Design and synthesis of a fluoroindolocarbazole series as selective topoisomerase I active agents. Discovery of water-soluble 3,9-difluoro-12,13-dihyd...
Basic Information
ID: ALA1149111
Journal: J Med Chem
Title: 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.
Authors: 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.
Abstract: A series of fluoroindolocarbazoles were studied with respect to their topoisomerase I activity, cytotoxicity, selectivity, and in vivo antitumor activity. Emerging from this series was BMS-251873, a potential clinical candidate possessing a robust pharmacological profile including curative antitumor activity against prostate carcinoma.
CiteXplore: 15027851
DOI: 10.1021/jm034197s
Patent ID: ┄