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II. SAR studies of pyridyl-piperazinyl-piperidine derivatives as CXCR3 chemokine antagonists.
Shao Y, Anilkumar GN, Carroll CD, Dong G, Hall JW 3rd, Hobbs DW, Jiang Y, Jenh CH, Kim SH, Kozlowski JA, McGuinness BF, Rosenblum SB, Schulman I, Shih NY, Shu Y, Wong MK, Yu W, Zawacki LG, Zeng Q. Shao Y, et al. Among authors: rosenblum sb. Bioorg Med Chem Lett. 2011 Mar 1;21(5):1527-31. doi: 10.1016/j.bmcl.2010.12.114. Epub 2010 Dec 28. Bioorg Med Chem Lett. 2011. PMID: 21277198
III. Identification of novel CXCR3 chemokine receptor antagonists with a pyrazinyl-piperazinyl-piperidine scaffold.
Kim SH, Anilkumar GN, Zawacki LG, Zeng Q, Yang DY, Shao Y, Dong G, Xu X, Yu W, Jiang Y, Jenh CH, Hall JW 3rd, Carroll CD, Hobbs DW, Baldwin JJ, McGuinness BF, Rosenblum SB, Kozlowski JA, Shankar BB, Shih NY. Kim SH, et al. Among authors: rosenblum sb. Bioorg Med Chem Lett. 2011 Dec 1;21(23):6982-6. doi: 10.1016/j.bmcl.2011.09.120. Epub 2011 Oct 5. Bioorg Med Chem Lett. 2011. PMID: 22018463
II. Novel HCV NS5B polymerase inhibitors: discovery of indole C2 acyl sulfonamides.
Anilkumar GN, Selyutin O, Rosenblum SB, Zeng Q, Jiang Y, Chan TY, Pu H, Wang L, Bennett F, Chen KX, Lesburg CA, Duca J, Gavalas S, Huang Y, Pinto P, Sannigrahi M, Velazquez F, Venkatraman S, Vibulbhan B, Agrawal S, Ferrari E, Jiang CK, Huang HC, Shih NY, George Njoroge F, Kozlowski JA. Anilkumar GN, et al. Among authors: rosenblum sb. Bioorg Med Chem Lett. 2012 Jan 1;22(1):713-7. doi: 10.1016/j.bmcl.2011.10.041. Epub 2011 Oct 20. Bioorg Med Chem Lett. 2012. PMID: 22104146
IV. Discovery of CXCR3 antagonists substituted with heterocycles as amide surrogates: improved PK, hERG and metabolic profiles.
Nair AG, Wong MK, Shu Y, Jiang Y, Jenh CH, Kim SH, Yang DY, Zeng Q, Shao Y, Zawacki LG, Duo J, McGuinness BF, Carroll CD, Hobbs DW, Shih NY, Rosenblum SB, Kozlowski JA. Nair AG, et al. Among authors: rosenblum sb. Bioorg Med Chem Lett. 2014 Feb 15;24(4):1085-8. doi: 10.1016/j.bmcl.2014.01.009. Epub 2014 Jan 11. Bioorg Med Chem Lett. 2014. PMID: 24486132
Novel CXCR3 antagonists with a piperazinyl-piperidine core.
McGuinness BF, Carroll CD, Zawacki LG, Dong G, Yang C, Hobbs DW, Jacob-Samuel B, Hall JW 3rd, Jenh CH, Kozlowski JA, Anilkumar GN, Rosenblum SB. McGuinness BF, et al. Among authors: rosenblum sb. Bioorg Med Chem Lett. 2009 Sep 1;19(17):5205-8. doi: 10.1016/j.bmcl.2009.07.020. Epub 2009 Jul 9. Bioorg Med Chem Lett. 2009. PMID: 19647429
I. Novel HCV NS5B polymerase inhibitors: discovery of indole 2-carboxylic acids with C3-heterocycles.
Anilkumar GN, Lesburg CA, Selyutin O, Rosenblum SB, Zeng Q, Jiang Y, Chan TY, Pu H, Vaccaro H, Wang L, Bennett F, Chen KX, Duca J, Gavalas S, Huang Y, Pinto P, Sannigrahi M, Velazquez F, Venkatraman S, Vibulbhan B, Agrawal S, Butkiewicz N, Feld B, Ferrari E, He Z, Jiang CK, Palermo RE, McMonagle P, Huang HC, Shih NY, Njoroge G, Kozlowski JA. Anilkumar GN, et al. Among authors: rosenblum sb. Bioorg Med Chem Lett. 2011 Sep 15;21(18):5336-41. doi: 10.1016/j.bmcl.2011.07.021. Epub 2011 Jul 19. Bioorg Med Chem Lett. 2011. PMID: 21840715
Structure-activity relationship (SAR) development and discovery of potent indole-based inhibitors of the hepatitis C virus (HCV) NS5B polymerase.
Chen KX, Vibulbhan B, Yang W, Sannigrahi M, Velazquez F, Chan TY, Venkatraman S, Anilkumar GN, Zeng Q, Bennet F, Jiang Y, Lesburg CA, Duca J, Pinto P, Gavalas S, Huang Y, Wu W, Selyutin O, Agrawal S, Feld B, Huang HC, Li C, Cheng KC, Shih NY, Kozlowski JA, Rosenblum SB, Njoroge FG. Chen KX, et al. Among authors: rosenblum sb. J Med Chem. 2012 Jan 26;55(2):754-65. doi: 10.1021/jm201258k. Epub 2012 Jan 6. J Med Chem. 2012. PMID: 22148957
Discovery of silyl proline containing HCV NS5A inhibitors with pan-genotype activity: SAR development.
Nair AG, Zeng Q, Selyutin O, Rosenblum SB, Jiang Y, Yang DY, Keertikar K, Zhou G, Dwyer MP, Kim SH, Shankar B, Yu W, Tong L, Chen L, Mazzola R, Caldwell J, Tang H, Allard ML, Buckle RN, Gauuan PJ, Holst CL, Martin GS, Naicker KP, Vellekoop S, Agrawal S, Liu R, Kong R, Ingravallo P, Xia E, Zhai Y, Nomeir A, Kozlowski JA. Nair AG, et al. Among authors: rosenblum sb. Bioorg Med Chem Lett. 2016 Mar 1;26(5):1475-9. doi: 10.1016/j.bmcl.2016.01.050. Epub 2016 Jan 19. Bioorg Med Chem Lett. 2016. PMID: 26850003
Discovery of fused tricyclic core containing HCV NS5A inhibitors with pan-genotype activity.
Yu W, Coburn CA, Yang DY, Meinke PT, Wong M, Rosenblum SB, Chen KX, Njoroge GF, Chen L, Dwyer MP, Jiang Y, Nair AG, Selyutin O, Tong L, Zeng Q, Zhong B, Ji T, Hu B, Agrawal S, Xia E, Zhai Y, Liu R, Kong R, Ingravallo P, Asante-Appiah E, Nomeir A, Fells J, Kozlowski JA. Yu W, et al. Among authors: rosenblum sb. Bioorg Med Chem Lett. 2016 Jul 1;26(13):3158-3162. doi: 10.1016/j.bmcl.2016.04.084. Epub 2016 Apr 30. Bioorg Med Chem Lett. 2016. PMID: 27180013
31 results