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Page 1
SAR of PXR transactivation in benzimidazole-based IGF-1R kinase inhibitors.
Zimmermann K, Wittman MD, Saulnier MG, Velaparthi U, Sang X, Frennesson DB, Struzynski C, Seitz SP, He L, Carboni JM, Li A, Greer AF, Gottardis M, Attar RM, Yang Z, Balimane P, Discenza LN, Lee FY, Sinz M, Kim S, Vyas D. Zimmermann K, et al. Among authors: greer af. Bioorg Med Chem Lett. 2010 Mar 1;20(5):1744-8. doi: 10.1016/j.bmcl.2010.01.087. Epub 2010 Jan 21. Bioorg Med Chem Lett. 2010. PMID: 20153189
Discovery of a (1H-benzoimidazol-2-yl)-1H-pyridin-2-one (BMS-536924) inhibitor of insulin-like growth factor I receptor kinase with in vivo antitumor activity.
Wittman M, Carboni J, Attar R, Balasubramanian B, Balimane P, Brassil P, Beaulieu F, Chang C, Clarke W, Dell J, Eummer J, Frennesson D, Gottardis M, Greer A, Hansel S, Hurlburt W, Jacobson B, Krishnananthan S, Lee FY, Li A, Lin TA, Liu P, Ouellet C, Sang X, Saulnier MG, Stoffan K, Sun Y, Velaparthi U, Wong H, Yang Z, Zimmermann K, Zoeckler M, Vyas D. Wittman M, et al. J Med Chem. 2005 Sep 8;48(18):5639-43. doi: 10.1021/jm050392q. J Med Chem. 2005. PMID: 16134929
Discovery and initial SAR of 3-(1H-benzo[d]imidazol-2-yl)pyridin-2(1H)-ones as inhibitors of insulin-like growth factor 1-receptor (IGF-1R).
Velaparthi U, Wittman M, Liu P, Stoffan K, Zimmermann K, Sang X, Carboni J, Li A, Attar R, Gottardis M, Greer A, Chang CY, Jacobsen BL, Sack JS, Sun Y, Langley DR, Balasubramanian B, Vyas D. Velaparthi U, et al. Bioorg Med Chem Lett. 2007 Apr 15;17(8):2317-21. doi: 10.1016/j.bmcl.2007.01.102. Epub 2007 Feb 4. Bioorg Med Chem Lett. 2007. PMID: 17317169
Imidazole moiety replacements in the 3-(1H-benzo[d]imidazol-2-yl)pyridin-2(1H)-one inhibitors of insulin-like growth factor receptor-1 (IGF-1R) to improve cytochrome P450 profile.
Velaparthi U, Liu P, Balasubramanian B, Carboni J, Attar R, Gottardis M, Li A, Greer A, Zoeckler M, Wittman MD, Vyas D. Velaparthi U, et al. Bioorg Med Chem Lett. 2007 Jun 1;17(11):3072-6. doi: 10.1016/j.bmcl.2007.03.048. Epub 2007 Mar 19. Bioorg Med Chem Lett. 2007. PMID: 17398093
2-(1H-Imidazol-4-yl)ethanamine and 2-(1H-pyrazol-1-yl)ethanamine side chain variants of the IGF-1R inhibitor BMS-536924.
Saulnier MG, Frennesson DB, Wittman MD, Zimmermann K, Velaparthi U, Langley DR, Struzynski C, Sang X, Carboni J, Li A, Greer A, Yang Z, Balimane P, Gottardis M, Attar R, Vyas D. Saulnier MG, et al. Bioorg Med Chem Lett. 2008 Mar 1;18(5):1702-7. doi: 10.1016/j.bmcl.2008.01.049. Epub 2008 Jan 18. Bioorg Med Chem Lett. 2008. PMID: 18258427
Balancing oral exposure with Cyp3A4 inhibition in benzimidazole-based IGF-IR inhibitors.
Zimmermann K, Wittman MD, Saulnier MG, Velaparthi U, Langley DR, Sang X, Frennesson D, Carboni J, Li A, Greer A, Gottardis M, Attar RM, Yang Z, Balimane P, Discenza LN, Vyas D. Zimmermann K, et al. Bioorg Med Chem Lett. 2008 Jul 15;18(14):4075-80. doi: 10.1016/j.bmcl.2008.05.104. Epub 2008 Jun 21. Bioorg Med Chem Lett. 2008. PMID: 18572407
Discovery and evaluation of 4-(2-(4-chloro-1H-pyrazol-1-yl)ethylamino)-3-(6-(1-(3-fluoropropyl)piperidin-4-yl)-4-methyl-1H-benzo[d]imidazol-2-yl)pyridin-2(1H)-one (BMS-695735), an orally efficacious inhibitor of insulin-like growth factor-1 receptor kinase with broad spectrum in vivo antitumor activity.
Velaparthi U, Wittman M, Liu P, Carboni JM, Lee FY, Attar R, Balimane P, Clarke W, Sinz MW, Hurlburt W, Patel K, Discenza L, Kim S, Gottardis M, Greer A, Li A, Saulnier M, Yang Z, Zimmermann K, Trainor G, Vyas D. Velaparthi U, et al. J Med Chem. 2008 Oct 9;51(19):5897-900. doi: 10.1021/jm800832q. Epub 2008 Sep 3. J Med Chem. 2008. PMID: 18763755
Discovery of a 2,4-disubstituted pyrrolo[1,2-f][1,2,4]triazine inhibitor (BMS-754807) of insulin-like growth factor receptor (IGF-1R) kinase in clinical development.
Wittman MD, Carboni JM, Yang Z, Lee FY, Antman M, Attar R, Balimane P, Chang C, Chen C, Discenza L, Frennesson D, Gottardis MM, Greer A, Hurlburt W, Johnson W, Langley DR, Li A, Li J, Liu P, Mastalerz H, Mathur A, Menard K, Patel K, Sack J, Sang X, Saulnier M, Smith D, Stefanski K, Trainor G, Velaparthi U, Zhang G, Zimmermann K, Vyas DM. Wittman MD, et al. J Med Chem. 2009 Dec 10;52(23):7360-3. doi: 10.1021/jm900786r. J Med Chem. 2009. PMID: 19778024
BMS-754807, a small molecule inhibitor of insulin-like growth factor-1R/IR.
Carboni JM, Wittman M, Yang Z, Lee F, Greer A, Hurlburt W, Hillerman S, Cao C, Cantor GH, Dell-John J, Chen C, Discenza L, Menard K, Li A, Trainor G, Vyas D, Kramer R, Attar RM, Gottardis MM. Carboni JM, et al. Mol Cancer Ther. 2009 Dec;8(12):3341-9. doi: 10.1158/1535-7163.MCT-09-0499. Mol Cancer Ther. 2009. PMID: 19996272
22 results