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Structure-Based Optimization of Potent, Selective, and Orally Bioavailable CDK8 Inhibitors Discovered by High-Throughput Screening

Journal of medicinal chemistry, 2016-10, Vol.59 (20), p.9337-9349

2016

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A selective chemical probe for exploring the role of CDK8 and CDK19 in human disease

Nature chemical biology, 2015-10, Vol.11 (12), p.973-980

2015

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Discovery of Potent, Selective, and Orally Bioavailable Small-Molecule Modulators of the Mediator Complex-Associated Kinases CDK8 and CDK19

Journal of medicinal chemistry, 2016-02, Vol.59 (3), p.1078-1101

2016

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Discovery of Potent, Orally Bioavailable, Small-Molecule Inhibitors of WNT Signaling from a Cell-Based Pathway Screen

Journal of medicinal chemistry, 2015-02, Vol.58 (4), p.1717-1735

2015

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Discovery of potent and selective CDK8 inhibitors from an HSP90 pharmacophore

Bioorganic & medicinal chemistry letters, 2016-03, Vol.26 (5), p.1443-1451

2016

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Large-Scale Assessment of Binding Free Energy Calculations in Active Drug Discovery Projects

Journal of chemical information and modeling, 2020-11, Vol.60 (11), p.5457-5474

2020

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Dual A2A/A2B Adenosine Receptor Antagonist M1069 Counteracts Immunosuppressive Mechanisms of Adenosine and Reduces Tumor Growth In Vivo

Molecular cancer therapeutics, 2024-11, Vol.23 (11), p.1517-1529

2024

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A selective chemical probe for exploring the role of CDK8 and CDK19 in human disease

Nature chemical biology, 2015-12, Vol.11 (12), p.973

2015

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Abstract 3500: Highly potent and selective ATM kinase inhibitor M4076: A clinical candidate drug with strong anti-tumor activity in combination therapies

Cancer research (Chicago, Ill.), 2019-07, Vol.79 (13_Supplement), p.3500-3500

2019

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Abstract A187: Exploring isoform-dependent functions of the mediator kinases in colorectal cancer

Molecular cancer therapeutics, 2018-01, Vol.17 (1_Supplement), p.A187-A187

2018

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The discovery and optimization of hexahydro-2H-pyrano[3,2-c]quinolines (HHPQs) as potent and selective inhibitors of the mitotic kinesin-5

Bioorganic & medicinal chemistry letters, 2010-03, Vol.20 (5), p.1491-1495

2010

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Enantioselective Synthesis of Tertiary Homoallylic Alcohols via Diastereoselective Addition of Allylsilanes to Ketones

Journal of the American Chemical Society, 1995-05, Vol.117 (21), p.5851-5852

1995

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2,8-Disubstituted-1,6-Naphthyridines and 4,6-Disubstituted-Isoquinolines with Potent, Selective Affinity for CDK8/19

ACS medicinal chemistry letters, 2016-06, Vol.7 (6), p.573-578

2016

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Abstract 3869: Phosphoproteomic-based identification of CDK8/CDK19 substrates in colorectal cancer

Cancer research (Chicago, Ill.), 2016-07, Vol.76 (14_Supplement), p.3869-3869

2016

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Abstract 3499: M1069 as dual A2A/A2B adenosine receptor antagonist counteracts immune-suppressive mechanisms of adenosine and reduces tumor growth in vivo

Cancer research (Chicago, Ill.), 2022-06, Vol.82 (12_Supplement), p.3499-3499

2022

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Abstract 129: Assessing the mechanism and therapeutic potential of modulators of the human mediator complex-associated protein kinases CDK8 and CDK19

Cancer research (Chicago, Ill.), 2017-07, Vol.77 (13_Supplement), p.129-129

2017

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Abstract PR02: Identification of a potent and selective chemical probe for exploring the role of CDK8/19 in cancer biology

Molecular cancer therapeutics, 2015-12, Vol.14 (12_Supplement_2), p.PR02-PR02

2015

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Abstract 4355: Elucidation of the different roles of CDK8 and CDK19 in colorectal cancer (CRC) using CRISPR gene editing technology

Cancer research (Chicago, Ill.), 2016-07, Vol.76 (14_Supplement), p.4355-4355

2016

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Abstract 3025: Discovery of preclinical development candidate inhibitors of the mediator complex-associated kinases CDK8 and CDK19 and evaluation of their therapeutic potential

Cancer research (Chicago, Ill.), 2016-07, Vol.76 (14_Supplement), p.3025-3025

2016

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Dual 5-HT1A agonists and 5-HT re-uptake inhibitors by combination of indole-butyl-amine and chromenonyl-piperazine structural elements in a single molecular entity

Bioorganic & medicinal chemistry, 2004-09, Vol.12 (18), p.4843-4852

2004

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The discovery and optimization of hexahydro-2 H-pyrano[3,2- c]quinolines (HHPQs) as potent and selective inhibitors of the mitotic kinesin-5

Bioorganic & medicinal chemistry letters, 2010, Vol.20 (5), p.1491-1495

2010

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Development of Polymer-Supported Benzotriazole as a Novel Traceless Linker for Solid-Phase Organic Synthesis(1)

Journal of organic chemistry, 1999-06, Vol.64 (13), p.4972-4975

1999

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Development of Polymer-Supported Benzotriazole as a Novel Traceless Linker for Solid-Phase Organic Synthesis1

Journal of organic chemistry, 1999-06, Vol.64 (13), p.4972-4975

1999

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Development of Polymer-Supported Benzotriazole as a Novel Traceless Linker for Solid-Phase Organic Synthesis 1

Journal of organic chemistry, 1999-06, Vol.64 (13), p.4972-4975

1999

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Cyclin-Dependent Kinase 8 - Antagonists & Inhibitors
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Structure-Based Optimization of Potent, Selective, and Orally Bioavailable CDK8 Inhibitors Discovered by High-Throughput Screening

Assessing the mechanism and therapeutic potential of modulators of the human Mediator complex-associated protein kinases

A selective chemical probe for exploring the role of CDK8 and CDK19 in human disease

Discovery of Potent, Selective, and Orally Bioavailable Small-Molecule Modulators of the Mediator Complex-Associated Kinases CDK8 and CDK19

Discovery of Potent, Orally Bioavailable, Small-Molecule Inhibitors of WNT Signaling from a Cell-Based Pathway Screen

Discovery of potent and selective CDK8 inhibitors from an HSP90 pharmacophore

Large-Scale Assessment of Binding Free Energy Calculations in Active Drug Discovery Projects

Dual A2A/A2B Adenosine Receptor Antagonist M1069 Counteracts Immunosuppressive Mechanisms of Adenosine and Reduces Tumor Growth In Vivo

A selective chemical probe for exploring the role of CDK8 and CDK19 in human disease

Abstract 3500: Highly potent and selective ATM kinase inhibitor M4076: A clinical candidate drug with strong anti-tumor activity in combination therapies

Abstract A187: Exploring isoform-dependent functions of the mediator kinases in colorectal cancer

The discovery and optimization of hexahydro-2H-pyrano[3,2-c]quinolines (HHPQs) as potent and selective inhibitors of the mitotic kinesin-5

Enantioselective Synthesis of Tertiary Homoallylic Alcohols via Diastereoselective Addition of Allylsilanes to Ketones

2,8-Disubstituted-1,6-Naphthyridines and 4,6-Disubstituted-Isoquinolines with Potent, Selective Affinity for CDK8/19

Abstract 3869: Phosphoproteomic-based identification of CDK8/CDK19 substrates in colorectal cancer

Abstract 3499: M1069 as dual A2A/A2B adenosine receptor antagonist counteracts immune-suppressive mechanisms of adenosine and reduces tumor growth in vivo

Abstract 129: Assessing the mechanism and therapeutic potential of modulators of the human mediator complex-associated protein kinases CDK8 and CDK19

Abstract PR02: Identification of a potent and selective chemical probe for exploring the role of CDK8/19 in cancer biology

Abstract 4355: Elucidation of the different roles of CDK8 and CDK19 in colorectal cancer (CRC) using CRISPR gene editing technology

Abstract 3025: Discovery of preclinical development candidate inhibitors of the mediator complex-associated kinases CDK8 and CDK19 and evaluation of their therapeutic potential

Dual 5-HT1A agonists and 5-HT re-uptake inhibitors by combination of indole-butyl-amine and chromenonyl-piperazine structural elements in a single molecular entity

The discovery and optimization of hexahydro-2 H-pyrano[3,2- c]quinolines (HHPQs) as potent and selective inhibitors of the mitotic kinesin-5

Development of Polymer-Supported Benzotriazole as a Novel Traceless Linker for Solid-Phase Organic Synthesis(1)

Development of Polymer-Supported Benzotriazole as a Novel Traceless Linker for Solid-Phase Organic Synthesis1

Development of Polymer-Supported Benzotriazole as a Novel Traceless Linker for Solid-Phase Organic Synthesis 1

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