Novel N-oxide of naphthalimides as prodrug leads against hypoxic solid tumor: synthesis and biological evaluation.
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.
Yin
Hong
H
Shanghai Key Lab of Chemical Biology, School of Pharmacy, East China University of Science and Technology, Shanghai 200237, China.
Xu
Yufang
Y
Qian
Xuhong
X
Li
Yuanli
Y
Liu
Jianwen
J
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
D000970:Antineoplastic Agents; D053644:Naphthalimides; D010087:Oxides; D011355:Prodrugs