title: Cytotoxic activity of new racemic and optically active N-phosphonoalkyl bicyclic β-amino acids against human malignant cell lines.
abstract: The cytotoxic effects of novel racemic and optically active constrained N-phosphonoalkyl bicyclic β-amino acids were tested against a panel of human tumor cell lines. All of the compounds investigated exhibited different concentration-dependent antiproliferative effects against the HT-29, MDA-MB-231, HepG2 and HeLa cell lines after 24 h treatment. The most sensitive cells were the HeLa cells at various concentrations of the four compounds tested. The aminophosphonate 3 exerted the most pronounced antiproliferative effect against the HeLa cells (inhibition of the cell vitality up to 70% at 0.5 mg/ml) and was not toxic to the normal Lep3 cells at lower concentration. Furthermore, the N-phosphonophenyl derivatives 1 and 2 displayed antiproliferative effect against mainly the MDA-MB-231 tumour cells at higher concentration.
authors.affiliation: Department of Organic Chemistry, University of Chemical Technology and Metallurgy, 1756, Sofia, Bulgaria. pepi_37@abv.bg
authors.forename: Petar T
authors.initials: PT
authors.lastname: Todorov
authors.forename: Diana W
authors.initials: DW
authors.lastname: Wesselinova
authors.forename: Nikola D
authors.initials: ND
authors.lastname: Pavlov
authors.forename: Jean
authors.initials: J
authors.lastname: Martinez
authors.forename: Monique
authors.initials: M
authors.lastname: Calmes
authors.forename: Emilia D
authors.initials: ED
authors.lastname: Naydenova
mesh_terms: D000596:Amino Acids / Q000138:chemical synthesis / Q000494:pharmacology*; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000494:pharmacology*; D001643:Bridged Bicyclo Compounds / Q000138:chemical synthesis / Q000494:pharmacology*; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D020128:Inhibitory Concentration 50; D063065:Organophosphonates / Q000138:chemical synthesis / Q000494:pharmacology*; D013237:Stereoisomerism
chemical_list: D000596:Amino Acids; D000970:Antineoplastic Agents; D001643:Bridged Bicyclo Compounds; D063065:Organophosphonates