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Indexed by:期刊论文

Date of Publication:2011-04-01

Journal:EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Included Journals:Scopus、SCIE、PubMed

Volume:46

Issue:4

Page Number:1274-1279

ISSN No.:0223-5234

Key Words:Triazole; Intercalation; Anticancer; Naphthalimides

Abstract:A novel series of 4-(4-phenyl-[1,2,3]-triazol-1-yl)-1,8-naphthalimide derivatives had been synthesized easily by employing "click reaction". For anti-tumor activity in vitro, all the compounds were found to be more toxic against MCF-7 than Hela and 7721 cells. 4a, 4b and 4e Showed improved cytotoxic activity against MCF-7 cells over Amonafide, in particular compound 4a, with an IC(50) could amount to 10(-7) M. The UV-vis spectra and Circular Dichroism titration indicated that the compounds behaved as effective DNA-intercalating agents. The investigation of their photo-damaging ability illuminated that these compounds could damage DNA effectively into form II and even form III. (c) 2011 Elsevier Masson SAS. All rights reserved.