A new series of 4-amino-6-methylthio-1H-pyrazolo[3,4-d]pyrimidines (I, R = cyclopropylamino, NHBu, morpholino, etc.), bearing the 2-chloro-2-phenylethyl chain at the N1 position, has been synthesized. The affinity of these compds. for A1 adenosine receptor (A1AR) was measured. The compds. showed poor affinity. A more interesting result was obtained by three examples of I 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
Synthesis of 1-(2-chloro-2-phenylethyl)-6-methylthio-1-H-pyrazolo[3,4-d]pyrimidines 4-amino substituted and their biological evaluation
SCHENONE S.;BRUNO O.;BONDAVALLI F.;RANISE A.;MOSTI L.;MENOZZI G.;FOSSA P.;
2004-01-01
Abstract
A new series of 4-amino-6-methylthio-1H-pyrazolo[3,4-d]pyrimidines (I, R = cyclopropylamino, NHBu, morpholino, etc.), bearing the 2-chloro-2-phenylethyl chain at the N1 position, has been synthesized. The affinity of these compds. for A1 adenosine receptor (A1AR) was measured. The compds. showed poor affinity. A more interesting result was obtained by three examples of I 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
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