title: Synthesis and inhibition of cancer cell proliferation of (1,3')-bis-tetrahydroisoquinolines and piperazine systems.
abstract: Some (1,3')-bis-tetrahydroisoquinolines were reported as scaffold intermediates for the synthesis of pentacyclic piperazine core alkaloids and their cytotoxicity against cancerous cell lines was evaluated. The NMR and X-ray structural assignments revealed an anti C3-C11 backbone stereochemistry of piperazine structures. Inhibition of cancer cell proliferation of (1,3')-bis-tetrahydroisoquinoline scaffolds and pentacyclic piperazine systems was assessed against three human cancer cell lines (K562 myelogenous leukemia, A549 lung carcinoma, MCF-7 breast adenocarcinoma) and both mouse tumor cell lines of blood (P388) and lymphocytic (L1210) leukemia with considerable activity against the latter. The cell cycle analysis was also studied by flow cytometry measurement on K562 cell line.
authors.affiliation: ICBMS, Institut de Chimie et Biochimie Moléculaires et Supramoléculaires, Laboratoire de Catalyse et Synthèse Organique, 43 boulevard du 11 novembre 1918, Villeurbanne, F-69622, France.
authors.forename: Sylvain
authors.initials: S
authors.lastname: Aubry
authors.forename: Stéphane
authors.initials: S
authors.lastname: Pellet-Rostaing
authors.forename: Jérémie
authors.initials: J
authors.lastname: Fournier Dit Chabert
authors.forename: Sylvie
authors.initials: S
authors.lastname: Ducki
authors.forename: Marc
authors.initials: M
authors.lastname: Lemaire
mesh_terms: D000970:Antineoplastic Agents / Q000737:chemistry / Q000494:pharmacology*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects*; D002626:Chemistry, Pharmaceutical / Q000379:methods*; D018360:Crystallography, X-Ray; D015195:Drug Design; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D020014:K562 Cells; D009682:Magnetic Resonance Spectroscopy; D008956:Models, Chemical; D008968:Molecular Conformation; D009369:Neoplasms / Q000188:drug therapy*; D010879:Piperazines / Q000138:chemical synthesis* / Q000494:pharmacology*; D044005:Tetrahydroisoquinolines / Q000138:chemical synthesis* / Q000494:pharmacology*
chemical_list: D000970:Antineoplastic Agents; D010879:Piperazines; D044005:Tetrahydroisoquinolines