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Page 1
Design and synthesis of a fluoroindolocarbazole series as selective topoisomerase I active agents. Discovery of water-soluble 3,9-difluoro-12,13-dihydro-13-[6-amino-beta-D-glucopyranosyl]-5H,13H-benzo[b]- thienyl[2,3-a]pyrrolo[3,4-c]carbazole- 5,7(6H)-dione (BMS-251873) with curative antitumor activity against prostate carcinoma xenograft tumor model.
Balasubramanian BN, St Laurent DR, Saulnier MG, Long BH, Bachand C, Beaulieu F, Clarke W, Deshpande M, Eummer J, Fairchild CR, Frennesson DB, Kramer R, Lee FY, Mahler M, Martel A, Naidu BN, Rose WC, Russell J, Ruediger E, Solomon C, Stoffan KM, Wong H, Wright JJ, Zimmermann K, Vyas DM. Balasubramanian BN, et al. Among authors: zimmermann k. J Med Chem. 2004 Mar 25;47(7):1609-12. doi: 10.1021/jm034197s. J Med Chem. 2004. PMID: 15027851
Discovery of a fluoroindolo[2,3-a]carbazole clinical candidate with broad spectrum antitumor activity in preclinical tumor models superior to the marketed oncology drug, CPT-11.
Saulnier MG, Balasubramanian BN, Long BH, Frennesson DB, Ruediger E, Zimmermann K, Eummer JT, St Laurent DR, Stoffan KM, Naidu BN, Mahler M, Beaulieu F, Bachand C, Lee FY, Fairchild CR, Stadnick LK, Rose WC, Solomon C, Wong H, Martel A, Wright JJ, Kramer R, Langley DR, Vyas DM. Saulnier MG, et al. Among authors: zimmermann k. J Med Chem. 2005 Apr 7;48(7):2258-61. doi: 10.1021/jm049090z. J Med Chem. 2005. PMID: 15801816
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. Among authors: zimmermann k. 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
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. Among authors: zimmermann k. 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
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. 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
Insulin-like growth factor-1 receptor (IGF-1R) kinase inhibitors: SAR of a series of 3-[6-(4-substituted-piperazin-1-yl)-4-methyl-1H-benzimidazol-2-yl]-1H-pyridine-2-one.
Velaparthi U, Saulnier MG, Wittman MD, Liu P, Frennesson DB, Zimmermann K, Carboni JM, Gottardis M, Li A, Greer A, Clarke W, Yang Z, Menard K, Lee FY, Trainor G, Vyas D. Velaparthi U, et al. Among authors: zimmermann k. Bioorg Med Chem Lett. 2010 May 15;20(10):3182-5. doi: 10.1016/j.bmcl.2010.03.057. Epub 2010 Mar 27. Bioorg Med Chem Lett. 2010. PMID: 20399649
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. Among authors: zimmermann k. J Med Chem. 2005 Sep 8;48(18):5639-43. doi: 10.1021/jm050392q. J Med Chem. 2005. PMID: 16134929
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. Among authors: zimmermann k. J Med Chem. 2009 Dec 10;52(23):7360-3. doi: 10.1021/jm900786r. J Med Chem. 2009. PMID: 19778024
712 results