The phenylamino-pyrimidine (PAP) nucleus has been demonstrated to be useful for the development of new drugs and is present in a wide variety of antiretroviral agents and tyrosine kinase inhibitors (TKIs). This review aims to evaluate the application of PAP derivatives in drugs and other bioactive compounds. It was concluded that PAP derivatives are still worth exploring, as they may provide highly competitive ATP TKI's with nano/picomolar activity.
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Phenylamino-pyrimidine (PAP) Privileged Structure: Synthesis and Medicinal Applications.
Curr Top Med Chem
November 2020
Fundacao Oswaldo Cruz, Instituto de Tecnologia em Farmacos, Farmanguinhos - Fiocruz, Laboratório de Sintese de Farmacos - LASFAR, Manguinhos, CEP 21041-250, Rio de Janeiro, RJ, Brazil.
The phenylamino-pyrimidine (PAP) nucleus has been demonstrated to be useful for the development of new drugs and is present in a wide variety of antiretroviral agents and tyrosine kinase inhibitors (TKIs). This review aims to evaluate the application of PAP derivatives in drugs and other bioactive compounds. It was concluded that PAP derivatives are still worth exploring, as they may provide highly competitive ATP TKI's with nano/picomolar activity.
View Article and Find Full Text PDFPhenylamino-pyrimidine (PAP) derivatives: a new class of potent and selective inhibitors of protein kinase C (PKC).
Arch Pharm (Weinheim)
July 1996
CIBA Pharmaceuticals Division, Oncology and Virology Research Department, Ciba-Geigy Limited., Basel, Switzerland.
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.
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