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Phenylamino-Pyrimidine (PAP) Derivatives: A New Class of Potent and Selective Inhibitors of Protein Kinase C (PKC)

✍ Scribed by Jürg Zimmermann; Giorgio Caravatti; Helmut Mett; Thomas Meyer; Marcel Müller; Nicholas B. Lydon; Doriano Fabbro

Publisher: John Wiley and Sons
Year: 1996
Tongue: English
Weight: 589 KB
Volume: 329
Category: Article
ISSN: 0365-6233
DOI: 10.1002/ardp.19963290707

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✦ Synopsis

Phenylamino-pyrimidines represent a novel class of inhibitors of the protein kinase C with a high degree of selectivity versus other serindthreonine and tyrosine kinases. Steady state kinetic analysis of N-(3-[ 1 -imidazolyl]-phenyl)-4-(3-pyridyl)-2-pyrimidinamine (3, 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-

a (Icso = 0.79 pM) and not the other subtypes tested. The inhibition constants of PKC-a and the antiproliferative effect on T24 human bladder carcinoma cells showed a qualitative correlation, although with some exceptions.

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