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RESEARCH PRODUCT

Design, synthesis, and SAR analysis of cytotoxic sinapyl alcohol derivatives.

Chang Xin ZhouYu ZhaoLi Hong HuBo Tao FanHongbin ZouHua BaiXiao Jiang HaoSheng Yi DongJing Xu GongJoachim StöckigtXiu Mei WuYi Hang WuLian Li SunHaibo Li

subject

Models MolecularClinical BiochemistryPharmaceutical ScienceQuantitative Structure-Activity RelationshipAntineoplastic AgentsBiochemistryChemical synthesisHeLachemistry.chemical_compoundInhibitory Concentration 50Cell Line TumorDrug DiscoveryElectrochemistryCytotoxic T cellHumansCytotoxicityMolecular BiologyIC50biologyPhenylpropionatesOrganic Chemistrybiology.organism_classificationIn vitroSinapyl alcoholchemistryBiochemistryCell cultureDrug DesignMolecular MedicineDrug Screening Assays AntitumorHeLa Cells

description

Five series totalling 51 of sinapyl alcohol derivatives were designed and synthesized. Their cytotoxicity analyses were performed oil 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 mu M, 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. (c) 2005 Elsevier Ltd. All rights reserved.

yearjournalcountryeditionlanguage
2005-09-28Bioorganicmedicinal chemistry
10.1016/j.bmc.2005.10.056https://pubmed.ncbi.nlm.nih.gov/16303311