Synthesis, molecular structure, DNA-binding, cytotoxicity, apoptosis and antioxidant activity of compounds containing aryloxazole.

European Journal of Medicinal Chemistry(2014)

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摘要
Three novel aryloxazole compounds 1–3 were synthesized and characterized. The crystal structures of compounds 2 and 3 show that N atom locates at β-position and O atom at α-position in naphthalene cycle. The DNA binding constants for compounds 1–3 are 4.44 × 103, 5.31 × 103 and 2.64 × 103 M−1, respectively. The viscosity measurements indicate that these compounds intercalate between the DNA base pairs. Upon irradiation, compounds 1–3 can effectively cleave pBR322 DNA. The cytotoxicity of the compounds against BEL-7402, A549, MG-63 and SKBR-3 were assayed by MTT method. The apoptosis and cell cycle arrest were investigated towards A549 cells. The antioxidant activities of the compounds against hydroxyl radicals were also explored.
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关键词
Aryloxazole compounds,DNA binding,Cytotoxicity,Cell cycle arrest,Apoptosis
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