Synthesis and biological activity of some novel Combretastatin analogues and related compounds

Abstract

http://dx.doi.org/10.21276/IJRDPL.227 8-0238.2017.6(4).2720-2725 ABSTRACT: CA-4 is a biologically very active compound by binding to the colchicine binding site which lead to the inhibition of microtubule polymerization as well as showing antiagiogenic and anticancer effects by selectively shutting down the tumor blood flow. To avoid the disadvantage of rather low in vivo efficiacy resulting from the isomerization of the cisstilbene derivative to the thermodynamically more stable trans-isomer, our research group started the project for CA-4 analogs synthesis. The incorporation of carbocycles with different ring sizes on the connecting carbonbridge of the natural compound prevents the system to undergo cis-trans-isomerization. The synthesis of the cyclopropane derivative of CA-4 via the cyclopropanation reaction with diazomethane, and further analogs with incorporated moieties for better water solubility.