title: The novel anti-tumor agents of 4-triazol-1,8-naphthalimides: synthesis, cytotoxicity, DNA intercalation and photocleavage.
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.
authors.affiliation: State Key Laboratory of Fine Chemicals, Dalian University of Technology, PO Box 89, 158 Zhongshan Road, Dalian 116012, China. xiaolianlidlut@gmail.com
authors.forename: Xiaolian
authors.initials: X
authors.lastname: Li
authors.forename: Yanjie
authors.initials: Y
authors.lastname: Lin
authors.forename: Qianqian
authors.initials: Q
authors.lastname: Wang
authors.forename: Yukun
authors.initials: Y
authors.lastname: Yuan
authors.forename: Hua
authors.initials: H
authors.lastname: Zhang
authors.forename: Xuhong
authors.initials: X
authors.lastname: Qian
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D002417:Cattle; D045744:Cell Line, Tumor; D004247:DNA / Q000737:chemistry*; D053837:DNA Cleavage / Q000187:drug effects* / Q000528:radiation effects*; D019008:Drug Resistance, Neoplasm / Q000187:drug effects; D004583:Electrons; D006801:Humans; D007364:Intercalating Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D008027:Light; D053644:Naphthalimides / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D014783:Viscosity
chemical_list: D000970:Antineoplastic Agents; D007364:Intercalating Agents; D053644:Naphthalimides; D004247:DNA