Structure–Activity Relationships of Phosphoinositide 3-Kinase (PI3K)/Mammalian Target of Rapamycin (mTOR) Dual Inhibitors: Investigations of Various 6,5-Heterocycles to Improve Metabolic Stability

2011 ◽  
Vol 54 (14) ◽  
pp. 5174-5184 ◽  
Author(s):  
Markian M. Stec ◽  
Kristin L. Andrews ◽  
Shon K. Booker ◽  
Sean Caenepeel ◽  
Daniel J. Freeman ◽  
...  
Keyword(s):  
Mammalian Target Of Rapamycin ◽  
Metabolic Stability ◽  
Target Of Rapamycin ◽  
Structure Activity Relationships ◽  
Structure Activity ◽  
Dual Inhibitors ◽  
Phosphoinositide 3 Kinase

Discovery and Optimization of a Series of Benzothiazole Phosphoinositide 3-Kinase (PI3K)/Mammalian Target of Rapamycin (mTOR) Dual Inhibitors

2011 ◽  
Vol 54 (6) ◽  
pp. 1789-1811 ◽  
Author(s):  
Noel D. D’Angelo ◽  
Tae-Seong Kim ◽  
Kristin Andrews ◽  
Shon K. Booker ◽  
Sean Caenepeel ◽  
...  
Keyword(s):  
Mammalian Target Of Rapamycin ◽  
Target Of Rapamycin ◽  
Dual Inhibitors ◽  
Phosphoinositide 3 Kinase

Lupeol Inhibits Proliferation and Promotes Apoptosis of Ovarian Cancer Cells by Inactivating Phosphoinositide-3-Kinase/Protein Kinase B/ Mammalian Target of Rapamycin Pathway

2020 ◽  
Vol 19 (2) ◽  
pp. 206-210
Author(s):  
Feng Chen ◽  
Bei Zhang
Keyword(s):  
Cell Cycle ◽  
Ovarian Cancer ◽  
Protein Kinase ◽  
Cell Viability ◽  
Cancer Cells ◽  
Protein Kinase B ◽  
Mammalian Target Of Rapamycin ◽  
Target Of Rapamycin ◽  
Ovarian Cancer Cells ◽  
Phosphoinositide 3 Kinase

Lupeol exhibits multiple pharmacological activities including, anticancerous, anti-inflammatory, and antioxidant. The aim of this study was to explore the anticancerous activity of lupeol on ovarian cancer cells and examine its mechanism of action. To this end, increasing concentrations of lupeol on cell viability, cell cycle, and apoptosis in Caov-3 cells were evaluated. Lupeol inhibited cell viability, induced G1 phase arrest in cell cycle, increased cell apoptosis, and inhibited the ratio of phospho-Akt/protein kinase B and phospho-mammalian target of rapamycin/mammalian target of rapamycin. In conclusion, these data suggest that lupeol may play a therapeutic role in ovarian cancer.

The imidazo[1,2-a]pyridine ring system as a scaffold for potent dual phosphoinositide-3-kinase (PI3K)/mammalian target of rapamycin (mTOR) inhibitors

2015 ◽  
Vol 25 (19) ◽  
pp. 4136-4142 ◽  
Author(s):  
Markian M. Stec ◽  
Kristin L. Andrews ◽  
Yunxin Bo ◽  
Sean Caenepeel ◽  
Hongyu Liao ◽  
...  
Keyword(s):  
Pyridine Ring ◽  
Mammalian Target Of Rapamycin ◽  
Mtor Inhibitors ◽  
Ring System ◽  
Target Of Rapamycin ◽  
Phosphoinositide 3 Kinase

scholarly journals Characterization of Antineovascularization Activity and Ocular Pharmacokinetics of Phosphoinositide 3-Kinase/Mammalian Target of Rapamycin Inhibitor GNE-947

2020 ◽  
Vol 48 (5) ◽  
pp. 408-419
Author(s):  
Xingrong Liu ◽  
Xiaorong Liang ◽  
Jenninfer LeCouter ◽  
Savita Ubhayakar ◽  
Jacob Chen ◽  
...  
Keyword(s):  
Mammalian Target Of Rapamycin ◽  
Target Of Rapamycin ◽  
Ocular Pharmacokinetics ◽  
Phosphoinositide 3 Kinase

Synthesis and biological activity of new 2,4,6-trisubstituted triazines as potential phosphoinositide 3-kinase inhibitors

2020 ◽  
Vol 44 (7-8) ◽  
pp. 393-402
Author(s):  
Minhang Xin ◽  
Hui-Yan Wang ◽  
Hao Zhang ◽  
Ying Shen ◽  
San-Qi Zhang
Keyword(s):  
Biological Activity ◽  
Anticancer Drugs ◽  
Antiproliferative Activity ◽  
Kinase Inhibitors ◽  
Mammalian Target Of Rapamycin ◽  
Target Of Rapamycin ◽  
Hct 116 ◽  
Phosphoinositide 3 Kinase ◽  
New Anticancer Drugs ◽  
Mcf 7

Twenty-five novel 2,4,6-trisubstituted triazines were synthesized and biologically evaluated. Most of the compounds synthesized showed good antiproliferative activity against HCT-116 and MCF-7. Compounds B18 and B19 showed the best antiproliferative activity. Further study showed B18 and B19 inhibited four phosphoinositide 3-kinase isoforms and mammalian target of rapamycin with good potency. These results demonstrate that 2,4,6-trisubstituted triazines are potentially useful phosphoinositide 3-kinase inhibitors for the development of new anticancer drugs.

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