190654-77-4

Upstream product

• 5451-40-1 2,6 dichloropurine 
• 108-42-9 3-chloro-aniline 
• 190655-14-2 2,6-dichloro-9-ethyl-9H-purine 
• 75-03-6 ethyl iodide 
• 190654-76-3 2-chloro-6-(3-chlorophenylamino)-purine 

Downstream Products

• 190654-11-6 1-[6-(3-chloro-phenylamino)-9-ethyl-9H-purin-2-yl]-pyrrolidine-2-carboxylic acid amide 
• 190654-48-9 6-(3-chloro-phenyl-amino)-9-ethyl-2-(3-hydroxy-2-methyl-prop-2-yl-amino)-9H-purine 
• 190654-49-0 6-(3-chloro-phenyl-amino)-9-ethyl-2-piperidino-9H-purine 
• 190654-04-7 N²-((1R,2R)-2-aminocyclohexyl)-N⁶-(3-chlorophenyl)-9-ethyl-9H-purine-2,6-diamine 
• 190654-17-2 6-(3-chloro-phenyl-amino)-9-ethyl-2-[imidazol-1-yl]-9H-purine 
• 190654-56-9 6-(3-chloro-phenyl-amino)-9-ethyl-2-[(S)-2-hydroxy-propylamino]-9H-purine 
• 190654-55-8 6-(3-chloro-phenyl-amino)-9-ethyl-2-[(R)-2-hydroxy-propylamino]-9H-purine 
• 190654-51-4 6-(3-chloro-phenyl-amino)-9-ethyl-2-[(R)-1-hydroxy-but-2-yl-amino)-9H-purine 
• 190654-50-3 6-(3-chloro-phenyl-amino)-9-ethyl-2-[(S)-1-hydroxy-but-2-yl-amino]-9H-purine 
• 190654-53-6 6-(3-chloro-phenyl-amino)-9-ethyl-2-(1,3-dihydroxy-prop-2-yl-amino)-9H-purine 
• 190654-25-2 2-[2-amino-phenyl-amino]-6-(3-chloro-phenyl-amino)-9-ethyl-9H-purine 
• 190653-76-0 2-(3-amino-propyl-amino)-6-(3-chloro-phenyl-amino)-9-ethyl-9H-purine 
• 190653-85-1 2-(tetrahydrofurfuryl-amino)-6-(3-chloro-phenyl-amino)-9-ethyl-9H-purine 
• 190654-09-2 2-(adamant-1-ylamino)-6-(3-chloro-phenyl-amino)-9-ethyl-9H-purine 

Relevant academic research and scientific papers

DUAL CLK/CDK1 INHIBITORS FOR CANCER TREATMENT

This disclosure generally relates to dual CLK2/CDK1 inhibitors or more potent and specific CLK inhibitors to target CLK2 and CDKl kinases in the treatment of germ-line mutations of the spliceosome leading to the development of cancers and other human dise

A triple exon-skipping luciferase reporter assay identifies a new CLK inhibitor pharmacophore

The splicing of pre-mRNA is a critical process in normal cells and is deregulated in cancer. Compounds that modulate this process have recently been shown to target a specific vulnerability in tumors. We have developed a novel cell-based assay that specifically activates luciferase in cells exposed to SF3B1 targeted compounds, such as sudemycin D6. This assay was used to screen a combined collection of approved drugs and bioactive compounds. This screening approach identified several active hits, the most potent of which were CGP-74514A and aminopurvalanol A, both have been reported to be cyclin-dependent kinases (CDKs) inhibitors. We found that these compounds, and their analogs, show significant cdc2-like kinase (CLK) inhibition and clear structure-activity relationships (SAR) at CLKs. We prepared a set of analogs and were able to ‘dial out’ the CDK activity and simultaneously developed CLK inhibitors with low nanomolar activity. Thus, we have demonstrated the utility of our exon-skipping assay and identified new molecules that exhibit potency and selectivity for CLK, as well as some structurally related dual CLK/CDK inhibitors.

Identification and optimization of inhibitors of trypanosomal cysteine proteases: Cruzain, rhodesain, and TbCatB

Trypanosoma cruzi and Trypanosoma brucei are parasites that cause Chagas' disease and African sleeping sickness, respectively. Both parasites rely on essential cysteine proteases for survival: cruzain for T. cruzi and TbCatB/rhodesain for T. brucei. A rec

SUBSTITUTED TRIAZINE AND PURINE COMPOUNDS, METHODS OF INHIBITING CRUZAIN AND RHODESAIN AND METHODS OF TREATING CHAGAS DISEASE AND AFRICAN TRYPANOSOMIASIS

The invention provides for novel triazine and purine compounds ( II ) that are useful for the treatment and prevention of mammalian protozoal diseases, including Af rican trypanosomiasis and Chagas disease.

2,6,9-Trisubstituted purines: Optimization towards highly potent and selective CDK1 inhibitors

Novel 2,6,9-substituted purine derivatives represent a class of potent and selective inhibitors of CDK1/cyclinB. The synthesis, SAR and biological profile of selected compounds are described.