Substituted E-3-(3-indolylmethylene)1,3-dihydroindol-2-ones with antiproliferative activity. Study of the effects on HL-60 leukemia cells

• The synthesis of new substituted E-3-(3-indolylmethylene)1,3-dihydroindol-2-ones is reported.
• Growth-inhibiting activity of the compounds was investigated.
• Additional studies on cell cycle progression using HL-60 leukemia cells have been made.
• Intracellular content of Mg2+ and Ca2+ was examined.

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+.

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