Parallel synthesis and cytotoxicity evaluation of a polyamine− quinone conjugates library

ML Bolognesi, N Calonghi, C Mangano…

Index: Bolognesi, Maria Laura; Calonghi, Natalia; Mangano, Chiara; Masotti, Lanfranco; Melchiorre, Carlo Journal of Medicinal Chemistry, 2008 , vol. 51, # 17 p. 5463 - 5467

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Citation Number: 28

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 μM range. Entry 1b caused apoptotic EGFR-mediated intracellular signaling. Thus, polyamino− quinones emerged as readily accessible and ...