Leoni Alberto, Locatelli Alessandra, Morigi Rita, Rambaldi Mirella, Cappadone Concettina, Farruggia Giovanna, Iotti Stefano, Merolle Lucia, Zini Maddalena, Stefanelli Claudio
Department of Pharmacy and Biotechnology, University of Bologna, Via Belmeloro 6, 40126 Bologna, Italy.
Department of Pharmacy and Biotechnology, University of Bologna, Via Belmeloro 6, 40126 Bologna, Italy.
Eur J Med Chem. 2014 May 22;79:382-90. doi: 10.1016/j.ejmech.2014.04.004. Epub 2014 Apr 3.
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+).
报道了新型取代的E-3-(3-吲哚基亚甲基)-1,3-二氢吲哚-2-酮的合成。根据美国国立癌症研究所（NCI）（位于马里兰州贝塞斯达）提供的方案评估了其抗增殖活性。对活性最高的化合物10在HL-60白血病细胞中的作用进行了进一步研究。所得结果表明，它会导致细胞周期进程受阻，使细胞停滞在G2/M期，同时伴随着细胞凋亡的激活，伴有氧化应激增加和二价阳离子稳态失调，细胞内游离Ca(2+)和Mg(2+)浓度显著升高。
