thienopyrimidine and Lung-Neoplasms

thienopyrimidine has been researched along with Lung-Neoplasms* in 1 studies

Other Studies

1 other study(ies) available for thienopyrimidine and Lung-Neoplasms

Article	Year
Discovery of new thienopyrimidine derivatives as potent and orally efficacious phosphoinositide 3-kinase inhibitors. Bioorganic & medicinal chemistry, 2018, 02-01, Volume: 26, Issue:3 A series of new thienopyrimidine derivatives has been discovered as potent PI3K inhibitors. The systematic SAR studies for these analogues are described. Among them, 8a and 9a exhibit nanomolar enzymatic potencies and sub-micromolar cellular anti-proliferative activities. 8a displays favorable pharmacokinetic profiles, while 9a easily undergoes deacetylation to yield a major metabolite 8a. Furthermore, 8a and 9a potently inhibit tumor growth in a dose-dependent manner in the NCI-H460 xenograft model with an acceptable safety profile. Topics: Administration, Oral; Animals; Antineoplastic Agents; Cell Line, Tumor; Cell Proliferation; Drug Evaluation, Preclinical; Enzyme Activation; Half-Life; Humans; Lung Neoplasms; Mice; Mice, Inbred BALB C; Mice, Nude; Microsomes, Liver; Phosphatidylinositol 3-Kinases; Phosphoinositide-3 Kinase Inhibitors; Protein Kinase Inhibitors; Pyrimidines; Structure-Activity Relationship; Transplantation, Heterologous	2018

Article

Year

Discovery of new thienopyrimidine derivatives as potent and orally efficacious phosphoinositide 3-kinase inhibitors.

Bioorganic & medicinal chemistry, 2018, 02-01, Volume: 26, Issue:3

A series of new thienopyrimidine derivatives has been discovered as potent PI3K inhibitors. The systematic SAR studies for these analogues are described. Among them, 8a and 9a exhibit nanomolar enzymatic potencies and sub-micromolar cellular anti-proliferative activities. 8a displays favorable pharmacokinetic profiles, while 9a easily undergoes deacetylation to yield a major metabolite 8a. Furthermore, 8a and 9a potently inhibit tumor growth in a dose-dependent manner in the NCI-H460 xenograft model with an acceptable safety profile.

Topics: Administration, Oral; Animals; Antineoplastic Agents; Cell Line, Tumor; Cell Proliferation; Drug Evaluation, Preclinical; Enzyme Activation; Half-Life; Humans; Lung Neoplasms; Mice; Mice, Inbred BALB C; Mice, Nude; Microsomes, Liver; Phosphatidylinositol 3-Kinases; Phosphoinositide-3 Kinase Inhibitors; Protein Kinase Inhibitors; Pyrimidines; Structure-Activity Relationship; Transplantation, Heterologous

2018