Cytotoxic activities of substituted 3-(3,4,5-trimethoxybenzylidene)-1,3-dihydroindol-2-ones and studies on their mechanisms of action

  • Eur J Med Chem. 2013 Jun:64:603-12. doi: 10.1016/j.ejmech.2013.03.033.
Aldo Andreani  1 ,  Massimiliano Granaiola ,  Alessandra Locatelli ,  Rita Morigi ,  Mirella Rambaldi ,  Lucilla Varoli ,  Francesco Vieceli Dalla Sega ,  Cecilia Prata ,  Tam L Nguyen ,  Ruoli Bai ,  Ernest Hamel
Affiliations
  • 1. Dipartimento di Farmacia e Biotecnologie FaBiT, Università di Bologna, Via Belmeloro 6, 40126 Bologna, Italy.
PMID: 23685944 DOI: 10.1016/j.ejmech.2013.03.033
Abstract

The synthesis of new trimethoxybenzylidene-indolinones 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.