title: Synthesis and biological evaluation of novel bis-aziridinylnaphthoquinone derivatives.
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 carcinomna cell lines and weak cytotoxic activities against HL60 and skin fibroblast (SF). The bisaziridinylnaphthoquinone 1a was the most potent agent among those tested, with an LD50 value of 0.57 microM against the BC-M1 cell line. It exhibited the weakest activity against SF and HL60 with LD50 values of 5.67 and 20.1 microM, 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.
authors.affiliation: Department of Biochemistry, Taipei Medical University, Taipei, Taiwan, 250 Wu Hsing Street Taipei, Taiwan 110, ROC.
authors.forename: Sheng-Tung
authors.initials: ST
authors.lastname: Huang
authors.forename: Hsien-Shou
authors.initials: HS
authors.lastname: Kuo
authors.forename: Chun-Mao
authors.initials: CM
authors.lastname: Lin
authors.forename: Hsin-Da
authors.initials: HD
authors.lastname: Tsai
authors.forename: Yi-Chen
authors.initials: YC
authors.lastname: Peng
authors.forename: Chien-Tsu
authors.initials: CT
authors.lastname: Chen
authors.forename: Yuh-Ling
authors.initials: YL
authors.lastname: Lin
mesh_terms: D001388:Aziridines / Q000138:chemical synthesis* / Q000633:toxicity*; D004353:Drug Evaluation, Preclinical / Q000379:methods; D006801:Humans; D009285:Naphthoquinones / Q000138:chemical synthesis* / Q000633:toxicity*; D014407:Tumor Cells, Cultured / Q000187:drug effects / Q000502:physiology
chemical_list: D001388:Aziridines; D009285:Naphthoquinones