title: Design, synthesis, and SAR analysis of cytotoxic sinapyl alcohol derivatives.
abstract: Five series totalling 51 of sinapyl alcohol derivatives were designed and synthesized. Their cytotoxicity analyses were performed on six human tumor cell lines such as PC-3, CNE, KB, A549, BEL-7404, and HeLa. Certain sinapyl alcohol derivatives showed significant cytotoxic activities. Compound 14d exhibited especially potent cytotoxicity against the BEL-7404 cell line with an IC50 value of 0.7 microM, which showed more cytotoxic activity than the positive control, cisplatin. The structure-cytotoxicity relationships were discussed and the CoMFA analysis was performed using the cytotoxic data against HeLa cells as a template.
authors.affiliation: Department of Traditional Chinese Medicine and Natural Drug Research, College of Pharmaceutical Sciences, Zhejiang University, 353 Yan An Road, Hangzhou 310031, China.
authors.forename: Hong Bin
authors.initials: HB
authors.lastname: Zou
authors.forename: Sheng Yi
authors.initials: SY
authors.lastname: Dong
authors.forename: Chang Xin
authors.initials: CX
authors.lastname: Zhou
authors.forename: Li Hong
authors.initials: LH
authors.lastname: Hu
authors.forename: Yi Hang
authors.initials: YH
authors.lastname: Wu
authors.forename: Hai Bo
authors.initials: HB
authors.lastname: Li
authors.forename: Jing Xu
authors.initials: JX
authors.lastname: Gong
authors.forename: Lian Li
authors.initials: LL
authors.lastname: Sun
authors.forename: Xiu Mei
authors.initials: XM
authors.lastname: Wu
authors.forename: Hua
authors.initials: H
authors.lastname: Bai
authors.forename: Bo Tao
authors.initials: BT
authors.lastname: Fan
authors.forename: Xiao Jiang
authors.initials: XJ
authors.lastname: Hao
authors.forename: Joachim
authors.initials: J
authors.lastname: Stöckigt
authors.forename: Yu
authors.initials: Y
authors.lastname: Zhao
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D045744:Cell Line, Tumor; D015195:Drug Design; D004354:Drug Screening Assays, Antitumor; D004563:Electrochemistry; D006367:HeLa Cells; D006801:Humans; D020128:Inhibitory Concentration 50; D008958:Models, Molecular; D010666:Phenylpropionates / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D021281:Quantitative Structure-Activity Relationship
chemical_list: D000970:Antineoplastic Agents; D010666:Phenylpropionates; C496130:sinapyl alcohol