Release Time:2019-03-09  Hits:

Indexed by: Journal Article

Date of Publication: 2011-04-01

Journal: EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Included Journals: PubMed、SCIE、Scopus

Volume: 46

Issue: 4

Page Number: 1274-1279

ISSN: 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.