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.
2008
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].
Bolognesi ML; Calonghi N; Mangano C; Masotti L; Melchiorre C.
File in questo prodotto:
Eventuali allegati, non sono esposti

I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.

Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11585/68231
 Attenzione

Attenzione! I dati visualizzati non sono stati sottoposti a validazione da parte dell'ateneo

Citazioni
  • ???jsp.display-item.citation.pmc??? 4
  • Scopus 37
  • ???jsp.display-item.citation.isi??? 34
social impact