title: Novel N-oxide of naphthalimides as prodrug leads against hypoxic solid tumor: synthesis and biological evaluation.
abstract: Novel tertiary amine N-oxides of naphthalimides were designed and synthesized as potential anticancer agents against hypoxic solid tumors. Although their ctDNA-binding affinities and cytotoxic activities against usual tumor cell lines were lower than those of corresponding amines, the N-oxides A1 and A4 showed hypoxia preference activities against A375 cells in vitro and might be used as interesting candidates of prodrug leads in hypoxic tumor cells.
authors.affiliation: Shanghai Key Lab of Chemical Biology, School of Pharmacy, East China University of Science and Technology, Shanghai 200237, China.
authors.forename: Hong
authors.initials: H
authors.lastname: Yin
authors.forename: Yufang
authors.initials: Y
authors.lastname: Xu
authors.forename: Xuhong
authors.initials: X
authors.lastname: Qian
authors.forename: Yuanli
authors.initials: Y
authors.lastname: Li
authors.forename: Jianwen
authors.initials: J
authors.lastname: Liu
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D015687:Cell Hypoxia / Q000187:drug effects; D045744:Cell Line, Tumor; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D053644:Naphthalimides / Q000138:chemical synthesis* / Q000494:pharmacology; D009369:Neoplasms / Q000188:drug therapy / Q000473:pathology; D010087:Oxides / Q000138:chemical synthesis* / Q000494:pharmacology; D011355:Prodrugs / Q000138:chemical synthesis*; D013329:Structure-Activity Relationship
chemical_list: D000970:Antineoplastic Agents; D053644:Naphthalimides; D010087:Oxides; D011355:Prodrugs