Design and synthesis of N-phenylacetyl (sulfonyl) 4,5-dihydropyrazole derivatives as potential antitumor agents

被引：34
|
作者：
Liu, Xin-Hua [1 ,2 ]
Ruan, Ban-Feng [2 ]
Liu, Jing-Xin [2 ]
Song, Bao-An [3 ]
Jing, Ling-Hong [3 ]
Li, Jun [1 ]
Yang, Yang [2 ]
Zhu, Hai-Liang [2 ]
Qi, Xing-Bao [4 ]
机构：
[1] Anhui Med Univ, Sch Pharm, Hefei 230032, Peoples R China
[2] Nanjing Univ, State Key Lab Pharmaceut Biotechnol, Nanjing 210093, 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：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2011年 / 21卷 / 10期
基金：
中国国家自然科学基金;
关键词：
Synthesis; Dihydropyrazole; Antitumor agent; Telomerase inhibitors; TELOMERASE; MOIETY;
D O I：
10.1016/j.bmcl.2011.03.066
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
A series of novel N-phenylacetyl (sulfonyl) 4,5-dihydropyrazole derivatives as potential telomerase inhibitors were synthesized. The bioassay tests show that compound 4a exhibited high activity against human gastric cancer cell SGC-7901, liver cancer Hep-G2 and human prostate PC-3 cell lines with IC50 values of 21.23 +/- 0.99, 29.43 +/- 0.32 and 30.89 +/- 1.07 mu M, respectively. All title compounds were assayed for telomerase inhibition by a modified TRAP assay, the results show that compound 4a can inhibit telomerase with IC50 value of 4.0 +/- 0.32 mu M. Docking simulation was performed to position compound 4a into the telomerase (3DU6) active site to determine the probable binding model. (C) 2011 Elsevier Ltd. All rights reserved.
引用
收藏
页码：2916 / 2920
页数：5
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