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Title: Exploring the chemical space around the privileged pyrazolo[3,4-d]pyrimidine scaffold: toward novel allosteric inhibitors of T315I-mutated Abl.
Authors: Vignaroli, Giulia
Mencarelli, M.
Sementa, Deborah
Crespan, E.
Kissova, M.
Maga, G.
Schenone, S.
Botta, Maurizio 
Botta, Maurizio 
Issue Date: 2014
Project: None 
A library of pyrazolo[3,4-d]pyrimidines, endowed with a high level of molecular diversity, has been developed applying a synthetic sequence that allowed C3, N1, C4, and C6 substitution. The enzymatic screening of this "privileged scaffold"-based compound collection, validated the use of a diversity-oriented approach in a field characteristically explored by target-oriented synthesis. In fact, several compounds showed high activity against the selected kinases (i.e., Src, Abl wt, and T315I mutated-form), furthermore and interestingly a new compound has emerged as an allosteric inhibitor of the T315I mutated-form of Abl, opening up new opportunities for the development of a novel class of noncompetitive inhibitors of Abl (T315I).
ISSN: 2156-8952
DOI: 10.1021/co500004e
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