Reznickova, Eva published the artcileActivity of 2,6,9-trisubstituted purines as potent PDGFRα kinase inhibitors with antileukaemic activity, Name: 4-(2-Pyrimidinyloxy)aniline, the publication is European Journal of Medicinal Chemistry (2019), 111663, database is CAplus and MEDLINE.
Receptor tyrosine kinase PDGFRα is often constitutively activated in various tumors and is regarded as a drug target. Here, we present a collection of 2,6,9-trisubstituted purines with nanomolar potency against PDGFRα and strong and selective cytotoxicity in the human eosinophilic leukemia cell line EOL-1 that expresses the FIP1L1-PDGFRA oncogene. In treated EOL-1 cells, the example compound 14q inhibited the autophosphorylation of PDGFRα and the phosphorylation of STAT3 and ERK1/2. Interestingly, we observed pronounced and even increased effects of 14q on PDGFRα and some of its downstream signalling pathways after drug washout. In accordance with suppressed PDGFRα signalling, treated cells were arrested in the G1 phase of the cell cycle and eventually underwent apoptosis. Our results show that substituted purines can be used as specific modulators of eosinophilic leukemia.
European Journal of Medicinal Chemistry published new progress about 105130-26-5. 105130-26-5 belongs to pyrimidines, auxiliary class Pyrimidine,Amine,Benzene,Ether, name is 4-(2-Pyrimidinyloxy)aniline, and the molecular formula is C10H9N3O, Name: 4-(2-Pyrimidinyloxy)aniline.
Referemce:
https://pubchem.ncbi.nlm.nih.gov/compound/Pyrimidine,
Pyrimidine – Wikipedia