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 |
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| Authors: | Saulnier Mark G Balasubramanian Balu N Long Byron H Frennesson David B Ruediger Edward Zimmermann Kurt Eummer Jeffrey T St Laurent Denis R Stoffan Karen M Naidu B Narasimhulu Mahler Mikael Beaulieu Francis Bachand Carol Lee Frank Y Fairchild Craig R Stadnick Linda K Rose William C Solomon Carola Wong Henry Martel Alain Wright John J Kramer Robert Langley David R Vyas Dolatrai M |
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| Institution: | The Bristol-Myers Squibb Pharmaceutical Research Institute, 5 Research Parkway, Wallingford, Connecticut 06492, USA. Mark.Saulnier@bms.com |
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| Abstract: | A series of fluoroglycosylated fluoroindolocarbazoles was examined with respect to their topoisomerase I activity, cytotoxicity, and selectivity. The lead clinical candidate from this series, BMS-250749, displays broad spectrum antitumor activity superior to CPT-11 against some preclinical xenograft models, including curative antitumor activity against Lewis lung carcinoma. |
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