新型香豆素二氢吡唑硫代乙酮衍生物的合成及其抗肿瘤活性

Synthesis and Anticancer Activities of Novel Coumarin-dihydropyrazole Thio-ethanone Derivatives

以3-乙酰基-6-香豆素为起始原料,设计并合成了一系列新型香豆素二氢吡唑硫代乙酮衍生物(6a^6g),其结构经1H NMR和元素分析表征。初步体外生物活性测定结果表明:丁硫基乙酰三氟甲基苯基香豆素二氢吡唑(6a)和丙硫基乙酰苯基香豆素二氢吡唑(6f)对癌细胞SGC-7901,MGC-803,Bcap-37和HepG-2具有较高的抑制增殖活性。用改进的TRAP法测试了6a,6e和6f的端粒酶活性,其中6f具有很强的抑制活性,其IC50为(1.27±0.18)μM。

A series novel coumarin-dihydropyrazole thio-ethanone derivatives were designed and synthesized from 3-acetyl-6-coumarin.The structures were characterized by 1H NMR and elemental analysis.The preliminary in vitro biological activities tests showed that [（butylthio）acetyl]-5-[2-（trifluoromethyl） phenyl]-dihydropyrazole （6a） and [（propylthio） acetyl]-5-[2-（trifluoromethyl） phenyl]-dihydropyrazole（6f） exhibited high anticancer activities against SGC-7901,MGC-803,Bcap-37 and HepG-2 cell lines.6a,6e and 6f were tested against telomerase by a modified TRAP assay and 6f showed the most potent inhibitory activity with IC50value of （1.27 ±0.18）μM.