Combretastatin biological activity

Brown T, Holt H Jr, Lee M (2006) Synthesis of Biologically Active Heterocyclic StUbene and Chalcone Analogs of Combretastatin. 2 1-51... 

It has been shown that combretastatin A-4 disrupts the microtubules of human umbilical vein endothelial cells (HUVECs) in culture, thus confirming that the tubulin binding properties shown in cell-free systems are retained when the compound enters cells and that tubulin binding is a significant component of the biological activity. Also 3-fluoro- and 3-chloro derivatives retained activity in human umbilical vein endothelial cells. This kind of activity against endothelial cells is extremely important, as endothelial cells play a key role in the angiogenic process. 

Benzo[b]furan and indole analogues of some recently identified benzo[b]thiophene inhibitors of tubulin polymerization have been synthesized, and their biological activity has been investigated. Among them, the compound 2-(3-hydroxy,4-methoxyphenyl),3-(3,4,5-trimethoxybenzoyl)-6-methoxyfuran-2-one 81 was the most active, exhibiting 5 times the level of potency of Combretastatin A-4. However, it is less potent than Combretastatin A-4 as inhibitor of [3H]colchicine... 

Many stilbene derivates (stilbenoids) are naturally present in plants. The most widely distributed stilbenoids are resveratrol, combretastatins, and pterostilbene. These agents are derived from terrestrial plants, microorganisms, marine organisms, and animals [1,2]. This chapter is a brief review on diverse biological activities of stilbenes in cells, organs, and animals. 

StUbenes such as resveratrol, combretastatin, and pterostUbene and their analogues possess a wide spectrum of biological activities. These compounds have been proved to be antioxidant reagents that cause cell apoptosis, suppress growing cancer cells, inhibit and activate spedfic enzymes, effed the animal aging and metabolisms... 

Synthesis of Biologically Active Heterocyclic Stilbene and Chalcone Analogs of Combretastatin... 

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