1007206-28-1

Upstream product

• 5419-55-6 Triisopropyl borate 
• 1272403-00-5 5-bromo-N,N-bis[(4-methoxyphenyl)methyl]pyrimidin-2-amine 
• 824-94-2 p-methoxybenzyl chloride 
• 76-09-5 2,3-dimethyl-2,3-butane diol 

Downstream Products

• 1272403-08-3 C₃₅H₃₆N₈O₃ 
• 1007208-63-0 [3-[4-[2-[bis[(4-methoxyphenyl)methyl]amino]pyrimidin-5-yl]-2-morpholin-4-yl-5,6-dihydropyrrolo[2,3-d]pyrimidin-7-yl]phenyl]-(4-methylpiperazin-1-yl)methanone 
• 1007208-13-0 4-[4-[2-[bis[(4-methoxyphenyl)methyl]amino]pyrimidin-5-yl]-2-morpholino-5,6-dihydropyrrolo[2,3-d]pyrimidin-7-yl]benzaldehyde 
• 1007210-13-0 [4-(4-{2-[bis-(4-methoxy-benzyl)-amino]-pyrimidin-5-yl}-2-morpholin-4-yl-5,6-dihydro-pyrrolo[2,3-d]pyrimidin-7-yl)-phenyl]-(4-methyl-piperazin-1-yl)-methanone 
• 1007207-65-9 N,N-bis[(4-methoxyphenyl)methyl]-5-(2-morpholino-6,7-dihydro-5H-pyrrolo[2,3-d]pyrimidin-4-yl)pyrimidin-2-amine 
• 1178564-19-6 1-[4-[2-[bis[(4-methoxyphenyl)methyl]amino]pyrimidin-5-yl]-2-morpholino-5,6-dihydro-pyrrolo[2,3-d]pyrimidin-7-yl]ethanone 
• 1007206-29-2 bis-(4-methoxybenzyl)-[5-(2-morpholin-4-yl-7-pyridin-4-yl-6,7-dihydro-5H-pyrrolo[2,3-d]pyrimidin-4-yl)-pyrimidin-2-yl]-amine 

Relevant academic research and scientific papers

Modification of a dihydropyrrolopyrimidine phosphoinositide 3-kinase (PI3K) inhibitor to improve oral bioavailability

Phosphoinositide 3-kinase (PI3K) is activated in various human cancer cells and well known as a cancer therapy target. We previously reported a dihydropyrrolopyrimidine derivative as a highly potent PI3K inhibitor that has strong tumor growth inhibition in a xenograft model. In this report, we describe further optimization to improve its bioavailability.

Discovery and biological activity of a novel class i PI3K inhibitor, CH5132799

Phosphatidylinositol 3-kinase (PI3K) is a lipid kinase and a promising therapeutic target for cancer. Using structure-based drug design (SBDD), we have identified novel PI3K inhibitors with a dihydropyrrolopyrimidine skeleton. Metabolic stability of the first lead series was drastically improved by replacing phenol with aminopyrimidine moiety. CH5132799, a novel class I PI3K inhibitor, exhibited a strong inhibitory activity especially against PI3Kα (IC50 = 0.014 μM). In human tumor cell lines with PI3K pathway activation, CH5132799 showed potent antiproliferative activity. CH5132799 is orally available and showed significant antitumor activity in PI3K pathway-activated human cancer xenograft models in mice.