Design,Synthesis and Cytotoxic Evaluation of o-Carboxamido Stilbene Analogues |
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| Authors: | Mohamad Nurul Azmi Mohd Fadzli Md Din Chin Hui Kee Munirah Suhaimi Ang Kheng Ping Kartini Ahmad Mohd Azlan Nafiah Noel F Thomas Khalit Mohamad Leong Kok Hoong Khalijah Awang |
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| Affiliation: | 1.Department of Chemistry, Faculty of Science, University of Malaya, Kuala Lumpur 50603, Malaysia; E-Mails: (M.N.A.); (M.F.D.); (C.H.K.); (M.S.); (A.K.P.); (N.F.T.);2.Department of Chemistry, Faculty of Science and Mathematics, Sultan Azlan Shah Campus, University Pendidikan Sultan Idris, Proton City 35950, Perak Darul Ridzuan, Malaysia; E-Mails: (K.A.); (M.A.N.);3.Department of Pharmacy, Faculty of Medicine, University of Malaya, 50603 Kuala Lumpur 50603, Malaysia; E-Mails: (K.M.); (L.K.H.) |
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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 (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. |
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| Keywords: | o-carboxamido stilbenes amido stilbenes Heck protocol cytotoxic effects |
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