- Expedient parallel synthesis of 2-amino-4-heteroarylpyrimidines
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(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.
- Bursavich, Matthew G.,Lombardi, Sabrina,Gilbert, Adam M.
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p. 4113 - 4116
(2007/10/03)
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- N-phenyl-2-pyrimidine-amine derivatives and process for the preparation thereof
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The present invention relates to an N-phenyl-2-pyrimidine-amine derivative showing a superior effect on lung cancer, gastric cancer, colon cancer, pancreatic cancer, hepatoma, prostatic cancer, breast cancer, chronic or acute leukemia, hematologic malignancy, encephalophyma, bladder cancer, rectal cancer, or cervical cancer, etc. of warm-blooded animals and its salt. The present invention also relates to a process for preparing the compound, and to a pharmaceutical composition for the treatment of the above various diseases, which comprises an effective amount of the compound as an active ingredient together with pharmaceutically acceptable inert carriers.
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- N-PHENYL-2-PYRIMIDINE-AMINE DERIVATIVES AND PROCESS FOR THE PREPARATION THEREOF
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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.
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- N-PHENYL-2-PYRIMIDINE-AMINE DERIVATIVES AND PROCESS FOR THE PREPARATION THEREOF
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The present invention relates to an N-Phenyl-2-pyrimidine-aminine derivative showing a superior effect on lung cancer, gastric cancer, colon cancer, pancreatic cancer, hepatoma, prostatic cancer, breast cancer, chronic or accute leukemia, hematologic malignancy, encephalophyma, bladder cancer, rectal cancer or cervical cancer, etc. of warm blooded animals and its salt. The present invention also relates to a process for preparing the compound, and to a pharmaceutical composition for the treatment of the above various disease, which comprises an effective amount of the compound as an active ingredient together with pharmaceutically acceptable inert carriers.
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Page 9-10; 19-20
(2010/02/09)
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- Phenylamino-pyrimidine (PAP) derivatives: A new class of potent and selective inhibitors of protein kinase C (PKC)
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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.
- Zimmermann, Juerg,Caravatti, Giorgio,Mett, Helmut,Meyer, Thomas,Mueller, Marcel,Lydon, Nicholas B.,Fabbro, Doriano
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p. 371 - 376
(2007/10/03)
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