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 Ca2+ and Mg2+.
Alberto Leoni, Alessandra Locatelli, Rita Morigi, Mirella Rambaldi, Concettina Cappadone, Giovanna Farruggia, et al. (2014). Substituted E-3-(3-indolylmethylene)1,3-dihydroindol-2-ones with antiproliferative activity. Study of the effects on HL-60 leukemia cells. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 79, 382-390 [10.1016/j.ejmech.2014.04.004].
Substituted E-3-(3-indolylmethylene)1,3-dihydroindol-2-ones with antiproliferative activity. Study of the effects on HL-60 leukemia cells
LEONI, ALBERTO;LOCATELLI, ALESSANDRA;MORIGI, RITA;RAMBALDI, MIRELLA;CAPPADONE, CONCETTINA;FARRUGGIA, GIOVANNA;IOTTI, STEFANO;MEROLLE, LUCIA;ZINI, MADDALENA;STEFANELLI, CLAUDIO
2014
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 Ca2+ and Mg2+.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
