title: Synthesis and cytotoxic evaluation of novel symmetrical taspine derivatives as anticancer agents.
abstract: It has been demonstrated that taspine derivatives act as anticancer agents, thus we designed and synthesized a novel class of symmetrical biphenyl derivatives. We evaluated the cytotoxicity and antitumor activity of biphenyls against five human tumor and normal cell lines. The results indicated that the majority of the compounds exhibited anticancer activity equivalent to or greater than the positive control. Compounds (11) and (12) demonstrated the most potent cytotoxic activity with IC₅₀ values between 19.41 µM and 29.27 µM. The potent antiproliferative capabilities of these compounds against ECV304 human transformed endothelial cells indicated that these biphenyls could potentially serve as antiangiogenic agents. We also reviewed the relationship between structure and activity based on the experimental results. Our findings provide a good starting point for further development of symmetrical biphenyl derivatives as potential novel anticancer agents.
authors.affiliation: College of Medicine, Xi'an Jiaotong University, No. 76 Yanta West Road, Xi'an, Shaanxi, Province 710061, P.R. China.
authors.forename: Jie
authors.initials: J
authors.lastname: Zhang
authors.forename: Yanmin
authors.initials: Y
authors.lastname: Zhang
authors.forename: Xiaoyan
authors.initials: X
authors.lastname: Pan
authors.forename: Sicen
authors.initials: S
authors.lastname: Wang
authors.forename: Langchon
authors.initials: L
authors.lastname: He
mesh_terms: D000470:Alkaloids / Q000737:chemistry / Q000494:pharmacology; D020533:Angiogenesis Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry* / Q000493:pharmacokinetics / Q000494:pharmacology; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D001713:Biphenyl Compounds / Q000138:chemical synthesis* / Q000737:chemistry* / Q000493:pharmacokinetics / Q000494:pharmacology*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects*; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D006846:Hydrocarbons, Halogenated / Q000138:chemical synthesis* / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D020128:Inhibitory Concentration 50; D058990:Molecular Targeted Therapy; D009369:Neoplasms / Q000188:drug therapy / Q000473:pathology; D013329:Structure-Activity Relationship
chemical_list: C568541:6,6'-bis(2-((3-chloro-4-fluorophenyl)amino)-2-oxoethoxy)-5,5'-dimethoxy- N,N'-dimethylbiphenyl-2,2'-dicarboxamide; D000470:Alkaloids; D020533:Angiogenesis Inhibitors; D000970:Antineoplastic Agents; D001713:Biphenyl Compounds; D006846:Hydrocarbons, Halogenated; C018394:taspine