New pyrazolo[1,5a]pyrimidines as orally active inhibitors of Lck
Copyright policy ) Nina, Gommermann; Peter, Buehlmayer; Anette, von Matt; Werner, Breitenstein; Keiichi, Masuya; Bernard, Pirard; Pascal, Furet; +2 Authors
Nina, Gommermann; Peter, Buehlmayer; Anette, von Matt; Werner, Breitenstein; Keiichi, Masuya; Bernard, Pirard; Pascal, Furet; Sandra W, Cowan-Jacob; Gisbert, Weckbecker;
New pyrazolo[1,5a]pyrimidines as orally active inhibitors of Lck
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.
- Novartis Institutes for BioMedical Research Switzerland
- Novartis (Switzerland) Switzerland
Administration, Oral, Lymphocyte Activation, Rats, Mice, Structure-Activity Relationship, Pyrimidines, Lymphocyte Specific Protein Tyrosine Kinase p56(lck), Microsomes, Liver, Animals, Humans, Interleukin-2
Administration, Oral, Lymphocyte Activation, Rats, Mice, Structure-Activity Relationship, Pyrimidines, Lymphocyte Specific Protein Tyrosine Kinase p56(lck), Microsomes, Liver, Animals, Humans, Interleukin-2
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This is an alternative to the "Influence" indicator, which also reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically).
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