Archives of Pharmacal Research

, Volume 36, Issue 6, pp 684–693 | Cite as

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

  • Azza T. TaherEmail author
  • Lamia W. Mohammed
Research Article


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.


1,3,4-benzotriazepin-5-one derivatives Synthesis Antitumor activity 



Thanks are due to the NCI, Bethesda, MD, and Chemotherapeutic Agents Repository. Attn: Thelma Dizon, USA for performing the antitumor testing of the synthesized compounds.


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Copyright information

© The Pharmaceutical Society of Korea 2013

Authors and Affiliations

  1. 1.Department of Organic Chemistry, Faculty of PharmacyCairo UniversityCairoEgypt

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