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Novel efficient anticancer agents and DNA-intercalators of 1,2,3-triazol-1,8-naphthalimides: design, synthesis, and biological activity

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Indexed by: Journal Article

Date of Publication: 2011-03-25

Journal: TETRAHEDRON

Included Journals: SCIE、Scopus

Volume: 67

Issue: 12

Page Number: 2299-2304

ISSN: 0040-4020

Key Words: Triazole; Intercalation; Anticancer; Naphthalimides

Abstract: Two novel series of 3-1,2,3-triazol-1,8-naphthalimides 5a-e, 7a-e were synthesized easily by employing 'click reaction'. Their bioactivities were evaluated. Compounds 5a-e were found to be more toxic against MCF-7 cells while 7a-e were more potent against 7721 cells, in particular 7a, the IC50 value of which against cell lines of MCF-7 and 7721 was 0.348 mu M and 0.258 mu M, respectively. Due to the phenyl group linked to 1,2,3-triazole, compound 5a not only showed higher DNA affinity but also more efficient DNA damaging ability than compound 7a. (C) 2011 Elsevier Ltd. All rights reserved.

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