Lee, Wendy; Ortwine, Daniel F.; Bergeron, Philippe; Lau, Kevin; Lin, Lichuan; Malek, Shiva; Nonomiya, Jim; Pei, Zhonghua; Robarge, Kirk D.; Schmidt, Stephen; Sideris, Steve; Lyssikatos, Joseph P. published the artcile< A hit to lead discovery of novel N-methylated imidazolo-, pyrrolo-, and pyrazolo-pyrimidines as potent and selective mTOR inhibitors>, Recommanded Product: 2,6-Dichloro-9-methyl-9H-purine, the main research area is imidazolo pyrrolo pyrazolo pyrimidine preparation mTOR inhibitor; Mammalian target of rapamycin; Oncology; PI3K/Akt/mTOR pathway; Structure based design; mTOR kinase inhibitors.
A series of N-7-methyl-imidazolopyrimidine inhibitors I [R1 = Me, Et; R2 = N-morpholinyl, N-homomorpholinyl, N-(S)-3-methylmorpholinyl, N-(R)-3-methylmorpholinyl] of the mTOR kinase have been designed and prepared, based on the hypothesis that the N-7-Me substituent on imidazolopyrimidine would impart selectivity for mTOR over the related PI3Kα and δ kinases. The corresponding N-Me substituted pyrrolo[3,2-d]pyrimidines and pyrazolo[4,3-d]pyrimidines also show potent mTOR inhibition with selectivity toward both PI3α and δ kinases. The most potent compound synthesized is pyrazolo[4,3-d]pyrimidine II [R1 = Me, R2 = (S)-3-ethylmorpholin-4-yl]. Compound II shows a Ki of 2 nM against mTOR inhibition, remarkable selectivity (>2900×) over PI3 kinases, and excellent potency in cell-based assays.
Bioorganic & Medicinal Chemistry Letters published new progress about Molecular docking. 2382-10-7 belongs to class chlorides-buliding-blocks, and the molecular formula is C6H4Cl2N4, Recommanded Product: 2,6-Dichloro-9-methyl-9H-purine.
Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics