Parallel synthesis and cytotoxicity evaluation of a polyamine-quinone conjugates library |
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Authors: | Bolognesi Maria Laura Calonghi Natalia Mangano Chiara Masotti Lanfranco Melchiorre Carlo |
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Institution: | Department of Pharmaceutical Sciences, Alma Mater Studiorum, University of Bologna, Via Belmeloro 6, 40126 Bologna, Italy. marialaura.bolognesi@unibo.it |
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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. |
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