1056015-98-5

Upstream product

• 203436-45-7 2,6-dichloro-9-isopropyl-9H-purine 
• 98-80-6 phenylboronic acid 
• 24388-23-6 2-phenyl-4,4,5,5-tetramethyl-1,3,2-dioxoborole 

Downstream Products

• 1056016-01-3 (R)-2-(1-hydroxy-but-2-ylamino)-6-phenyl-9-iso-propylpurine 

Relevant academic research and scientific papers

Pyrimido five-membered heterocyclic compound and application as mutant IDH2 inhibitor

The invention relates to a pyrimido five-membered heterocyclic compound and an application of the pyrimido five-membered heterocyclic compound as a mutant IDH2 inhibitor, and specifically discloses apyrimido five-membered heterocyclic compound capable of being used as a mutant IDH2 inhibitor, or a stereoisomer or tautomer thereof, or a pharmaceutically acceptable salt, a hydrate or a solvate thereof. The invention also relates to a pharmaceutical composition containing the compound, and application of the pharmaceutical composition in preparation of drugs for preventing and/or treating mutantIDH2 mediated diseases.

Roscovitine-derived, dual-specificity inhibitors of cyclin-dependent kinases and casein kinases 1

Cyclin-dependent kinases (CDKs) and casein kinases 1 (CK1) are involved in the two key molecular features of Alzheimer's disease, production of amyloid-β peptides (extracellular plaques) and hyper-phosphorylation of Tau (intracellular neurofibrillary tangles). A series of 2,6,9-trisubstituted purines, structurally related to the CDK inhibitor roscovitine, have been synthesized. They mainly differ by the substituent on the C-6 position. These compounds were screened for kinase inhibitory activities and antiproliferative effects. Several biaryl derivatives displayed potent inhibition of both CDKs and CK1. In particular, derivative 13a was a potent inhibitor of CDK1/cyclin B (IC50: 220 nM), CDK5/p25 (IC50: 80 nM), and CK1 (IC 50: 14 nM). Modeling of these molecules into the ATP-binding pocket of CK1δ provided a rationale for the increased selectivity toward this kinase. 13a was able to prevent the CK1-dependent production of amyloid-β in a cell model. CDK/CK1 dual-specificity inhibitors may have important applications in Alzheimer's disease and cancers.