556808-20-9Relevant academic research and scientific papers
Synthesis, in vitro, and in vivo evaluation of phosphate ester derivatives of combretastatin A-4
Hadimani, Mallinath B.,Hua, Jianyi,Jonklaas, M. Devan,Kessler, Raymond J.,Sheng, Yezhou,Olivares, Adrian,Tanpure, Rajendra P.,Weiser, Aimee,Zhang, Jianxing,Edvardsen, Klaus,Kane, Robert R.,Pinney, Kevin G.
, p. 1505 - 1508 (2003)
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 μM), 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.
