Novel naphthalimide derivatives as potential apoptosis-inducing agents: design, synthesis and biological evaluation.
A series of novel naphthalimide derivatives with flexible alkyl/aryl moieties 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 comparable antitumor activities over Amonafide with the IC(50) values of 10(-6) to 10(-5)M. More importantly, flow cytometric analysis indicated that the derivatives could effectively induce G(2)/M arrest and progress to apoptosis in HL-60 cell line after double staining with annexin V-FITC and propidium iodide. The present work provided a novel class of naphthalimide-based derivatives with potent apoptosis-inducing and antitumor activities for further optimization.
Wu
Aibin
A
Shanghai Key Laboratory of Chemical Biology, School of Pharmacy, East China University of Science and Technology, Shanghai 200237, China.
Xu
Yufang
Y
Qian
Xuhong
X
Wang
Jin
J
Liu
Jianwen
J
D000970:Antineoplastic Agents / Q000737:chemistry* / Q000494:pharmacology*; D017209:Apoptosis / Q000187:drug effects*; D004354:Drug Screening Assays, Antitumor; D016195:G2 Phase / Q000187:drug effects; D018922:HL-60 Cells; D006801:Humans; D053644:Naphthalimides / Q000737:chemistry* / Q000494:pharmacology*
D000970:Antineoplastic Agents; D053644:Naphthalimides