112676-08-1Relevant academic research and scientific papers
Potent and selective inhibitors of the Abl-kinase: Phenylaminopyrimidine (PAP) derivatives
Zimmermann, Juerg,Buchdunger, Elisabeth,Mett, Helmut,Meyer, Thomas,Lydon, Nicholas B.
, p. 187 - 192 (2007/10/03)
Due to its relatively clear etiology, chronic myelogenous leukemia (CML) represents an ideal disease target for a therapy using a selective inhibitor of the Bcr-Abl tyrosine protein kinase. Extensive optimization of the class of phenylamino-pyrimidines yielded highly potent and selective Bcr-Abl kinase inhibitors. Compound 1 shows high potency (IC50 = 38 nM) and selectivity for the Abl tyrosine protein kinase at the in vitro level.
Preparation of Substituted N-Phenyl-4-aryl-2-pyrimidinamines as Mediator Release Inhibitors
Paul, Rolf,Hallett, William A.,Hanifin, John W.,Reich, Marvin F.,Johnson, Bernard D.,et al.
, p. 2716 - 2725 (2007/10/02)
The role of immunologically released mediators, such as histamine, leukotrienes, and platelet-activating factor, is well-established for asthma and other allergic disorders.Developing therapeutic agents which would block mediator release from mast cells and other relevant cell types would provide a rational approach to asthma therapy.Using human basophil as a screen, a series of 4-aryl-2-(phenylamino)pyrimidines was found which inhibited mediator release.These compounds were prepared by condensing acetyl heterocycles with dimethylformamide dimethyl acetal to form enaminones which are cyclized with aryl guanidines to give pyrimidines.After examining a large number of analogs, N--4-(2-pyridinyl)-2-pyrimidinamine (1-27) was chosen for toxicological evaluation.
