Design, synthesis and biological evaluation of 7H-pyrrolo[2,3-d]pyrimidin-4-amine derivatives as selective Btk inhibitors with improved pharmacokinetic properties for the treatment of rheumatoid arthritis.
Sign Up to like & getrecommendations! Published in 2018 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2017.12.079
Abstract: Bruton's tyrosine kinase (Btk) is a Tec family kinase with a well-defined role in the B cell receptor (BCR) and Fcγ receptor (FcR) signaling pathways, which makes it a uniquely attractive target for the treatment… read more here.
Keywords: pyrimidin amine; treatment; pyrrolo pyrimidin; btk ... See more keywords
Synthesis and crystal structure of N-(4-chlorophenyl)-5,7-dimethyl-1,2,4-triazolo[1,5-a]pyrimidin-2-amine
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DOI: 10.1107/s2056989016019629
Abstract: The title compound, N-(4-chlorophenyl)-5,7-dimethyl-1,2,4-triazolo[1,5-a]pyrimidin-2-amine, was synthesized by cyclization of 1-(4,6-dimethylpyrimidin-2-yl)-4-phenylthiosemicarbazide in the presence of Ni(NO3)2. In the crystal, molecules form inversion dimers via pairs of N—H⋯N hydrogen bonds, which are packed into layers by π-stacking… read more here.
Keywords: chlorophenyl dimethyl; pyrimidin amine; triazolo pyrimidin; dimethyl triazolo ... See more keywords
Discovery of N,4-Di(1H-pyrazol-4-yl)pyrimidin-2-amine-Derived CDK2 Inhibitors as Potential Anticancer Agents: Design, Synthesis, and Evaluation
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DOI: 10.3390/molecules28072951
Abstract: Cyclin-dependent kinase 2 (CDK2) has been garnering considerable interest as a target to develop new cancer treatments and to ameliorate resistance to CDK4/6 inhibitors. However, a selective CDK2 inhibitor has yet to be clinically approved.… read more here.
Keywords: pyrazol pyrimidin; pyrimidin amine; cancer; cdk2 inhibitors ... See more keywords
Discovery of Novel Dual Adenosine A2A and A1 Receptor Antagonists with 1H-Pyrazolo[3,4-d]pyrimidin-6-amine Core Scaffold as Anti-Parkinson’s Disease Agents
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DOI: 10.3390/ph15080922
Abstract: New compounds with 1H-pyrazolo [3,4-d]pyrimidin-6-amine core scaffolds were synthesized and characterized in vitro to determine their affinity for human A2A and A1 receptors. Among the tested compounds, a few compounds displayed nanomolar binding affinities for… read more here.
Keywords: disease; amine core; parkinson disease; pyrazolo pyrimidin ... See more keywords