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Combretastatin-Chalcone Hybrids: Synthesis and Cytotoxicity

[ Vol. 3 , Issue. 4 ]


Nguyen-Hai Nam and Ahn Byung-Zun   Pages 373 - 377 ( 5 )


A series of all-trans-1-aryl-4-aryl-5-aryl-2,4-pentanediene-1-one (3), a hybridized form of chalcone and combretastatin, was synthesized and evaluated against a panel of cancer cell lines, including B16, murine melanoma; HCT116, colon cancer; A431, human epidermoid carcinoma; and human umbilical venous endothelial cells (HUVEC). Structure-activity relationships analysis of this series revealed that a 2,5-dihydroxyphenyl at position 1 of the 2,4- pentanediene-1-one was essential for cytotoxicity. all-trans-1-(2,5-Dihydroxyphenyl)-5-(4-methoxyphenyl)-4-(3,4,5- trimethoxyphenyl)-2,4-pentanediene-1-one (3a) was the most potent compound from this series.


Combretastatin, chalcone, synthesis, cytotoxicity


Department of Pharmaceutical Chemistry, Hanoi University of Pharmacy, 13-15 Le Thanh Tong, Hanoi, Vietnam.

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