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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.

Schenone, S., Bruno, O., Bondavalli, F., Ranise, A., Mosti, L., Menozzi, G., et al. (2004). Synthesis of 1-(2-chloro-2-phenylethyl)-6-methylthio-1H-pyrazolo[3,4-d]pyrimidines 4-Amino Substituted and Their Biological Evaluation. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 39(2), 153-160 [10.1016/j.ejmech.2003.11.007].

Synthesis of 1-(2-chloro-2-phenylethyl)-6-methylthio-1H-pyrazolo[3,4-d]pyrimidines 4-Amino Substituted and Their Biological Evaluation.

MANETTI, FABRIZIO;MORBIDELLI, LUCIA;
2004-01-01

Abstract

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.
2004
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Schenone, S., Bruno, O., Bondavalli, F., Ranise, A., Mosti, L., Menozzi, G., et al. (2004). Synthesis of 1-(2-chloro-2-phenylethyl)-6-methylthio-1H-pyrazolo[3,4-d]pyrimidines 4-Amino Substituted and Their Biological Evaluation. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 39(2), 153-160 [10.1016/j.ejmech.2003.11.007].
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11365/21442
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