The synthesis of new trimethoxybenzylideneeindolinones is reported. Their cytotoxic activity was evaluated according to Developmental Therapeutics Program, National Cancer Institute, Bethesda, MD, drug screen protocols. The study of the mechanism of action suggests that inhibition of Nox4 in B1647 cells (acute myeloid leukemia) could contribute to the antiproliferative effect of some compounds. Moreover, inhibition of tubulin assembly was observed for the most cytotoxic compound, and the structural basis for this activity was delineated by binding models.
A. Andreani, M. Granaiola, A. Locatelli, R. Morigi, M. Rambaldi, L. Varoli, et al. (2013). Cytotoxic activities of substituted 3-(3,4,5-trimethoxybenzylidene)- 1,3-dihydroindol-2-ones and studies on their mechanisms of action. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 64, 603-612 [10.1016/j.ejmech.2013.03.03].
Cytotoxic activities of substituted 3-(3,4,5-trimethoxybenzylidene)- 1,3-dihydroindol-2-ones and studies on their mechanisms of action
LOCATELLI, ALESSANDRA;MORIGI, RITA;RAMBALDI, MIRELLA;VIECELI DALLA SEGA, FRANCESCO;PRATA, CECILIA;
2013
Abstract
The synthesis of new trimethoxybenzylideneeindolinones is reported. Their cytotoxic activity was evaluated according to Developmental Therapeutics Program, National Cancer Institute, Bethesda, MD, drug screen protocols. The study of the mechanism of action suggests that inhibition of Nox4 in B1647 cells (acute myeloid leukemia) could contribute to the antiproliferative effect of some compounds. Moreover, inhibition of tubulin assembly was observed for the most cytotoxic compound, and the structural basis for this activity was delineated by binding models.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
