pi103 has been researched along with pyrimidine* in 3 studies
3 other study(ies) available for pi103 and pyrimidine
| Article | Year |
|---|---|
Discovery of thiapyran-pyrimidine derivatives as potential EGFR inhibitors.
Topics: Antineoplastic Agents; Cell Line, Tumor; Cell Proliferation; Dose-Response Relationship, Drug; Drug Discovery; Drug Screening Assays, Antitumor; ErbB Receptors; Humans; Molecular Docking Simulation; Molecular Structure; Protein Kinase Inhibitors; Pyrans; Pyrimidines; Structure-Activity Relationship | 2020 |
Rational discovery of a highly novel and selective mTOR inhibitor.
Aided by Structure Based Drug Discovery (SBDD), we rapidly designed a highly novel and selective series of mTOR inhibitors. This chemotype conveys exquisite kinase selectivity, excellent in vitro and in vivo potencies and ADME safety profiles. These compounds could serve as good tools to explore the potential of TORC inhibition in various human diseases. Topics: Binding, Competitive; Drug Discovery; Furans; Humans; Models, Molecular; Molecular Structure; Morpholines; Phosphatidylinositol 3-Kinase; Protein Binding; Protein Kinase Inhibitors; Pyridines; Pyrimidines; Structure-Activity Relationship; TOR Serine-Threonine Kinases | 2019 |
Design, synthesis, anticancer activity and docking studies of novel 4-morpholino-7,8-dihydro-5H-thiopyrano[4,3-d]pyrimidine derivatives as mTOR inhibitors.
A series of 7,8-dihydro-5H-thiopyrano[4,3-d]pyrimidine derivatives (7a-q, 10a-q) were designed, synthesized and their chemical structures were confirmed by 1H NMR, 13C NMR, MS and HRMS spectrum.All the compounds were evaluated for the inhibitory activity against mTOR kinase at 10 μM level. Five selected compounds (7b, 7e, 7h, 10b and 10e) were further evaluated for the inhibitory activity against PI3Ka at 10 μM level, and the IC50 values against mTOR kinase and two cancer cell lines. Twelve of the target compounds exhibited moderate antitumor activities. The most promising compound 7e showed strong antitumor activities against mTOR kinase, H460 and PC-3 cell lines with IC50 values of 0.80 ± 0.15 μM, 7.43 ± 1.45 μM and 11.90 ± 0.94 μM, which were 1.28 to 1.71-fold more active than BMCL-200908069-1 (1.37 ± 0.07 μM, 9.52 ± 0.29 μM, 16.27 ± 0.54 μM), respectively. Structure-activity relationships (SARs) and docking studies indicated that the thiopyrano[4,3-d]pyrimidine scaffolds exerted little effect on antitumor activities of target compounds. Substitutions of aryl group at C-4 position had a significant impact on the antitumor activities, and 4-OH substitution produced the best potency. Topics: Antineoplastic Agents; Binding Sites; Cell Line, Tumor; Cell Survival; Drug Design; Humans; Molecular Docking Simulation; Protein Binding; Protein Kinase Inhibitors; Protein Structure, Tertiary; Pyrimidines; Structure-Activity Relationship; TOR Serine-Threonine Kinases | 2014 |