, Secrist JA 3rd, Li C, Chase R, Curry S, Huang HC, Tong X, Njoroge FG. Arasappan A, et al. Bioorg Med Chem Lett. 2012 May 1;22(9):3229-34. doi: 10.1016/j.bmcl.2012.03.036. Epub 2012 Mar 13. Bioorg Med Chem Lett. 2012. PMID: 22472692
Synthesis and SAR of geminal substitutions at the C5' carbosugar position of pyrimidine-derived HCV inhibitors.
Verma VA, Rossman R, Bennett F, Chen L, Gavalas S, Girijavallabhan V, Huang Y, Kim SH, Kosinski A, Pinto P, Rizvi R, Shankar B, Tong L, Velazquez F, Venkatraman S, Kozlowski J, MacCoss M, Kwong CD, Bansal N, Kezar HS 3rd, Reynolds RC, Maddry JA, Ananthan S, Secrist JA 3rd, Li C, Chase R, Curry S, Huang HC, Tong X, Njoroge FG, Arasappan A. Verma VA, et al. Bioorg Med Chem Lett. 2012 Nov 15;22(22):6967-73. doi: 10.1016/j.bmcl.2012.08.111. Epub 2012 Sep 7. Bioorg Med Chem Lett. 2012. PMID: 23036957
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
Development of a prodrug of hydantoin based TACE inhibitor.
Tong L, Kim SH, Chen L, Kosinski A, Shankar BB, Girijavallabhan V, Yang DY, Yu W, Zhou G, Shih NY, Chen S, Hu M, Lundell D, Niu X, Umland S, Kozlowski JA. Tong L, et al. Bioorg Med Chem Lett. 2017 Aug 15;27(16):3704-3708. doi: 10.1016/j.bmcl.2017.07.007. Epub 2017 Jul 3. Bioorg Med Chem Lett. 2017. PMID: 28711352
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. Among authors: girijavallabhan vm. 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
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: girijavallabhan vm. 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
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. 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
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: girijavallabhan vm. 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
Synthesis and SAR of pyridothiazole substituted pyrimidine derived HCV replication inhibitors.
Girijavallabhan VM, Alvarez C, Bennett F, Chen L, Gavalas S, Huang Y, Kim SH, Kosinski A, Pinto P, Rizvi R, Rossman R, Shankar B, Tong L, Velazquez F, Venkatraman S, Verma VA, Kozlowski J, Shih NY, Piwinski JJ, MacCoss M, Kwong CD, Bansal N, Clark JL, Fowler AT, Kezar HS 3rd, Valiyaveettil J, Reynolds RC, Maddry JA, Ananthan S, Secrist JA 3rd, Li C, Chase R, Curry S, Huang HC, Tong X, Njoroge FG, Arasappan A. Girijavallabhan VM, et al. Bioorg Med Chem Lett. 2012 Sep 1;22(17):5652-7. doi: 10.1016/j.bmcl.2012.06.099. Epub 2012 Jul 15. Bioorg Med Chem Lett. 2012. PMID: 22858143
63 results