A Novel Photocleaver with Long Wavelength Absorption-Highly Efficient Antitumor Agent: 4-(2-Diethyla

来源 :Chemical Research in Chinese Universities | 被引量 : 0次 | 上传用户:xulingxuan
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The photocleavage abilities of a novel family of compounds, 8-oxo-8%H%-acenaphtho pyrrole-9-carbonitrile and its derivatives(compounds 1—5) were evaluated with M13 mp18 single strand circular DNA. Only compound 1 with a diethylamine group could bind to DNA %via% electrostatic attraction and intercalation. At a concentration of 50 μmol/L, it could generate singlet oxygen to cleave circular DNA into linear DNA under the irradiation of long wavelength light(λ>400 nm). The antitumor {ability} of compound 1 was also evaluated in vitro, and its IC_ 50 on HeLa cells was as low as 6.8 μmol/L. The photocleavage abilities of a novel family of compounds, 8-oxo-8% H% -acenaphtho pyrrole-9-carbonitrile and its derivatives (compounds 1-5) were evaluated as M13 mp18 single strand circular DNA. group could bind to DNA% via% electrostatic attraction and intercalation. At a concentration of 50 μmol / L, it could generate singlet oxygen to cleave circular DNA into linear DNA under the irradiation of long wavelength light (λ> 400 nm). The antitumor {ability} of compound 1 was also evaluated in vitro, and its IC 50 on HeLa cells was as low as 6.8 μmol / L.
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