Substituted E-3-(3-indolylmethylene)1,3-dihydroindol-2-ones with antiproliferative activity. Study of the effects on HL-60 leukemia cells.
Eur J Med Chem, 2014/5/22;79:382-90.
Leoni A[1], Locatelli A[1], Morigi R[1], Rambaldi M[2], Cappadone C[1], Farruggia G[1], Iotti S[1], Merolle L[1], Zini M[3], Stefanelli C[4]
Affiliations
PMID: 24747749
Impact factor: 7.088
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+).
Keywords: Antiproliferative activity; Apoptosis; Divalent cations; Indolyl-indol-2-one; Knoevenagel reaction
MeSH terms
Antineoplastic Agents; Cell Cycle; Cell Death; Cell Proliferation; Dose-Response Relationship, Drug; Drug Screening Assays, Antitumor; HL-60 Cells; Humans; Indoles; Molecular Structure; Oxidative Stress; Structure-Activity Relationship; Tumor Cells, Cultured
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