Lin, Songwen; Wang, Chunyang; Ji, Ming; Wu, Deyu; Lv, Yuanhao; Sheng, Li; Han, Fangbin; Dong, Yi; Zhang, Kehui; Yang, Yakun; Li, Yan; Chen, Xiaoguang; Xu, Heng published the artcile< Discovery of new thienopyrimidine derivatives as potent and orally efficacious phosphoinositide 3-kinase inhibitors>, Category: esters-buliding-blocks, the main research area is thienopyrimidine synthesis antitumor SAR pharmacokinetics phosphoinositide kinase PI3K; Acetylation; Anti-tumor activities; Phosphoinositide 3-kinase inhibitors; Thienopyrimidine.
A series of new thienopyrimidine derivatives has been discovered as potent PI3K inhibitors. The systematic SAR studies for these analogs are described. Among them, I and II exhibit nanomolar enzymic potencies and sub-micromolar cellular anti-proliferative activities. I displays favorable pharmacokinetic profiles, while II easily undergoes deacetylation to yield a major metabolite I. Furthermore, I and II potently inhibit tumor growth in a dose-dependent manner in the NCI-H460 xenograft model with an acceptable safety profile.
Bioorganic & Medicinal Chemistry published new progress about Acetylation. 112-63-0 belongs to class esters-buliding-blocks, and the molecular formula is C19H34O2, Category: esters-buliding-blocks.
Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics