Author/Authors :
Mallinath B. Hadimani، نويسنده , , Jianyi Hua، نويسنده , , M. Devan Jonklaas، نويسنده , , Raymond J. Kessler، نويسنده , , Yezhou Sheng، نويسنده , , Adrian Olivares، نويسنده , , Rajendra P. Tanpure، نويسنده , , Aimee Weiser، نويسنده , , Jianxing Zhang، نويسنده , , Klaus Edvardsen، نويسنده , , Robert R. Kane، نويسنده , , Kevin G. Pinney، نويسنده ,
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 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.
