Design, Synthesis and Cytotoxic Evaluation of o-Carboxamido Stilbene Analogues.

Autor: Azmi, Mohamad Nurul, Md Din, Mohd Fadzli, Chin Hui Kee, Suhaimi, Munirah, Ang Kheng Ping, Ahmad, Kartini, Nafiah, Mohd Azlan, Thomas, Noel F., Mohamad, Khalit, Leong Kok Hoong, Awang, Khalijah
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Zdroj: International Journal of Molecular Sciences; Dec2013, Vol. 14 Issue 12, p23369-23389, 21p, 2 Diagrams, 1 Chart, 1 Graph
Abstrakt: Resveratrol, a natural stilbene found in grapes and wines exhibits a wide range of pharmacological properties. Resveratrol is also known as a good chemopreventive agent for inhibiting carcinogenesis processes that target kinases, cyclooxygenases, ribonucleotide reductase and DNA polymerases. A total of 19 analogues with an amide moiety were synthesized and the cytotoxic effects of the analogues on a series of human cancer cell lines are reported. Three compounds 6d, 6i and 6n showed potent cytotoxicity against prostate cancer DU-145 (IC50 = 16.68 µM), colon cancer HT-29 (IC50 = 7.51 µM) and breast cancer MCF-7 (IC50 = 21.24 µM), respectively, which are comparable with vinblastine. The resveratrol analogues were synthesized using the Heck method. [ABSTRACT FROM AUTHOR]
Databáze: Complementary Index