A library of 24 derivatives designed by combining two natural products-derived fragments was prepared and tested to determine their anticancer potential in HT29 colon cancer cells. All library members inhibit cell proliferation as measured by MTT mitochondrial functional assay, with IC50 values in the 1-100 microM range. Entry 1b caused apoptotic EGFR-mediated intracellular signaling. Thus, polyamino-quinones emerged as readily accessible and easily diversified scaffolds for anticancer lead discovery.
Bolognesi ML, Calonghi N, Mangano C, Masotti L, Melchiorre C. (2008). Parallel synthesis and cytotoxicity evaluation of a polyamine-quinone conjugates library. JOURNAL OF MEDICINAL CHEMISTRY, 51, 5463-5467 [10.1021/jm800637b].
Parallel synthesis and cytotoxicity evaluation of a polyamine-quinone conjugates library
BOLOGNESI, MARIA LAURA;CALONGHI, NATALIA;MANGANO, CHIARA;MASOTTI, LANFRANCO;MELCHIORRE, CARLO
2008
Abstract
A library of 24 derivatives designed by combining two natural products-derived fragments was prepared and tested to determine their anticancer potential in HT29 colon cancer cells. All library members inhibit cell proliferation as measured by MTT mitochondrial functional assay, with IC50 values in the 1-100 microM range. Entry 1b caused apoptotic EGFR-mediated intracellular signaling. Thus, polyamino-quinones emerged as readily accessible and easily diversified scaffolds for anticancer lead discovery.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
