Novel naphthalimide derivatives as potential apoptosis-inducing agents: Design, synthesis and biological evaluation

作者：Wu Aibin; Xu Yufang; Qian Xuhong^*; Wang Jin; Liu Jianwen

来源：European Journal of Medicinal Chemistry, 2009, 44(11): 4674-4680.

DOI：10.1016/j.ejmech.2009.07.011

• Naphthalimide
• Antitumor
• Cytotoxicity
• G(2)/M arrest
• Apoptosis

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 IC50 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.

• 出版日期2009-11
• 单位华东理工大学