A Novel Photocleaver with Long Wavelength Absorption-Highly Efficient Antitumor Agent: 4-(2-Diethylamino-ethylamino)-8-oxo-8H-acenaphtho-1,2-bpyrrole-9-carbonitrile

摘要

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.