1007206-29-2

Upstream product

• 1007206-25-8 4-chloro-2-morpholin-4-yl-7-pyridin-4-yl-6,7-dihydro-5H-pyrrolo[2,3-d]pyrimidine 
• 1007206-28-1 N,N-bis[(4-methoxyphenyl)methyl]-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)pyrimidin-2-amine 
• 127915-15-5 2-oxotetrahydrofuran-3-carboxylic acid methyl ester 
• 1178564-17-4 5-(2-hydroxyethyl)-2-morpholin-4-yl-pyrimidine-4,6-diol 
• 1007206-27-0 4-[4,6-dichloro-5-(2-chloroethyl)-pyrimidin-2-yl]-morpholine 

Relevant academic research and scientific papers

Lead optimization of a dihydropyrrolopyrimidine inhibitor against phosphoinositide 3-kinase (PI3K) to improve the phenol glucuronic acid conjugation

Our lead compound for a phosphoinositide 3-kinase (PI3K) inhibitor (1) was metabolically unstable because of rapid glucuronidation of the phenol moiety. Based on structure-activity relationship (SAR) information and a FlexSIS docking simulation score, aminopyrimidine was identified as a bioisostere of phenol. An X-ray structure study revealed a hydrogen bonding pattern of aminopyrimidine derivatives. Finally, aminopyrimidine derivatives 33 showed strong tumor growth inhibition against a KPL-4 breast cancer xenograft model in vivo.

PYRIMIDINE DERIVATIVE AS PI3K INHIBITOR AND USE THEREOF

A drug is provided that is useful as a preventive or therapeutic for cancer as a result of having superior PI3K inhibitory effects as well as superior stability in the body and water-solubility. A compound, or pharmaceutically acceptable salt thereof, rep