Phospshoinositide 3-Kinase (PI3K)/Mammalian Target of Rapamycin (mTOR) Dual Inhibitors: Discovery and Structure–Activity Relationships of a Series of Quinoline and Quinoxaline Derivatives

2011 ◽  
Vol 54 (13) ◽  
pp. 4735-4751 ◽  
Author(s):  
Nobuko Nishimura ◽  
Aaron Siegmund ◽  
Longbin Liu ◽  
Kevin Yang ◽  
Marian C. Bryan ◽  
...  
Keyword(s):  
Mammalian Target Of Rapamycin ◽  
Target Of Rapamycin ◽  
Structure Activity Relationships ◽  
Structure Activity ◽  
Quinoxaline Derivatives ◽  
Dual Inhibitors

scholarly journals Structure–Activity Relationships and in Vivo Evaluation of Quinoxaline Derivatives for PET Imaging of β-Amyloid Plaques

2013 ◽  
Vol 4 (7) ◽  
pp. 596-600 ◽  
Author(s):  
Masashi Yoshimura ◽  
Masahiro Ono ◽  
Kenji Matsumura ◽  
Hiroyuki Watanabe ◽  
Hiroyuki Kimura ◽  
...  
Keyword(s):  
Pet Imaging ◽  
Amyloid Plaques ◽  
In Vivo Evaluation ◽  
Structure Activity Relationships ◽  
Structure Activity ◽  
Quinoxaline Derivatives ◽  
Β Amyloid

Syntheses and Structure−Activity Relationships of 5,6,7,8-Tetrahydro-5,5,8,8-tetramethyl-2-quinoxaline Derivatives with Retinoic Acid Receptor α Agonistic Activity

2000 ◽  
Vol 43 (3) ◽  
pp. 409-419 ◽  
Author(s):  
Kouichi Kikuchi ◽  
Shigeki Hibi ◽  
Hiroyuki Yoshimura ◽  
Naoki Tokuhara ◽  
Kenji Tai ◽  
...  
Keyword(s):  
Retinoic Acid ◽  
Retinoic Acid Receptor ◽  
Acid Receptor ◽  
Structure Activity Relationships ◽  
Structure Activity ◽  
Quinoxaline Derivatives ◽  
Agonistic Activity ◽  
Retinoic Acid Receptor Α

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

Novel Dual Inhibitors of 5-Lipoxygenase and Thromboxane A2 Synthetase: Synthesis and Structure-Activity Relationships of 3-Pyridylmethyl-Substituted 2-Amino-6-hydroxybenzothiazole Derivatives

1994 ◽  
Vol 37 (19) ◽  
pp. 3062-3070 ◽  
Author(s):  
Shigeki Hibi ◽  
Yasushi Okamoto ◽  
Katsuya Tagami ◽  
Hirotoshi Numata ◽  
Naoki Kobayashi ◽  
...  
Keyword(s):  
Thromboxane A2 ◽  
Structure Activity Relationships ◽  
Structure Activity ◽  
Dual Inhibitors

scholarly journals 4EBP1/c-MYC/PUMA and NF-κB/EGR1/BIM pathways underlie cytotoxicity of mTOR dual inhibitors in malignant lymphoid cells

Blood ◽  
2016 ◽  
Vol 127 (22) ◽  
pp. 2711-2722 ◽  
Author(s):  
Seongseok Yun ◽  
Nicole D. Vincelette ◽  
Katherine L. B. Knorr ◽  
Luciana L. Almada ◽  
Paula A. Schneider ◽  
...  
Keyword(s):  
Acute Lymphocytic Leukemia ◽  
Mammalian Target Of Rapamycin ◽  
Lymphocytic Leukemia ◽  
Lymphoid Cells ◽  
Target Of Rapamycin ◽  
Leukemia Cells ◽  
Key Points ◽  
Dual Inhibitors

Key Points Agents that inhibit both complexes containing the mammalian target of rapamycin are particularly toxic to acute lymphocytic leukemia cells. This killing reflects engagement of a 4EBP1/c-MYC/PUMA axis downstream of mTORC1 and an NF-κB/EGR1/BIM axis downstream of mTORC2.

Synthesis and structure–activity relationships of PI3K/mTOR dual inhibitors from a series of 2-amino-4-methylpyrido[2,3- d ]pyrimidine derivatives

2014 ◽  
Vol 24 (18) ◽  
pp. 4538-4541 ◽  
Author(s):  
Fangbin Han ◽  
Songwen Lin ◽  
Peng Liu ◽  
Jing Tao ◽  
Chongqin Yi ◽  
...  
Keyword(s):  
Pyrimidine Derivatives ◽  
Structure Activity Relationships ◽  
Structure Activity ◽  
Dual Inhibitors

scholarly journals Synthesis, Biological Evaluation and Structure-Activity Relationships of New Quinoxaline Derivatives as Anti-Plasmodium falciparum Agents

Molecules ◽  
2014 ◽  
Vol 19 (2) ◽  
pp. 2166-2180 ◽  
Author(s):  
Ana Gil ◽  
Adriana Pabón ◽  
Silvia Galiano ◽  
Asunción Burguete ◽  
Silvia Pérez-Silanes ◽  
...  
Keyword(s):  
Plasmodium Falciparum ◽  
Biological Evaluation ◽  
Structure Activity Relationships ◽  
Structure Activity ◽  
Quinoxaline Derivatives
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