Literature DB >> 20483608

New pyrazolo[1,5a]pyrimidines as orally active inhibitors of Lck.

Nina Gommermann1, Peter Buehlmayer, Anette von Matt, Werner Breitenstein, Keiichi Masuya, Bernard Pirard, Pascal Furet, Sandra W Cowan-Jacob, Gisbert Weckbecker.   

Abstract

A novel series of pyrazolo[1,5a]pyrimidines was optimized to target lymphocyte-specific kinase (Lck). An efficient synthetic route was developed and SAR studies toward activity and selectivity are described, leading to Lck inhibitors with enzymatic, cellular and in vivo potency. Copyright 2010 Elsevier Ltd. All rights reserved.

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Year:  2010        PMID: 20483608     DOI: 10.1016/j.bmcl.2010.04.112

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  2 in total

1.  Small Molecule Amyloid-β Protein Precursor Processing Modulators Lower Amyloid-β Peptide Levels via cKit Signaling.

Authors:  Ci-Di Chen; Ella Zeldich; Christina Khodr; Kaddy Camara; Tze Yu Tung; Emma C Lauder; Patrick Mullen; Taryn J Polanco; Yen-Yu Liu; Dean Zeldich; Weiming Xia; William E Van Nostrand; Lauren E Brown; John A Porco; Carmela R Abraham
Journal:  J Alzheimers Dis       Date:  2019       Impact factor: 4.472

2.  A facile, regioselective synthesis of novel 3-(N-phenylcarboxamide)pyrazolo[1,5-a]pyrimidine analogs in the presence of KHSO4 in aqueous media assisted by ultrasound and their antibacterial activities.

Authors:  Shunan Kaping; Ivee Boiss; Laishram Indira Singha; Philippe Helissey; Jai N Vishwakarma
Journal:  Mol Divers       Date:  2015-10-28       Impact factor: 2.943

  2 in total

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