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

Azmi, Mohamad Nurul and Md Din, Mohd Fadzli and Kee, Chin Hui and Suhaimi, Munirah and Ang, Kheng Ping and Ahmad, Kartini and Nafiah, Mohd Azlan and Thomas, Noel Francis and Leong, Kok Hoong and Awang, Khalijah (2013) Design, synthesis and cytotoxic evaluation of o-carboxamido stilbene analogues. International Journal of Molecular Sciences, 14 (12). pp. 23369-23389. ISSN 1661-6596, DOI

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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.

Item Type: Article
Funders: University of Malaya Postgraduate Research Grant (PPP) (PV090/2011A) and (PV050/2012A), Ministry of Higher Education (MOHE) Fundamental Research Grant Scheme (2010-0063-101-02), 02), University of Malaya Research Grant (UMRG) (RP001/2012B), ScienceFund (SF018-2013)
Uncontrolled Keywords: o-carboxamido stilbenes; amido stilbenes; Heck protocol; cytotoxic effects
Subjects: Q Science > Q Science (General)
Q Science > QD Chemistry
Q Science > QH Natural history > QH301 Biology
R Medicine
R Medicine > RC Internal medicine > RC0254 Neoplasms. Tumors. Oncology (including Cancer)
R Medicine > RM Therapeutics. Pharmacology
R Medicine > RS Pharmacy and materia medica
Divisions: Faculty of Medicine
Faculty of Science > Department of Chemistry
Depositing User: Dr. Leong Kok Hoong
Date Deposited: 22 May 2014 02:10
Last Modified: 13 Feb 2019 03:03

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