title: Novel naphthalimide-benzoic acid conjugates as potential apoptosis-inducing agents: design, synthesis, and biological activity.
abstract: A series of novel naphthalimide derivatives with 4-[4-(3,3-diphenylallyl)piperazin-1-yl]benzoic acid as side chain were designed and synthesized. Their antitumor activities were evaluated against a variety of cancer cell lines in vitro. Preliminary results showed that most of the derivatives had cytotoxic activity comparable with that of amonafide, with IC₅₀ values of 10⁻⁶-10⁻⁵ M. Interestingly, compound 12e had the unique antitumor activity against MCF-7 among the cancer cell lines tested. More importantly, flow cytometric analysis indicated that compared with amonafide, the target compounds could effectively induce G₂/M arrest and progress to apoptosis in HL-60 cells after double staining with annexin V-FITC and propidium iodide. The present work provided a novel class of naphthalimide-based derivatives with potential apoptosis-inducing and improved antitumor activity for further optimization.
authors.affiliation: School of Chemistry and Environmental Engineering, Yangtze University, Jingzhou 434023, China. abwu@yangtzeu.edu.cn
authors.forename: Aibin
authors.initials: A
authors.lastname: Wu
authors.forename: Ping
authors.initials: P
authors.lastname: Mei
authors.forename: Yufang
authors.initials: Y
authors.lastname: Xu
authors.forename: Xuhong
authors.initials: X
authors.lastname: Qian
mesh_terms: D000225:Adenine; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000633:toxicity*; D017209:Apoptosis; D019817:Benzoic Acid / Q000138:chemical synthesis* / Q000737:chemistry / Q000633:toxicity*; D045744:Cell Line, Tumor; D004354:Drug Screening Assays, Antitumor; D018922:HL-60 Cells; D006801:Humans; D053644:Naphthalimides / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology / Q000633:toxicity*; D063065:Organophosphonates; D013329:Structure-Activity Relationship
chemical_list: D000970:Antineoplastic Agents; D053644:Naphthalimides; D063065:Organophosphonates; C037020:amonafide; D019817:Benzoic Acid; D000225:Adenine