Abstract
BPR0L075 (2) is a potential anticancer drug candidate designed from Combretastatin A-4 (1) based on the bioisosterismprinciple.Metabolites of 2, proposed from in vitrohumanmicrosome 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.
Original language | English |
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Pages (from-to) | 4941-4945 |
Number of pages | 5 |
Journal | Journal of Medicinal Chemistry |
Volume | 52 |
Issue number | 15 |
DOIs | |
Publication status | Published - Aug 13 2009 |
ASJC Scopus subject areas
- Molecular Medicine
- Drug Discovery