title: Novel naphthalimide-amino acid conjugates with flexible leucine moiety as side chain: design, synthesis and potential antitumor activity.
abstract: A series of novel naphthalimide derivatives with flexible leucine side chains were designed and synthesized. Their antitumor activities were evaluated against HeLa, A549, P388, HL-60, MCF-7, HCT-8 and A375 cancer cell lines in vitro. The preliminary results showed that most of the derivatives had moderate antitumor activities with the IC(50) values of 10(-6)-10(-5) M. More importantly, compounds 8a-c exhibited exclusive antitumor activities against MCF-7 cell line. The interaction between compound 8b and BSA was also investigated. DNA binding experiments showed that these derivatives behaved as DNA intercalating agents. This work provided a novel class of naphthalimide-based lead compounds with exclusive antitumor activities against MCF-7 cell line for further optimization.
authors.affiliation: Shanghai Key Laboratory of Chemical Biology, School of Pharmacy, East China University of Science and Technology, Shanghai 200237, China.
authors.forename: Aibin
authors.initials: A
authors.lastname: Wu
authors.forename: Yufang
authors.initials: Y
authors.lastname: Xu
authors.forename: Xuhong
authors.initials: X
authors.lastname: Qian
mesh_terms: D000596:Amino Acids / Q000737:chemistry* / Q000494:pharmacology; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D001943:Breast Neoplasms / Q000188:drug therapy; D045744:Cell Line, Tumor; D015195:Drug Design; D005260:Female; D006801:Humans; D020128:Inhibitory Concentration 50; D007364:Intercalating Agents; D007930:Leucine; D053644:Naphthalimides / Q000737:chemistry* / Q000494:pharmacology; D013329:Structure-Activity Relationship
chemical_list: D000596:Amino Acids; D000970:Antineoplastic Agents; D007364:Intercalating Agents; D053644:Naphthalimides; D007930:Leucine