Pyrazolo[3,4-d]pyrimidines containing an extended 3-substituent as potent inhibitors of Lck -- a selectivity insight |
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Authors: | Burchat Andrew F Calderwood David J Friedman Michael M Hirst Gavin C Li Biqin Rafferty Paul Ritter Kurt Skinner Barbara S |
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Affiliation: | Abbott Bioresearch Center, 100 Research Drive, Worcester, MA 01605-5314, USA. |
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Abstract: | 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. |
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