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个人信息Personal Information
教授
博士生导师
硕士生导师
性别：男
毕业院校：日本冈山大学
学位：博士
所在单位：化工学院
学科：精细化工. 应用化学
办公地点：大连理工大学西部校区E209
联系方式：13591789942
电子邮箱：jncui@dlut.edu.cn
Novel acenaphthopyrazine derivatives as antitumor agents against MCF-7 cells: molecular synthesis, optical properties, and DNA-binding studies
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论文类型：期刊论文
发表时间：2012-02-01
发表刊物：MONATSHEFTE FUR CHEMIE
收录刊物：SCIE、Scopus
卷号：143
期号：2
页面范围：243-250
ISSN号：0026-9247
关键字：Acenaphthopyrazine derivatives; MCF-7 cells; Intercalator; DNA binding; Antitumor
摘要：A series of novel acenaphthopyrazine derivatives was synthesized from acenaphthylene-1,2-dione via three steps, including bromination, cyclization, and SNArH reaction. These new compounds exhibited potential antiproliferative activity against MCF-7 cells in vitro, and 3-[2-(dimethylamino)ethylamino]acenaphtho[1,2-b]pyrazine-8,9-dicarbonitrile exhibited the highest activity (IC (50) = 4.60 mu M). DNA-binding experiments suggested that these derivatives bind to DNA through intercalation with intrinsic binding constants K all above 10(5) M-1. Optical property studies indicated that these compounds have long emission wavelength (lambda (em) > 560 nm), high quantum yields in toluene (I broken vertical bar(f) = 0.59 for 3-(morpholin-4-yl)acenaphtho[1,2-b]pyrazine-8,9-dicarbonitrile), and large Stokes shift (Delta S > 130 nm).