Novel 3-(2-(3-methyl-5-substituted-phenyl-4,5-dihydropyrazol-1-yl)-2-oxoethoxy)-2-substituted-phenyl-4H-chromen-4-one: Synthesis and Anticancer Activity

被引：5
|
作者：
Liu, Xin-Hua [1 ,2 ]
Li, Jun [1 ]
Wu, Fan-Rong [1 ]
Song, Bao-An [3 ]
Bhadury, Pinaki S. [3 ]
Shi, Lei [4 ]
机构：
[1] Anhui Med Univ, Sch Pharm, Hefei 230032, Peoples R China
[2] Nanjing Univ, State Key Lab Pharmaceut Biotechnol, Nanjing 210093, Jiangsu, Peoples R China
[3] Guizhou Univ, Educ Minist, Key Lab Green Pesticide & Agr Bioengn, Guiyang 550025, Peoples R China
[4] China Pharmaceut Univ, Sch Pharm, Nanjing 210009, Peoples R China
来源：
MEDICINAL CHEMISTRY | 2011年 / 7卷 / 06期
基金：
中国国家自然科学基金;
关键词：
4H-chromen; dihydropyrazole; molecular docking; anticancer activity; ANTIBACTERIAL ACTIVITY; DERIVATIVES SYNTHESIS;
D O I：
10.2174/157340611797928442
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Ten novel 3-(2-(3-methyl-5-substituted-phenyl-4,5-dihydropyrazol-1-yl)-2-oxo-ethoxy)-2-substituted-phenyl-4H-chromen-4-one derivatives were synthesized and characterized by H-1 NMR and C-13 NMR. All of the compounds have been screened for their anticancer activity. The bioassay tests show that compound 6af exhibited potentially high activity against human gastric cancer cell SGC-7901 with IC50 value of 4.01 +/- 0.97 mu g/mL. Also, the title compounds were assayed for telomerase inhibition. The results show that compounds 6cf, 6af can strongly inhibit telomerase with IC50 values of 4.89 +/- 0.11 and 5.02 +/- 0.91 mu M, respectively. Docking simulation was performed to position compound 6cf into the telomerase (3DU6) active site to determine the probable binding model.
引用
收藏
页码：605 / 610
页数：6
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