title: Synthesis and biological evaluation of new securinine analogues as potential anticancer agents.
abstract: A series of new securinine analogues was prepared by Heck reaction from readily accessible securinine and commercially available iodoarenes. The in vitro cytotoxicity of the prepared compounds was assayed against a panel of four cancer cell lines: A375, A549, HCT-116 and HL-60 showing promising growth inhibition with excellent IC50 values in the nanomolar range. The plasmatic stability of the most potent analogue was also investigated demonstrating that they might serve as valuable leads for the development of anticancer drugs.
authors.affiliation: PSL Research University, Chimie ParisTech - CNRS, Institut de Recherche de Chimie Paris, Paris, 75005, France.
authors.forename: Marc
authors.initials: M
authors.lastname: Perez
authors.affiliation: PSL Research University, Chimie ParisTech - CNRS, Institut de Recherche de Chimie Paris, Paris, 75005, France.
authors.forename: Tahar
authors.initials: T
authors.lastname: Ayad
authors.affiliation: Institut de Recherche Pierre Fabre, Gaillac, 81600, France.
authors.forename: Philippe
authors.initials: P
authors.lastname: Maillos
authors.affiliation: Unité de Service et de Recherche CNRS-Pierre Fabre n°3388 ETaC CRDPF, Toulouse, 31035, France.
authors.forename: Valérie
authors.initials: V
authors.lastname: Poughon
authors.affiliation: Unité de Service et de Recherche CNRS-Pierre Fabre n°3388 ETaC CRDPF, Toulouse, 31035, France. Electronic address: jacques.fahy@pierre-fabre.com.
authors.forename: Jacques
authors.initials: J
authors.lastname: Fahy
authors.affiliation: PSL Research University, Chimie ParisTech - CNRS, Institut de Recherche de Chimie Paris, Paris, 75005, France. Electronic address: virginie.vidal@chimie-paristech.fr.
authors.forename: Virginie
authors.initials: V
authors.lastname: Ratovelomanana-Vidal
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D017209:Apoptosis / Q000187:drug effects; D001381:Azepines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D004354:Drug Screening Assays, Antitumor; D019665:Euphorbiaceae / Q000737:chemistry; D006572:Heterocyclic Compounds, Bridged-Ring / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D006801:Humans; D007783:Lactones / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D009369:Neoplasms / Q000188:drug therapy; D010880:Piperidines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*
chemical_list: D000970:Antineoplastic Agents; D001381:Azepines; D006572:Heterocyclic Compounds, Bridged-Ring; D007783:Lactones; D010880:Piperidines; C000785:securinine
keywords: Anticancer activity; Heck reaction; Plasmatic stability; Securinine; Semisynthesis