203436-33-3

Upstream product

• 185408-97-3 2-chloro-N-phenyl-9H-purin-6-amine 
• 62-53-3 aniline 
• 5451-40-1 2,6 dichloropurine 
• 75-30-9 2-iodo-propane 
• 203436-45-7 2,6-dichloro-9-isopropyl-9H-purine 
• 75-26-3 isopropyl bromide 

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.

Design, synthesis and biological evaluation of novel histone deacetylase1/2 (HDAC1/2) and cyclin-dependent Kinase2 (CDK2) dual inhibitors against malignant cancer

In the current study, we have designed and synthesized a series of novel histone deacetylase1/2 (HDAC1/2) and cyclin-dependent kinase2 (CDK2) dual inhibitors by integrating purine-based pharmacophore into the recognition cap group of CS055. The representative compound 14d with excellent antiproliferative activities towards five solid cancer cells, showed potent inhibitory activities against HDAC1, HDAC2 and CDK2 with IC50 values of 70.7 nM, 23.1 nM and 0.80 μM, respectively. Besides, compound 14d could effectively block the cell cycle in the G2/M phase and induce apoptosis, which might be related to increasing intracellular ROS levels. Importantly, compound 14d exhibited desirable pharmacokinetic (PK) properties with the intraperitoneal bioavailability of 50.8percent in ICR mice, and potent in vivo antitumor activity in the HCT116 xenograft model. Therefore, compound 14d could be considered as a promising lead compound for the development of multitargeting anticancer agents.

Purine inhibitors of cyclin dependent kinase 2

A 2,6,9-trisubstituted purine composition having the following formula: STR1 where X is a amino, oxo, thio, of sulfone moiety, R1 is a lower alkyl, substituted lower alkyl, cycloalkyl, substituted cycloalkyl, cycloheteroalkyl, substituted cyclo

Synthesis and activity of 2,6,9-trisubstituted purines

The preparation of a series of 2,6,9-trisubstituted purines and the structure-activity data for the inhibition of cyclin dependent kinase, CDK2 are presented.