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Bioorg Med Chem Lett. 2003 May 5;13(9):1505-8.

Synthesis, in vitro, and in vivo evaluation of phosphate ester derivatives of combretastatin A-4.

Author information

1
Department of Chemistry & Biochemistry, Center for Drug Discovery, Baylor University, Waco, TX 76798-7348, USA.

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 (IC(50)=1-2 microM), 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 CA4P analogues.

PMID:
12699742
DOI:
10.1016/s0960-894x(03)00206-3
[Indexed for MEDLINE]

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