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Synthesis and antitumor evaluation of some new 1,3,4-oxadiazole-based heterocycles

被引：191
作者：
Bondock, Samir [1 ,2 ]
Adel, Shymaa [1 ]
Etman, Hassan A. [1 ]
Badria, Farid A. [3 ]
机构：
[1] Mansoura Univ, Fac Sci, Dept Chem, ET-35516 Mansoura, Egypt
[2] King Khalid Univ, Fac Sci, Dept Chem, Abha 9004, Saudi Arabia
[3] Mansoura Univ, Fac Pharm, Dept Pharmacognosy, ET-35516 Mansoura, Egypt
来源：
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2012年 / 48卷
关键词：
1,3,4-Oxadiazole; Pyrazole; Thiazole; Thiophene; Antitumor activity; SUBSTITUTED PYRAZOLYL-1,3,4-OXADIAZOLES; ANTIMICROBIAL ACTIVITY; CONVENIENT SYNTHESIS; DERIVATIVES; THIAZOLE; AGENTS;
D O I：
10.1016/j.ejmech.2011.12.013
中图分类号：
R914 [药物化学];
学科分类号：
100705 [微生物与生化药学];
摘要：
The synthetic strategies and characterization of some novel 1,3,4-oxadiazole derivatives carrying different pharmacophores and heterocyclic rings that are relevant to potential antitumor and cytotoxic activities are described. The antitumor activities of the newly synthesized compounds were evaluated according to the protocol of the National Cancer Institute (NCI) in-vitro disease-oriented human cells screening panel assay. The results revealed that five compounds, namely 2, 7a, ha, 12b, and 17; displayed promising in-vitro antitumor activity in the 4-cell lines assay. Incorporating a thiazole ring to 1,3,4-oxadiazole skeleton resulted in better antitumor activities than those displayed by the pyrazole and thiophene ring systems. Transformation of 1,3,4-oxadiazole 2 to N-(6-amino-7H-pyrazolo[5,1-c][1,2,4] triazol-3-yl)benzamide (15) diminished the antitumor activity. (C) 2011 Elsevier Masson SAS. All rights reserved.
引用
收藏
页码：192 / 199
页数：8
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