Combretastatin-Chalcone Hybrids: Synthesis and Cytotoxicity

Title: Combretastatin-Chalcone Hybrids: Synthesis and Cytotoxicity

Volume: 3 Issue: 4

Author(s): Nguyen-Hai Nam and Ahn Byung-Zun

Affiliation:

Keywords: Combretastatin, chalcone, synthesis, cytotoxicity

Abstract: 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.

Cite this article as:

Nguyen-Hai Nam and Ahn Byung-Zun , Combretastatin-Chalcone Hybrids: Synthesis and Cytotoxicity, Medicinal Chemistry 2007; 3 (4) . https://dx.doi.org/10.2174/157340607781024366