http://www.cnr.it/ontology/cnr/individuo/prodotto/ID27529
Synthesis, biological evaluation and docking studies of 4-amino substituted 1H-pyrazolo[3,4-d]pyrimidines. (Articolo in rivista)
- Type
- Label
- Synthesis, biological evaluation and docking studies of 4-amino substituted 1H-pyrazolo[3,4-d]pyrimidines. (Articolo in rivista) (literal)
- Anno
- 2008-01-01T00:00:00+01:00 (literal)
- Alternative label
Schenone S, Brullo C, Bruno O, Bondavalli F, Mosti L, Maga G, Crespan E, Carraro F, Manetti F, Tintori C, Botta M. (2008)
Synthesis, biological evaluation and docking studies of 4-amino substituted 1H-pyrazolo[3,4-d]pyrimidines.
in European journal of medicinal chemistry
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- Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#autori
- Schenone S, Brullo C, Bruno O, Bondavalli F, Mosti L, Maga G, Crespan E, Carraro F, Manetti F, Tintori C, Botta M. (literal)
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- Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#descrizioneSinteticaDelProdotto
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- ISI Web of Science (WOS) (literal)
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- Institute of Molecular Genetics, IGM-CNR, via Abbiategrasso 207, I-27100 Pavia, Italy
Dipartimento Farmaco Chimico Tecnologico, Universita degli Studi di Siena, via Aldo Moro, I-53100 Siena, Italy; Dipartimento di Chimica delle Sostanze Naturali, Universita di Napoli Federico II, via D. Montesano 49, I-80131 Napoli, Italy; Institute of Veterinary Biochemistry and Molecular Biology, University of Zürich-Irchel, CH-8057 Zürich, Switzerland; European Research Centre for Drug Discovery and Development, Universita degli Studi di Siena, I-53100 Siena, Italy (literal)
- Titolo
- Synthesis, biological evaluation and docking studies of 4-amino substituted 1H-pyrazolo[3,4-d]pyrimidines. (literal)
- Abstract
- The synthesis of new 4-amino substituted pyrazolo[3,4-d]pyrimidines along with their activity in cell-free enzymatic assays on Src and Abl tyrosine kinases is reported. Some compounds emerged as good dual inhibitors of the two enzymes, showed antiproliferative effects on two Bcr-Abl positive leukemia cell lines K-562 and KU-812, and induced apoptosis, as demonstrated by the PARP assay. Docking studies have been also performed to analyze the binding mode of compounds under study and to identify the structural determinants of their interaction with both Src and Abl. (literal)
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