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

页码：2916 / 2920

页数：5

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