166306-32-7

Upstream product

• 123367-27-1 (E)-3-(dimethylamino)-1-(pyridin-4-yl)prop-2-en-1-one 

Relevant academic research and scientific papers

Phenylamino-pyrimidine (PAP) derivatives: A new class of potent and selective inhibitors of protein kinase C (PKC)

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.

Anti-hepatitis B application of conjugate

The invention mainly provides application of a conjugate in preparation of a medicine for treating hepatitis B virus infection. The conjugate is obtained by connecting formyl in an orlistat structureto amino in a phenylaminopyrimidine compound structure,

Potent and selective inhibitors of the Abl-kinase: Phenylaminopyrimidine (PAP) derivatives

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.

PYRIMIDINE DERIVATIVES AND PROCESSES FOR THE PREPARATION THEREOF

There are described N-phenyl-2-pyrimidine-amine derivatives of formula I wherein R1 is 4-pyrazinyl, 1-methyl-1H-pyrrolyl, amino- or amino-lower alkyl-substituted phenyl wherein the amino group in each case is free, alkylated or acylated, 1H-indolyl or 1H-imidazolyl bonded at a five-membered ring carbon atom, or unsubstituted or lower alkyl-substituted pyridyl bonded at a ring carbon atom and unsubstituted or substituted at the nitrogen atom by oxygen, R2, R3, R9, X, Y, n and R10 are defined in claim 1 These compounds can be used, for example, in the therapy of tumoral diseases.There are described N-phenyl-2-pyrimidine-amine derivatives of formula I (I) wherein R1 is 4-pyrazinyl, 1-methyl-1H-pyrrolyl, amino- or amino-lower alkyl-substituted phenyl wherein the amino group in each case is free, alkylated or acylated, 1H-indolyl or 1H-imidazolyl bonded at a five-membered ring carbon atom, or unsubstituted or lower alkyl-substituted pyridyl bonded at a ring carbon atom and unsubstituted or substituted at the nitrogen atom by oxygen, R2, R3, R9, X, Y, n and R10 are defined in claim 1. These compounds can be used, for example, in the therapy of tumoral diseases.