181065-58-7Relevant articles and documents
Expedient parallel synthesis of 2-amino-4-heteroarylpyrimidines
Bursavich, Matthew G.,Lombardi, Sabrina,Gilbert, Adam M.
, p. 4113 - 4116 (2007/10/03)
(Chemical Equation Presented) An expedient synthesis of diverse 2-amino-4-heteroarylpyrimidines via a 2-chloropyrimidine intermediate is described. A series of potentially biologically active analogues have been synthesized in two parallel steps to afford focused arrays.
N-PHENYL-2-PYRIMIDINE-AMINE DERIVATIVES AND PROCESS FOR THE PREPARATION THEREOF
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Page 10; 21, (2010/02/09)
The present invention relates to an N-phenyl-2-pyrimidine-amine derivative showing a superior effect on tumor, lung cancer, gastric cancer, etc. of warm-blooded animals and its salt. The present invention also relates to a process for preparing the compound and a pharmaceutical composition for the prevention and treatment of such diseases as tumor, lung cancer, gastric cancer, etc., which comprises the compound as an active ingredient.
Phenylamino-pyrimidine (PAP) derivatives: A new class of potent and selective inhibitors of protein kinase C (PKC)
Zimmermann, Juerg,Caravatti, Giorgio,Mett, Helmut,Meyer, Thomas,Mueller, Marcel,Lydon, Nicholas B.,Fabbro, Doriano
, p. 371 - 376 (2007/10/03)
Phenylamino-pyrimidines represent a novel class of inhibitors of the protein kinase C with a high degree of selectivity versus other serine/threonine and tyrosine kinases. Steady state kinetic analysis of N-(3-[1-imidazolyl]-phenyl)-4-(3-pyridyl)-2-pyrimidinamine (5), which showed potent inhibitory activity, revealed competitive kinetics relative to ATP. The adjacent H-bond acceptor of the pyrimidine moiety next to an H-bond donor of the phenylamine was found to be crucial for inhibitory activity. N-(3-Nitro-phenyl)-4-(3-pyridyl)-2-pyrimidinamine (7) preferentially inhibited PKC-α (IC50 = 0.79 μM) and not the other subtypes tested. The inhibition constants of PKC-α and the antiproliferative effect on T24 human bladder carcinoma cells showed a qualitative correlation, although with some exceptions.