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W1965038511 abstract "BPR0L075 (2) is a potential anticancer drug candidate designed from Combretastatin A-4 (1) based on the bioisosterism principle. Metabolites of 2, proposed from in vitro human microsome studies, were synthesized, leading to the identification of metabolite-derived analogue 10 with 40−350 pM potency against various cancer cell lines. Insights gained from the major inactive metabolite of 2 led to the development of 29, with better pharmacokinetics and improved potency in the tumor xenograft model than 2." @default.
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W1965038511 date "2009-07-08" @default.
W1965038511 modified "2023-10-09" @default.
W1965038511 title "Synthesis and Evaluation of 3-Aroylindoles as Anticancer Agents: Metabolite Approach" @default.
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W1965038511 doi "https://doi.org/10.1021/jm900060s" @default.
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