Synthesis of novel 6,6a,7,8-tetrahydro-5H-naphtho[1,2-e]pyrimido[4,5-b][1,4]diazepines under microwave irradiation as potential anti-tumor agents

被引：25

作者：

Insuasty, Braulio ^{[1
]}

Garcia, Angelica ^{[1
]}

Quiroga, Jairo ^{[1
]}

Abonia, Rodrigo ^{[1
]}

Nogueras, Manuel ^{[2
]}

Cobo, Justo ^{[2
]}

机构：

[1] Univ Valle, Dept Chem, Heterocycl Cpds Res Grp, Cali 25360, Colombia

[2] Univ Jaen, Dept Inorgan & Organ Chem, Jaen 23071, Spain

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2010年 / 45卷 / 07期

关键词：

Aminopyrimidines; Arylidene-1-tetralones; Naphtho[1,2-e]pyrimido[4,5-b][1,4]diazepines; Microwave irradiation; Antitumoral activity; ORGANIC SYNTHESES; ONE-STEP; 6-AMINOPYRIMIDINES; CYCLOCONDENSATION; INHIBITORS; KETONES;

D O I：

10.1016/j.ejmech.2010.03.004

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A new series of 6,6a,7,8-tetrahydro-5H-naphtho[1,2-e]pyrimido[4,5-b][1,4]diazepines 4a-f and 5a-f were efficiently synthesized in good yields from the reaction of E-2-arylidene-1-tetralones 1 and the respective tri- or tetraaminopyrimidines 2 or 3 under microwave irradiation using DMF as solvent and catalytic amounts of BF3 center dot OEt2. Six of the obtained compounds were selected and tested by the National Cancer Institute (NCI-USA) against 60 different tumor cell lines. In particular, compounds 5a, 5c and Se presented remarkable anti-tumor activity against melanoma cancer in SK-MEL-5 cell line. (C) 2010 Elsevier Masson SAS. All rights reserved.

引用

页码：2841 / 2846

页数：6

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