Novel 3-(1-acetyl-5-(substituted-phenyl)-4,5-dihydro-1H-pyrazol-3-yl)-7-fluoro-2H-chromen-2-one Derivatives: Synthesis and Anticancer Activity

被引：17

作者：

Cai, Zheng-Yu ^{[1
]}

Yang, Yang ^{[1
]}

Liu, Xin-Hua ^{[1
]}

Qi, Xing-Bao ^{[2
]}

机构：

[1] Anhui Univ Technol, Sch Chem & Chem Engn, Maanshan 243002, Peoples R China

[2] China Pharmaceut Univ, Sch Pharm, Nanjing 210009, Peoples R China

来源：

LETTERS IN DRUG DESIGN & DISCOVERY | 2010年 / 7卷 / 09期

基金：

中国国家自然科学基金;

关键词：

Coumarin; Dihydropyrazole; Molecular Docking; Antitumor Agent; ANTIBACTERIAL ACTIVITY;

D O I：

10.2174/157018010792929540

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of novel coumarin derivatives containing 4,5-dihydropyrazole moiety as potential telomerase inhibitors were synthesized. The bioassay tests showed that compound 3b exhibited potentially high activity against human gastric cancer cell SGC-7901 with IC50 value was 2.98 +/- 0.16. Docking simulation was performed to position compound 3b into the telomerase (3DU6) active site to determine the probable binding model. The result shows that some coumarin containing 4,5-dihydropyrazole moiety can combine well with the telomerase active site and may have use as potential telomerase inhibitors.

引用

页码：640 / 643

页数：4

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