title: Synthesis, biological evaluation, and molecular docking studies of resveratrol derivatives possessing chalcone moiety as potential antitubulin agents.
abstract: Twenty-three resveratrol derivatives possessing chalcone moiety were synthesized and characterized, and their biological activities were also evaluated as potential antiproliferation and tubulin polymerization inhibitors. Compound C19 exhibited the most potent activity in vitro, which inhibited the growth of HepG2, B16-F10, and A549 cell lines with IC(50) values of 0.2, 0.1, and 1.4 μg/mL, respectively. Compound C19 also exhibited significant tubulin polymerization inhibitory activity (IC(50)=2.6 μg/mL). Docking simulation was performed to position compound C19 into the tubulin-colchicine binding site to determine the probable binding mode.
authors: State Key Laboratory of Pharmaceutical Biotechnology, Nanjing University, Nanjing, PR China.
authors: Ban-Feng
authors: BF
authors: Ruan
authors: Xiang
authors: X
authors: Lu
authors: Jian-Feng
authors: JF
authors: Tang
authors: Yao
authors: Y
authors: Wei
authors: Xiao-Liang
authors: XL
authors: Wang
authors: Yan-Bin
authors: YB
authors: Zhang
authors: Li-Sheng
authors: LS
authors: Wang
authors: Hai-Liang
authors: HL
authors: Zhu
mesh_terms: D001665:Binding Sites; D045744:Cell Line, Tumor; D002599:Chalcone / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D006801:Humans; D011485:Protein Binding; D000077185:Resveratrol; D013267:Stilbenes / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D050257:Tubulin Modulators / Q000138:chemical synthesis*
chemical_list: D013267:Stilbenes; D050257:Tubulin Modulators; D002599:Chalcone; D000077185:Resveratrol