Synthesis of new 1,3,4-benzotriazepin-5-one derivatives and their biological evaluation as antitumor agents

被引:0
作者
Azza T. Taher
Lamia W. Mohammed
机构
[1] Cairo University,Department of Organic Chemistry, Faculty of Pharmacy
来源
Archives of Pharmacal Research | 2013年 / 36卷
关键词
1,3,4-benzotriazepin-5-one derivatives; Synthesis; Antitumor activity;
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学科分类号
摘要
New derivatives of 1,3,4-benzotriazepin-5-one were designed and synthesized as structural analogues to the antitumor agents devazepide and asperlicin. An efficient and novel approach to the synthesis of 2-amino-1,3,4-benzotriazepin-5-one 2 was developed and its structure was confirmed. The newly synthesized derivatives were evaluated for their in vitro antitumor activity on 60 different cell lines. Compounds 8 and 9 displayed the most potent antitumor activity against several cell lines specifically ovarian cancer, renal cancer and prostate cancer, while compounds 5, 10 and 12 showed significant activities against UO-31 renal cancer cell line.
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页码:684 / 693
页数:9
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