Design, synthesis and cytotoxic evaluation of o-carboxamido stilbene analogues

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Abstract

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 (IC 50 = 16.68 μM), colon cancer HT-29 (IC 50 = 7.51 μ M) and breast cancer MCF-7 (IC 50 = 21.24 μM), respectively, which are comparable with vinblastine. The resveratrol analogues were synthesized using the Heck method. © 2013 by the authors; licensee MDPI, Basel, Switzerland.

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Azmi, M. N., Md Din, M. F., Kee, C. H., Suhaimi, M., Ping, A. K., Ahmad, K., … Awang, K. (2013). Design, synthesis and cytotoxic evaluation of o-carboxamido stilbene analogues. International Journal of Molecular Sciences, 14(12), 23369–23389. https://doi.org/10.3390/ijms141223369

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