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

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...

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Detalles Bibliográficos
Autores principales: Azmi, Mohamad Nurul, Md Din, Mohd Fadzli, Kee, Chin Hui, Suhaimi, Munirah, Ping, Ang Kheng, Ahmad, Kartini, Nafiah, Mohd Azlan, Thomas, Noel F., Mohamad, Khalit, Hoong, Leong Kok, Awang, Khalijah
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Molecular Diversity Preservation International (MDPI) 2013
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Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3876051/
https://www.ncbi.nlm.nih.gov/pubmed/24287912
http://dx.doi.org/10.3390/ijms141223369
Descripción
Sumario: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 μM) 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.

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