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Synthesis and Biological Evaluation of Novel bis-Aziridinylnaphthoquinone Derivatives

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Abstract:



A series of bis-aziridinylnaphthoquinone derivatives has been prepared. The cytotoxic activities and DNA alkylation abilities of these synthetic bis-aziridinylnaphthoquinone derivatives were investigated. They displayed significant cytotoxicity against human carcinoma cell lines and weak cytotoxic activities against HL60 and skin fibroblast (SF). The bis-aziridinylnaphthoquinone 1a was the most potent agent among those tested, with an LD50 value of 0.57 μM against the BC-M1 cell line. It exhibited the weakest activity against SF and HL60 with LD50 values of 5.67 and 20.1 μM, respectively, and it was able to alkylate DNA after chemical reduction in vitro. The analogues without aziridinyl moiety 2a and 3a lack DNA alkylation abilities.

Keywords: Key words: bis-Aziridinylnaphthoquinone derivative

Document Type: Research Article

DOI: http://dx.doi.org/10.3727/096504002108748231

Affiliations: Department of Biochemistry, Taipei Medical University, Taipei, Taiwan, 250 Wu Hsing Street Taipei, Taiwan 110, ROC

Publication date: January 1, 2002

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  • Formerly: Oncology Research Incorporating Anti-Cancer Drug Design
    Oncology Research Featuring Preclinical and Clincal Cancer Therapeutics publishes research of the highest quality that contributes to an understanding of cancer in areas of molecular biology, cell biology, biochemistry, biophysics, genetics, biology, endocrinology, and immunology, as well as studies on the mechanism of action of carcinogens and therapeutic agents, reports dealing with cancer prevention and epidemiology, and clinical trials delineating effective new therapeutic regimens.
cog/or/2002/00000013/00000004/or280
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