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.
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.
Reaction between 2-(N-methyl)dichloroacetamido-5-chlorobenzoplenone and aqueous ammonia yields l-methyl-3-amino-3,4-dihydroxy-4-phenyl-6-chloro-1,2,3,4-tetral~ydroquinoline-2-one which dehydrates readily to give the title compound. Structural proof of this substance is reported and several of its transformation products are described.
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