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

作者：Azmi Mohamad Nurul; Din Mohd Fadzli Md; Kee Chin Hui; Suhaimi Munirah; Ping Ang Kheng; Ahmad Kartini; Nafiah Mohd Azlan; Thomas Noel F; Mohamad Khalit; Hoong Leong Kok; Awang Khalijah^*

来源：International Journal of Molecular Sciences, 2013, 14(12): 23369-23389.

DOI：10.3390/ijms141223369

• o-carboxamido stilbenes
• amido stilbenes
• Heck protocol
• cytotoxic effects

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 M), colon cancer HT-29 (IC50 = 7.51 M) and breast cancer MCF-7 (IC50 = 21.24 M), respectively, which are comparable with vinblastine. The resveratrol analogues were synthesized using the Heck method.

• 出版日期2013-12