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KMID : 0043320130360060684
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Archives of Pharmacal Research
2013 Volume.36 No. 6 p.684 ~ p.693
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Synthesis of new 1,3,4-benzotriazepin-5-one derivatives and their biological evaluation as antitumor agents
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Taher Azza T.
Mohammed Lamia W.
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Abstract
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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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KEYWORD
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1,3,4-benzotriazepin-5-one derivatives, Synthesis, Antitumor activity
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