Synthesis of new pyrazole derivatives and their anticancer evaluation

被引：98
|
作者：
Nitulescu, George Mihai [1 ]
Draghici, Constantin [2 ]
Missir, Alexandru Vasile [1 ]
机构：
[1] Carol Davila Univ Med & Pharm, Fac Pharm, Dept Pharmaceut Chem, Bucharest 020956, Romania
[2] Romanian Acad Costin D Nenitescu, Organ Chem Ctr, Bucharest 060023, Romania
来源：
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2010年 / 45卷 / 11期
关键词：
1-Methyl-1H-pyrazole-4-carboxylic acid; Acyl thiourea; Thiazolylidenes; Anticancer activity; Pyrazole amines; NATIONAL-CANCER-INSTITUTE; TUMOR-CELL-LINES; ANTITUMOR AGENTS; CDK INHIBITORS; DRUG DISCOVERY; KINASE;
D O I：
10.1016/j.ejmech.2010.07.064
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
A series of functionally substituted pyrazole compounds have been synthesized and evaluated in vitro for their antiproliferative effects on a panel of 60 cellular lines, according to the National Cancer Institute screening protocol. Three of the 12 tested compounds showed moderate antitumor activity, one of them being chosen for the 5-dose assay and presented logGl(50) values up to -5.75. (C) 2010 Elsevier Masson SAS. All rights reserved.
引用
收藏
页码：4914 / 4919
页数：6
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