title: Design, synthesis and cytotoxic evaluation of o-carboxamido stilbene analogues.
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.
authors.affiliation: Department of Chemistry, Faculty of Science, University of Malaya, Kuala Lumpur 50603, Malaysia. khalijah@um.edu.my.
authors.forename: Mohamad Nurul
authors.initials: MN
authors.lastname: Azmi
authors.forename: Mohd Fadzli Md
authors.initials: MF
authors.lastname: Din
authors.forename: Chin Hui
authors.initials: CH
authors.lastname: Kee
authors.forename: Munirah
authors.initials: M
authors.lastname: Suhaimi
authors.forename: Ang Kheng
authors.initials: AK
authors.lastname: Ping
authors.forename: Kartini
authors.initials: K
authors.lastname: Ahmad
authors.forename: Mohd Azlan
authors.initials: MA
authors.lastname: Nafiah
authors.forename: Noel F
authors.initials: NF
authors.lastname: Thomas
authors.forename: Khalit
authors.initials: K
authors.lastname: Mohamad
authors.forename: Leong Kok
authors.initials: LK
authors.lastname: Hoong
authors.forename: Khalijah
authors.initials: K
authors.lastname: Awang
mesh_terms: D016588:Anticarcinogenic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000633:toxicity; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D015195:Drug Design; D004354:Drug Screening Assays, Antitumor; D019073:HT29 Cells; D006801:Humans; D061986:MCF-7 Cells; D000077185:Resveratrol; D013267:Stilbenes / Q000138:chemical synthesis / Q000737:chemistry* / Q000633:toxicity
chemical_list: D016588:Anticarcinogenic Agents; D013267:Stilbenes; D000077185:Resveratrol