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

International Journal of Molecular Sciences

Mohamad Nurul Azmi¹  Mohd Fadzli Md Din¹  Chin Hui Kee¹  Munirah Suhaimi¹  Ang Kheng Ping¹  Kartini Ahmad²  Mohd Azlan Nafiah²  Noel F. Thomas¹  Khalit Mohamad³  Leong Kok Hoong³ 

[1] Department of Chemistry, Faculty of Science, University of Malaya, Kuala Lumpur 50603, Malaysia; E-Mails:;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:;Department of Pharmacy, Faculty of Medicine, University of Malaya, 50603 Kuala Lumpur 50603, Malaysia; E-Mails:

关键词: o-carboxamido stilbenes;    amido stilbenes;    Heck protocol;    cytotoxic effects;   

DOI  :  10.3390/ijms141223369

来源: mdpi

【 摘 要 】

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.

【 授权许可】

CC BY   
© 2013 by the authors; licensee MDPI, Basel, Switzerland