title: Synthesis and Biological Evaluation of Novel Aromatic Imide-Polyamine Conjugates.
abstract: Three types of conjugates in which aromatic imide scaffolds were coupled to diverse amine/polyamine motifs were synthesized, and their antitumor activities were evaluated in vitro and in vivo. Results showed that the conjugate11eof 1,8-naphthilimide with spermine had pronounced effects on inhibiting tumor cell proliferation and inducing tumor cell apoptosis via ROS-mediated mitochondrial pathway. The in vivo assays on three H22 tumor transplant models revealed that compound11eexerted potent ability in preventing lung cancer metastasis and extending lifespan. Furthermore, the efficacy of11ein inhibiting tumor growth and improving body weight index were better than that of positive control, amonafide. Our study demonstrates that compound11eis a valuable lead compound for further investigation.
authors.affiliation: Department of Pharmacology, Shenyang Pharmaceutical University, Shenyang 110016, China. songxu666@163.com.|Pharmaceutical College, Henan University, Kaifeng 475001, China. songxu666@163.com.
authors.forename: Ming
authors.initials: M
authors.lastname: Li
authors.affiliation: College of Chemistry and Chemical Engineering, Henan University, Kaifeng 475001, China. wangyuxia@henu.edu.cn.
authors.forename: Yuxia
authors.initials: Y
authors.lastname: Wang
authors.affiliation: Pharmaceutical College, Henan University, Kaifeng 475001, China. 18237878517@163.com.
authors.forename: Jianying
authors.initials: J
authors.lastname: Zhang
authors.affiliation: Pharmaceutical College, Henan University, Kaifeng 475001, China. xiesq@henu.edu.cn.
authors.forename: Songqiang
authors.initials: S
authors.lastname: Xie
authors.affiliation: Key Laboratory of Natural Medicine and Immuno-Engineering, Kaifeng 475001, China. wcjsxq@henu.edu.cn.
authors.forename: Chaojie
authors.initials: C
authors.lastname: Wang
authors.affiliation: Department of Pharmacology, Shenyang Pharmaceutical University, Shenyang 110016, China. yingliang_1016@163.com.
authors.forename: Yingliang
authors.initials: Y
authors.lastname: Wu
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000494:pharmacology* / Q000627:therapeutic use; D017209:Apoptosis / Q000187:drug effects; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D006801:Humans; D007094:Imides / Q000138:chemical synthesis / Q000494:pharmacology / Q000627:therapeutic use; D008114:Liver Neoplasms, Experimental / Q000188:drug therapy* / Q000473:pathology; D008175:Lung Neoplasms / Q000188:drug therapy* / Q000556:secondary; D008297:Male; D051379:Mice; D011073:Polyamines / Q000138:chemical synthesis / Q000494:pharmacology* / Q000627:therapeutic use; D023041:Xenograft Model Antitumor Assays
chemical_list: D000970:Antineoplastic Agents; D007094:Imides; D011073:Polyamines
keywords: amonafide; antitumor; naphthalimide; polyamine; synthesis