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
收藏
页码：640 / 643
页数：4
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