Novel 5-(2-hydroxyphenyl)-3-substituted-2,3-dihydro-1,3,4-oxadiazole-2-thione derivatives: Promising anticancer agents

被引：190
|
作者：
Aboraia, AS [1 ]
Abdel-Rahman, HM [1 ]
Mahfouz, NM [1 ]
El-Gendy, MA [1 ]
机构：
[1] Assiut Univ, Fac Pharm, Pharmaceut Med Chem Dept, Assiut 71526, Egypt
来源：
BIOORGANIC & MEDICINAL CHEMISTRY | 2006年 / 14卷 / 04期
关键词：
anticancer activity; 1,3,4-oxadiazoles; Mannich basest; salicylate analogs;
D O I：
10.1016/j.bmc.2005.09.053
中图分类号：
Q5 [生物化学]; Q7 [分子生物学];
学科分类号：
071010 ; 081704 ;
摘要：
A series of 5-(2-hydroxyphenyl)-3-susstituted-2,3-dihydro-1,3,4-oxadiazole-2-thione derivatives was synthesized and 13 of them were selected by the National Cancer Institute (NCl) and evaluated for their in vitro anticancer activity. Seven of the investigated compounds, 3i, 3j, 3k, 3o, 3p, 3q, and 3r, displayed high anticancer activity in the primary assay. These compounds have been selected for a full anticancer screening against a 60-cell panel assay where they showed non-selective broad spectrum and promising activity against all cancer cell lines. Compounds 3j and 3k proved to be the active members in this Study compared to 5-fluorouracil and cyclophosphamide as reference drugs, respectively. Compounds 3j and 3k were identified as promising lead compounds. (c) 2005 Elsevier Ltd. All rights reserved.
引用
收藏
页码：1236 / 1246
页数：11
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