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Parallel synthesis and cytotoxicity evaluation of a polyamine-quinone conjugates library.

Authors :
Bolognesi ML
Calonghi N
Mangano C
Masotti L
Melchiorre C
Source :
Journal of medicinal chemistry [J Med Chem] 2008 Sep 11; Vol. 51 (17), pp. 5463-7. Date of Electronic Publication: 2008 Aug 13.
Publication Year :
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.

Details

Language :
English
ISSN :
1520-4804
Volume :
51
Issue :
17
Database :
MEDLINE
Journal :
Journal of medicinal chemistry
Publication Type :
Academic Journal
Accession number :
18698755
Full Text :
https://doi.org/10.1021/jm800637b