Design, synthesis, and SAR analysis of cytotoxic sinapyl alcohol derivatives.
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.
Zou
Hong Bin
HB
Department of Traditional Chinese Medicine and Natural Drug Research, College of Pharmaceutical Sciences, Zhejiang University, 353 Yan An Road, Hangzhou 310031, China.
Dong
Sheng Yi
SY
Zhou
Chang Xin
CX
Hu
Li Hong
LH
Wu
Yi Hang
YH
Li
Hai Bo
HB
Gong
Jing Xu
JX
Sun
Lian Li
LL
Wu
Xiu Mei
XM
Bai
Hua
H
Fan
Bo Tao
BT
Hao
Xiao Jiang
XJ
Stöckigt
Joachim
J
Zhao
Yu
Y
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
D000970:Antineoplastic Agents; D010666:Phenylpropionates; C496130:sinapyl alcohol