330792-74-0Relevant articles and documents
Pyrazolo[3,4-d]pyrimidines containing an extended 3-substituent as potent inhibitors of Lck -- a selectivity insight.
Burchat, Andrew F,Calderwood, David J,Friedman, Michael M,Hirst, Gavin C,Li, Biqin,Rafferty, Paul,Ritter, Kurt,Skinner, Barbara S
, p. 1687 - 1690 (2002)
A series of para-substituted 3-phenyl pyrazolopyrimidines was synthesized and evaluated as inhibitors of lck. The nature of the substitution affected enzyme selectivity and potency for lck, src, kdr, and tie-2. The para-phenoxyphenyl analogue 2 is an orally active lck inhibitor with a bioavailability of 69% and exhibits an extended duration of action in animal models of T cell inhibition.
Substituted 4-amino-1H-pyrazolo[3,4-d]pyrimidines as multi-targeted inhibitors of insulin-like growth factor-1 receptor (IGF1R) and members of ErbB-family receptor kinases
Wang, Gary T.,Mantei, Robert A.,Hubbard, Robert D.,Wilsbacher, Julie L.,Zhang, Qian,Tucker, Lora,Hu, Xiaoming,Kovar, Peter,Johnson, Eric F.,Osterling, Donald J.,Bouska, Jennifer,Wang, Jieyi,Davidsen, Steven K.,Bell, Randy L.,Sheppard, George S.
scheme or table, p. 6067 - 6071 (2010/11/18)
This Letter describes the lead discovery, optimization, and biological characterization of a series of substituted 4-amino-1H-pyrazolo[3,4-d] pyrimidines as potent inhibitors of IGF1R, EGFR, and ErbB2. The leading compound 11 showed an IGF1R IC50 of 12 nM, an EGFR (L858R) IC50 of 31 nM, and an ErbB2 IC50 of 11 nM, potent activity in cellular functional and anti-proliferation assays, as well as activity in an in vivo pharmacodynamic assay.