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以4-氟苯甲酸(Ⅰ)为原料,通过酯化、肼解制得4-氟苯甲酰肼(Ⅱ),Ⅱ再与芳香醛反应得到相应的酰腙(Ⅲa～Ⅲh),最后以苯和二甲基甲酰胺(DMF)为溶剂,Ⅲa～Ⅲh与巯基乙酸脱水环化成2-芳基-3-(4-氟苯甲酰胺基)-4-噻唑啉酮类化合物(Ⅳa～Ⅳh),并利用IR、1HNMR、13CNMR、ESI-MS和元素分析对Ⅳa～Ⅳh的结构进行了表征,用MTT法评价了体外对HepG-2、A549-1和231-2的3种癌细胞株的体外生长抑制活性。结果表明,Ⅳa～Ⅳh均具有潜在的体外抑制癌细胞生长活性,其中,Ⅳb,Ⅳf活性最强。
4-Fluorobenzoylhydrazide (Ⅱ) was prepared by esterification and hydrazinolysis from 4-fluorobenzoic acid (Ⅰ), and then reacted with aromatic aldehyde to give the corresponding acyl hydrazones (Ⅲa ~ Ⅲh) Benzene and dimethylformamide (DMF) as solvent, dehydration and cyclization of Ⅲa ~ Ⅲh and thioglycolic acid into 2-aryl-3- (4-fluorobenzamido) -4-thiazolinones (Ⅳa ~ Ⅳh ), And the structures of Ⅳa ~ Ⅳh were characterized by IR, 1HNMR, 13CNMR, ESI-MS and elemental analysis. The effects of HepG-2, A549-1 and 231-2 on three cancer cell lines In vitro growth inhibitory activity. The results showed that Ⅳa ~ Ⅳh all have the potential to inhibit the growth of cancer cells in vitro, of which, Ⅳb, Ⅳf the strongest activity.