310401-64-0

Upstream product

• 62-53-3 aniline 
• 137-43-9 Cyclopentyl bromide 
• 185408-97-3 2-chloro-N-phenyl-9H-purin-6-amine 
• 5451-40-1 2,6 dichloropurine 
• 211733-67-4 9-(cyclopentyl)-2,6-(dichloro)-9H-purine 

Relevant academic research and scientific papers

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.

Derivatives of purine, their preparation process and pharmaceutical compositions containing them

A compound of the formula wherein R is defined as in the specification, which compounds have an inhibitory effect vis-à-vis cycline-dependent kinase proteins (cdk) and are endowed with antimitotic properties.