title: Substituted E-3-(3-indolylmethylene)1,3-dihydroindol-2-ones with antiproliferative activity. Study of the effects on HL-60 leukemia cells.
abstract: The synthesis of new substituted E-3-(3-indolylmethylene)1,3-dihydroindol-2-ones is reported. The antiproliferative activity was evaluated according to protocols available at the National Cancer Institute (NCI), Bethesda, MD. The action of the most active compound 10 was further investigated in HL-60 leukemia cells. Results obtained show that it causes a block in cell cycle progression, with cell arrest in the G2/M phase, associated with activation of apoptosis accompanied with increased oxidative stress and deregulation of the homeostasis of divalent cations, with significant increase in the cellular concentrations of free Ca(2+) and Mg(2+).
authors.affiliation: Department of Pharmacy and Biotechnology, University of Bologna, Via Belmeloro 6, 40126 Bologna, Italy.
authors.forename: Alberto
authors.initials: A
authors.lastname: Leoni
authors.affiliation: Department of Pharmacy and Biotechnology, University of Bologna, Via Belmeloro 6, 40126 Bologna, Italy.
authors.forename: Alessandra
authors.initials: A
authors.lastname: Locatelli
authors.affiliation: Department of Pharmacy and Biotechnology, University of Bologna, Via Belmeloro 6, 40126 Bologna, Italy.
authors.forename: Rita
authors.initials: R
authors.lastname: Morigi
authors.affiliation: Department of Pharmacy and Biotechnology, University of Bologna, Via Belmeloro 6, 40126 Bologna, Italy. Electronic address: mirella.rambaldi@unibo.it.
authors.forename: Mirella
authors.initials: M
authors.lastname: Rambaldi
authors.affiliation: Department of Pharmacy and Biotechnology, University of Bologna, Via Belmeloro 6, 40126 Bologna, Italy.
authors.forename: Concettina
authors.initials: C
authors.lastname: Cappadone
authors.affiliation: Department of Pharmacy and Biotechnology, University of Bologna, Via Belmeloro 6, 40126 Bologna, Italy.
authors.forename: Giovanna
authors.initials: G
authors.lastname: Farruggia
authors.affiliation: Department of Pharmacy and Biotechnology, University of Bologna, Via Belmeloro 6, 40126 Bologna, Italy.
authors.forename: Stefano
authors.initials: S
authors.lastname: Iotti
authors.affiliation: Department of Pharmacy and Biotechnology, University of Bologna, Via Belmeloro 6, 40126 Bologna, Italy.
authors.forename: Lucia
authors.initials: L
authors.lastname: Merolle
authors.affiliation: Department of Biomedical and Neuromotor Sciences, University of Bologna, 40126 Bologna, Italy.
authors.forename: Maddalena
authors.initials: M
authors.lastname: Zini
authors.affiliation: Department for Life Quality Studies, University of Bologna, Rimini Campus, 47921 Rimini, Italy.
authors.forename: Claudio
authors.initials: C
authors.lastname: Stefanelli
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D002453:Cell Cycle / Q000187:drug effects; D016923:Cell Death / Q000187:drug effects; D049109:Cell Proliferation / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D004354:Drug Screening Assays, Antitumor; D018922:HL-60 Cells; D006801:Humans; D007211:Indoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D015394:Molecular Structure; D018384:Oxidative Stress / Q000187:drug effects; D013329:Structure-Activity Relationship; D014407:Tumor Cells, Cultured
chemical_list: D000970:Antineoplastic Agents; D007211:Indoles
keywords: Antiproliferative activity; Apoptosis; Divalent cations; Indolyl-indol-2-one; Knoevenagel reaction