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A novel photocleaver with long wavelength absorption - Highly efficient antitumor agent: 4-(2-diethylamino-ethylamino)-8-oxo-8H-acenaphtho-[ 1,2-b] pyrrole-9-carbonitrile

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Indexed by:期刊论文

Date of Publication:2005-07-01

Journal:CHEMICAL RESEARCH IN CHINESE UNIVERSITIES

Included Journals:SCIE、ISTIC、CSCD

Volume:21

Issue:4

Page Number:480-483

ISSN No.:1005-9040

Key Words:photocleaver; 8-oxo-8H-acenaphtho[1,2-b]pyrrole-9-carbonitrile; singlet oxygen; cytotoxicity

Abstract:The photocleavage abilities of a novel family of compounds, 8-oxo-8H-acenaphtho[1, 2-b] pyrrole-9-carbonitrile and its derivatives(compounds 1-5) were evaluated with MI3 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 mu mol/L, it could generate singlet oxygen to cleave circular DNA into linear DNA under the irradiation of long wavelength light(lambda > 400 nm). The antitumor ability of compound 1 was also evaluated in vitro, and its IC50 on HeLa cells was as low as 6.8 mu mol/L.

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