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Page 1
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: stoffan k. J Med Chem. 2005 Sep 8;48(18):5639-43. doi: 10.1021/jm050392q. J Med Chem. 2005. PMID: 16134929
Novel 1H-(benzimidazol-2-yl)-1H-pyridin-2-one inhibitors of insulin-like growth factor I (IGF-1R) kinase.
Wittman MD, Balasubramanian B, Stoffan K, Velaparthi U, Liu P, Krishnanathan S, Carboni J, Li A, Greer A, Attar R, Gottardis M, Chang C, Jacobson B, Sun Y, Hansel S, Zoeckler M, Vyas DM. Wittman MD, et al. Among authors: stoffan k. Bioorg Med Chem Lett. 2007 Feb 15;17(4):974-7. doi: 10.1016/j.bmcl.2006.11.041. Epub 2006 Nov 17. Bioorg Med Chem Lett. 2007. PMID: 17187980
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: stoffan 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
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: stoffan km. 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: stoffan km. J Med Chem. 2005 Apr 7;48(7):2258-61. doi: 10.1021/jm049090z. J Med Chem. 2005. PMID: 15801816