期刊
CHEMICO-BIOLOGICAL INTERACTIONS
卷 180, 期 2, 页码 220-225出版社
ELSEVIER IRELAND LTD
DOI: 10.1016/j.cbi.2009.02.015
关键词
2H-azirine-2-azetidinone; Cytotoxicity; Apoptosis; HL-60 cells
资金
- Conselho Nacional de Desenvolvimento Cientifico e Tecnologico (CNPq)
- Financiadora de Estudos e Projetos (FINEP)
- Instituto Claude Bernard (InCB)
2-Azetidinones and 2H-azirines show antibacterial and cytotoxic activities, however the biological properties of molecules containing both 2H-azirine and 2-azetidinone functions in the same structure had never been evaluated before. In the present study, two 2H-azirine-2-azetidinones (1 and 2) and three 2H-azirines (3-5) were synthesized from 2-formyl-3-phenyl-2H-azirine-N-arylimines with diphenylketene. The compounds were assayed for antibacterial and cytotoxic activities. None of them showed antibacterial activity on the tested strains, but both 2H-azirine-2-azetidinones showed cytotoxicity against four tumor cell lines (HL-60, leukemia; HCT-8, colon cancer; MDA-MB435, melanoma; and SF-295, CNS).The IC50 values of 1 ranged from 1.1 to 10.5 mu M and from 3.8 to 26.6 mu M for 2. The mechanism of cell growth inhibition of 1 and 2 towards HL-60 cell line was also investigated. Membrane damage, cell viability, DNA synthesis inhibition and morphological changes were evaluated. The preliminary findings suggested that 1 and 2 induce apoptosis. (C) 2009 Elsevier Ireland Ltd. All rights reserved.
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