A new series of 4-amino-6-methylthio-1H-pyrazolo[3,4-d]pyrimidines (2a-m) bearing the 2-chloro-2-phenylethyl chain at the N1 position, has been synthesized. The affinity of these compounds for A1 adenosine receptor (A1AR) was measured. The compounds showed poor affinity. A more interesting result was obtained by 2a, 2d, 2g, which demonstrated inhibitory activity on cell proliferation of the A-431 cell line stimulated by epithelial growth factor (EGF) and on EGF receptor tyrosine kinase (EGFR-TK) phosphorylation.
|Autori:||SCHENONE S.; BRUNO O.; BONDAVALLI F.; RANISE A.; MOSTI L.; MENOZZI G.; FOSSA P.; MANETTI F.; MORBIDELLI L.; TRINCAVELLI L.; MARTINI C.; LUCACCHINI A.|
|Titolo:||Synthesis of 1-(2-chloro-2-phenylethyl)-6-methylthio-1H-pyrazolo[3,4-d]pyrimidines 4-amino substituted and their biological evaluation|
|Anno del prodotto:||2004|
|Digital Object Identifier (DOI):||10.1016/j.ejmech.2003.11.007|
|Appare nelle tipologie:||1.1 Articolo in rivista|