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

作     者：ZHANGZhi-chao LüZhe QIANXu-hong SHENGHui 

作者机构：StateKeyLaboratoryofFineChemicalsDalianUniversityofTechnologyDalian116012P.R.China TheFirstClinicalHospitalJilinUniversityChangchun130021P.R.China 

出 版 物：《Chemical Research in Chinese Universities》 (高等学校化学研究（英文版）)

年 卷 期：2005年第21卷第4期

页      面：480-483页

核心收录：

学科分类：1007[医学-药学(可授医学、理学学位)] 081704[工学-应用化学] 07[理学] 08[工学] 0817[工学-化学工程与技术] 070303[理学-有机化学] 0703[理学-化学] 10[医学] 

基　　金：SupportedbytheNationalKeyProjectforBasicResearch(No.2003CB114400)andtheNationalNaturalScienceFoundationofChina(No.30400106) 

主　　题：Photocleaver 8-Oxo-8H-acenaphtho[1,2-b]pyrrole-9-carbonitrile Singlet oxygen Cytotoxicity 

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(λ400 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.