Synthesis and Biological Evaluation of 3-Heterocyclyl-7,8,9,10-tetrahydro-(7,10-ethano)-1,2,4-triazolo[3,4-a]phthalazines and Analogues as Subtype-Selective Inverse Agonists for the GABAAα5 Benzodiazepine Binding Site

Leslie J. Street; Francine Sternfeld; Richard A. Jelley; Austin J. Reeve; Robert W. Carling; Kevin W. Moore; Ruth M. McKernan; Bindi Sohal; Susan Cook; Andrew Pike; Gerard R. Dawson; Frances A. Bromidge; Keith A. Wafford; Guy R. Seabrook; Sally A. Thompson; George Marshall; Goplan V. Pillai; José L. Castro; John R. Atack; Angus M. MacLeod

doi:10.1021/jm0407613

Synthesis and Biological Evaluation of 3-Heterocyclyl-7,8,9,10-tetrahydro-(7,10-ethano)-1,2,4-triazolo[3,4-a]phthalazines and Analogues as Subtype-Selective Inverse Agonists for the GABAAα5 Benzodiazepine Binding Site

Journal of Medicinal Chemistry ◽

10.1021/jm0407613 ◽

2004 ◽

Vol 47 (14) ◽

pp. 3642-3657 ◽

Cited By ~ 50

Author(s):

Leslie J. Street ◽

Francine Sternfeld ◽

Richard A. Jelley ◽

Austin J. Reeve ◽

Robert W. Carling ◽

...

Keyword(s):

Binding Site ◽

Biological Evaluation ◽

Inverse Agonists ◽

Benzodiazepine Binding ◽

Subtype Selective ◽

Synthesis And Biological Evaluation

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Faculty Opinions recommendation of Synthesis and biological evaluation of gamma-aminophosphonates as potent, subtype-selective sphingosine 1-phosphate receptor agonists and antagonists.

Faculty Opinions – Post-Publication Peer Review of the Biomedical Literature ◽

10.3410/f.1064759.517678 ◽

2007 ◽

Author(s):

Hugh Rosen

Keyword(s):

Biological Evaluation ◽

Receptor Agonists ◽

Sphingosine 1 Phosphate ◽

Subtype Selective ◽

Synthesis And Biological Evaluation ◽

Receptor Agonists And Antagonists

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Design, synthesis and biological evaluation of new carbazole-coumarin hybrids as dual binding site inhibitors of acetylcholinesterase

Journal of Molecular Structure ◽

10.1016/j.molstruc.2020.129784 ◽

2021 ◽

Vol 1229 ◽

pp. 129784

Author(s):

Meng-qiu Song ◽

Wei Min ◽

Jing Wang ◽

Xi-Xi Si ◽

Xiu-Jun Wang ◽

...

Keyword(s):

Binding Site ◽

Biological Evaluation ◽

Design Synthesis ◽

Synthesis And Biological Evaluation

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Design, Synthesis, and Biological Evaluation of Stable Colchicine-Binding Site Tubulin Inhibitors 6-Aryl-2-benzoyl-pyridines as Potential Anticancer Agents

Journal of Medicinal Chemistry ◽

10.1021/acs.jmedchem.1c00715 ◽

2021 ◽

Author(s):

Hao Chen ◽

Shanshan Deng ◽

Najah Albadari ◽

Mi-Kyung Yun ◽

Sicheng Zhang ◽

...

Keyword(s):

Binding Site ◽

Anticancer Agents ◽

Biological Evaluation ◽

Design Synthesis ◽

Tubulin Inhibitors ◽

Colchicine Binding Site ◽

Synthesis And Biological Evaluation

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Design, Synthesis, and Biological Evaluation of 7H-Thiazolo[3,2-b]-1,2,4-triazin-7-one Derivatives as Dual Binding Site Acetylcholinesterase Inhibitors

Heterocycles ◽

10.3987/com-18-12820 ◽

2013 ◽

Vol 87 (12) ◽

Author(s):

Chun Hu ◽

Si-Jie Liu ◽

Li-Bo Cui ◽

Hiu-Lan Xu ◽

Tie-Ying Wang ◽

...

Keyword(s):

Binding Site ◽

Acetylcholinesterase Inhibitors ◽

Biological Evaluation ◽

Design Synthesis ◽

Synthesis And Biological Evaluation

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Synthesis and biological evaluation of novel cyclopropyl derivatives as subtype-selective ligands for estrogen receptor

Journal of Pharmacy and Pharmacology ◽

10.1111/jphp.12908 ◽

2018 ◽

Vol 70 (7) ◽

pp. 910-918 ◽

Cited By ~ 2

Author(s):

Zunyuan Wang ◽

Yewei Yang ◽

Xiaoliang Zheng ◽

Tao Zhang ◽

Wenhai Huang ◽

...

Keyword(s):

Estrogen Receptor ◽

Biological Evaluation ◽

Selective Ligands ◽

Subtype Selective ◽

Synthesis And Biological Evaluation

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Design, Synthesis, and Biological Evaluation of Dual Binding Site Acetylcholinesterase Inhibitors: New Disease-Modifying Agents for Alzheimer's Disease

Journal of Medicinal Chemistry ◽

10.1021/jm0503289 ◽

2005 ◽

Vol 48 (23) ◽

pp. 7223-7233 ◽

Cited By ~ 143

Author(s):

Pilar Muñoz-Ruiz ◽

Laura Rubio ◽

Esther García-Palomero ◽

Isabel Dorronsoro ◽

María del Monte-Millán ◽

...

Keyword(s):

Alzheimer’S Disease ◽

Alzheimer's Disease ◽

Binding Site ◽

Acetylcholinesterase Inhibitors ◽

Biological Evaluation ◽

New Disease ◽

Design Synthesis ◽

Disease Modifying ◽

Disease Modifying Agents ◽

Synthesis And Biological Evaluation

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Design, synthesis and biological evaluation of resveratrol-cinnamoyl derivates as tubulin polymerization inhibitors targeting the colchicine binding site

Bioorganic Chemistry ◽

10.1016/j.bioorg.2019.103319 ◽

2019 ◽

Vol 93 ◽

pp. 103319 ◽

Cited By ~ 3

Author(s):

Yong Yin ◽

Bao-Ping Lian ◽

Yuan-Zheng Xia ◽

Yu-Ying Shao ◽

Ling-Yi Kong

Keyword(s):

Binding Site ◽

Biological Evaluation ◽

Tubulin Polymerization ◽

Design Synthesis ◽

Colchicine Binding Site ◽

Tubulin Polymerization Inhibitors ◽

Synthesis And Biological Evaluation

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Structure-Guided Design, Synthesis, and Biological Evaluation of (2-(1H-Indol-3-yl)-1H-imidazol-4-yl)(3,4,5-trimethoxyphenyl) Methanone (ABI-231) Analogues Targeting the Colchicine Binding Site in Tubulin

Journal of Medicinal Chemistry ◽

10.1021/acs.jmedchem.9b00706 ◽

2019 ◽

Vol 62 (14) ◽

pp. 6734-6750 ◽

Cited By ~ 8

Author(s):

Qinghui Wang ◽

Kinsie E. Arnst ◽

Yuxi Wang ◽

Gyanendra Kumar ◽

Dejian Ma ◽

...

Keyword(s):

Binding Site ◽

Biological Evaluation ◽

Design Synthesis ◽

Colchicine Binding Site ◽

Synthesis And Biological Evaluation

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Synthesis and biological evaluation of conformationally constrained sphingosine-1-phosphate analogs as subtype selective S1P receptor agonist/antagonist

10.18130/v3wg9m ◽

2008 ◽

Author(s):

Ran Zhu

Keyword(s):

Receptor Agonist ◽

Biological Evaluation ◽

Conformationally Constrained ◽

Sphingosine 1 Phosphate ◽

S1p Receptor ◽

Subtype Selective ◽

Synthesis And Biological Evaluation

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Synthesis and biological evaluation of 7H-thiazolo[3,2-b]-1,2,4-triazin-7-one derivatives as dual binding site acetylcholinesterase inhibitors

European Journal of Medicinal Chemistry ◽

10.1016/j.ejmech.2014.05.020 ◽

2014 ◽

Vol 81 ◽

pp. 237-244 ◽

Cited By ~ 19

Author(s):

Sijie Liu ◽

Ruofeng Shang ◽

Lanxiang Shi ◽

David Chi-Cheong Wan ◽

Huangquan Lin

Keyword(s):

Binding Site ◽

Acetylcholinesterase Inhibitors ◽

Biological Evaluation ◽

Synthesis And Biological Evaluation

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