294648-01-4

Upstream product

• 294647-99-7 2-chloro-6-[4-(2-pyridyl)phenylmethylamino]purine 
• 75-26-3 isopropyl bromide 
• 294647-99-7 2-chloro-6-[4-(2-pyridyl)phenylmethylamino]-purine 
• 5451-40-1 2,6-dichloro-7H-purine 
• 294647-97-5 1-[4-(pyridin-2-yl)phenyl]methanamine 
• 203436-45-7 2,6-dichloro-9-isopropyl-9H-purine 

Downstream Products

• 294646-77-8 (R)-CR8 
• 1243148-40-4 (S)-3-[9-isopropyl-6-(4-pyridin-2-yl-benzylamino)-9H-purin-2-ylamino]-propane-1,2-diol 
• 1130281-21-8 2-(1,3-Dihydroxyprop-2-ylamino)-6-[4-(2-pyridyl)phenylmethylamino]-9-isopropylpurine 
• 1056016-24-0 2-(1-hydroxy-2-methylprop-2-ylamino)-6-[4-(2-pyridyl)phenylmethylamino]-9-iso-propylpurine 
• 1056016-22-8 (R)-2-(1-hydroxy-3-methylbut-2-ylamino)-6-[4-(2-pyridyl)phenylmethylamino]-9-iso-propylpurine 

Relevant academic research and scientific papers

Synthesis and biological evaluation of selective and potent cyclin-dependent kinase inhibitors

A new series of 2,6,9-trisubstituted purines, structurally related to the cyclin-dependent kinase (CDK) inhibitor Roscovitine, has been synthesized. These compounds mainly differ by the substituent on the C-2 position which encompasses a diol group. These

USE OF PURINE DERIVATIVES FOR THE MANUFACTURE OF A MEDICAMENT

The invention relates to the use of purine derivatives in the manufacture of a medicament for treating pathological conditions in which an imbalance between cell division and apoptosis is involved, and more particularly in which excessive apoptosis is res

METHOD OF TREATMENT OF POLYCYSTIC DISEASES AND CHRONIC LYMPHOCYTIC LEUKEMIA

The present invention concerns a method of treatment of polycystic diseases or of reducing and/or avoiding cyst formation in a patient with cystic disease, which comprises at least one step consisting in administering to said patient an effective amount of a 2,6,9-trisubstituted purine compound of formula (VII): wherein A represents alternatively a (A.1) or (A.2) group.

Practical synthesis of roscovitine and CR8

Roscovitine and CR8 are potent inhibitors of cyclin-dependent kinases. A scalable synthesis of both inhibitors is described. In the case of CR8, the biarylmethylamine moiety was obtained as a stable and high-purity salt.

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.