1448338-07-5

Upstream product

• 1448338-03-1 N²-(4-aminocyclohexyl)-N⁶-(4-bromobenzyl)-9-cyclopentyl-9H-purine-2,6-diamine 
• 768-35-4 3-fluorophenylboronic acid 
• 211733-67-4 9-(cyclopentyl)-2,6-(dichloro)-9H-purine 
• 5451-40-1 2,6 dichloropurine 
• 1448337-97-0 (4-bromobenzyl)(2-chloro-9-cyclopentyl-9H-purine-6-yl)amine 

Relevant academic research and scientific papers

2-SUBSTITUTED-6-BIARYLMETHYLAMINO-9-CYCLOPENTYL-9H-PURINE DERIVATIVES, USE THEREOF AS MEDICAMENTS, AND PHARMACEUTICAL COMPOSITIONS

This invention relates to novel 2-substituted-6-biarylmethylamino-9-cyclopentyl-9H-purine derivatives, showing activity as specific inhibitors of growth and angiogenesis of hepatocellular carcinoma. The invention further includes pharmaceutical compositions containing the 2-substituted-6-biarylmethylamino-9-cyclopentylpurines.

A novel series of highly potent 2,6,9-trisubstituted purine cyclin-dependent kinase inhibitors

The inhibition of overactive CDKs during cancer remains an important strategy in cancer drug development. We synthesized and screened a novel series of 2-substituted-6-biarylmethylamino-9-cyclopentylpurine derivatives for improved CDK inhibitory activity and antiproliferative effects. One of the most potent compounds, 6b, exhibited strong cytotoxicity in the human melanoma cell line G361 that correlated with robust CDK1 and CDK2 inhibition and caspase activation. In silico modeling of 6b in the active site of CDK2 revealed a high interaction energy, which we believe is due to the 6-heterobiarylmethylamino substitution of the purine moiety.