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- Hadimani, MB, et al.
(författare)
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Synthesis, in vitro, and in vivo evaluation of phosphate ester derivatives of combretastatin A-4
- 2003
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Ingår i: Bioorganic & Medicinal Chemistry Letters. - 0960-894X. ; 13:9, s. 1505-1508
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Tidskriftsartikel (refereegranskat)abstract
- Combretastatin A-4 disodiumphosphate (CA4P), a prodrug formulation of the natural product combretastatin A-4 (CA4), is currently in clinical investigation for the treatment of cancer. In vivo, CA4P is rapidly enzymatically converted to CA4, a potent inhibitor of tubulin polymerization (IC50 = 1-2 muM), and rapidly causes bloodflow shutdown in tumor tissues. A variety of alkyl and aryl di- and triesters of CA4P have been synthesized and evaluated as potential CA4 prodrugs and/or stable CAV analogues. (C) 2003 Elsevier Science Ltd. All rights reserved.
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