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排名必读论文期刊顶会热点AI 简史溯源树小脉星探人才迁徙塔尖人才国防情报追踪开源工具智慧手语
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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.

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

JOURNAL OF MEDICINAL CHEMISTRY（2005）

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摘要
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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