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-β- 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

Balu Balasubramanian ,B Narasimhulu Naidu,Mark G Saulnier,Denis R St Laurent,Byron H Long,Carol Bachand,Wendy Clarke,Alain Martel,David B Frennesson,Henry Wong,Carola Solomon,Milind Deshpande,Jeffrey Eummer,Dolatrai M Vyas,Craig R Fairchild,William C Rose,Kurt Zimmermann,Mikael Mahler,Françis Beaulieu ,E H Ruediger ,Robert A Kramer ,Karen Stoffan ,Frank Y Lee ,John J Wright ,John Wellesley Russell

doi:10.1021/jm034197s

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-β- 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

Balu Balasubramanian , B Narasimhulu Naidu + Show 23 more

https://doi.org/10.1021/jm034197s

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Journal: Journal of Medicinal Chemistry	Publication Date: Feb 20, 2004
Citations: 37

Affiliation: Bristol-Myers Squibb (United States)

#Prostate Carcinoma #Antitumor Activity + Show 6 more

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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.

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