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Antiviral Drug Discovery for the Treatment of COVID-19 Infections

Viruses, 2022-05, Vol.14 (5), p.961

2022

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Selective inhibition of the BD2 bromodomain of BET proteins in prostate cancer

Nature (London), 2020-02, Vol.578 (7794), p.306-310

2020

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Discovery of N‑Ethyl-4-[2-(4-fluoro-2,6-dimethyl-phenoxy)-5-(1-hydroxy-1-methyl-ethyl)phenyl]-6-methyl-7-oxo‑1H‑pyrrolo[2,3‑c]pyridine-2-carboxamide (ABBV-744), a BET Bromodomain Inhibitor with Selectivity for the Second Bromodomain

Journal of medicinal chemistry, 2020-05, Vol.63 (10), p.5585-5623

2020

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Exploitation of Castration-Resistant Prostate Cancer Transcription Factor Dependencies by the Novel BET Inhibitor ABBV-075

Molecular cancer research, 2017-01, Vol.15 (1), p.35-44

2017

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Discovery of N -Ethyl-4-[2-(4-fluoro-2,6-dimethyl-phenoxy)-5-(1-hydroxy-1-methyl-ethyl)phenyl]-6-methyl-7-oxo-1 H -pyrrolo[2,3- c ]pyridine-2-carboxamide (ABBV-744), a BET Bromodomain Inhibitor with Selectivity for the Second Bromodomain

Journal of medicinal chemistry, 2020-05, Vol.63 (10), p.5585-5623

2020

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HEXIM1 as a Robust Pharmacodynamic Marker for Monitoring Target Engagement of BET Family Bromodomain Inhibitors in Tumors and Surrogate Tissues

Molecular cancer therapeutics, 2017-02, Vol.16 (2), p.388-396

2017

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Preclinical Characterization of BET Family Bromodomain Inhibitor ABBV-075 Suggests Combination Therapeutic Strategies

Cancer research (Chicago, Ill.), 2017-06, Vol.77 (11), p.2976-2989

2017

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Vulnerability of Small-Cell Lung Cancer to Apoptosis Induced by the Combination of BET Bromodomain Proteins and BCL2 Inhibitors

Molecular cancer therapeutics, 2017-08, Vol.16 (8), p.1511-1520

2017

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Discovery of a Potent Chloroacetamide GPX4 Inhibitor with Bioavailability to Enable Target Engagement in Mice, a Potential Tool Compound for Inducing Ferroptosis In Vivo

Journal of medicinal chemistry, 2023-03, Vol.66 (6), p.3852-3865

2023

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Selective Inhibition of the Second Bromodomain of BET Family Proteins Results in Robust Antitumor Activity in Preclinical Models of Acute Myeloid Leukemia

Molecular cancer therapeutics, 2021-10, Vol.20 (10), p.1809-1819

2021

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Highlights of the Structure–Activity Relationships of Benzimidazole Linked Pyrrolidines Leading to the Discovery of the Hepatitis C Virus NS5A Inhibitor Pibrentasvir (ABT-530)

Journal of medicinal chemistry, 2018-05, Vol.61 (9), p.4052-4066

2018

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Discovery of ABT-267, a Pan-Genotypic Inhibitor of HCV NS5A

Journal of medicinal chemistry, 2014-03, Vol.57 (5), p.2047-2057

2014

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Abstract DDT01-05: ABBV-744: A first-in-class highly BDII-selective BET bromodomain inhibitor

Cancer research (Chicago, Ill.), 2018-07, Vol.78 (13_Supplement), p.DDT01-05-DDT01-05

Kati, Warren

2018

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Co-clinical Modeling of the Activity of the BET Inhibitor Mivebresib (ABBV-075) in AML

In vivo (Athens), 2022-07, Vol.36 (4), p.1615-1627

2022

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Discovery and optimization of novel constrained pyrrolopyridone BET family inhibitors

Bioorganic & medicinal chemistry letters, 2018-06, Vol.28 (10), p.1804-1810

2018

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Synthesis and Biological Characterization of Aryl Uracil Inhibitors of Hepatitis C Virus NS5B Polymerase: Discovery of ABT-072, a trans-Stilbene Analog with Good Oral Bioavailability

Journal of medicinal chemistry, 2018-02, Vol.61 (3), p.1153-1163

2018

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Biomarkers for the clinical development of antiviral therapies

Cytometry. Part B, Clinical cytometry, 2021-01, Vol.100 (1), p.19-32

2021

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Methylpyrrole inhibitors of BET bromodomains

Bioorganic & medicinal chemistry letters, 2017-05, Vol.27 (10), p.2225-2233

2017

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Relative Replication Capacity and Selective Advantage Profiles of Protease Inhibitor-Resistant Hepatitis C Virus (HCV) NS3 Protease Mutants in the HCV Genotype 1b Replicon System

Antimicrobial Agents and Chemotherapy, 2008-03, Vol.52 (3), p.1101-1110

2008

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Identification of aryl dihydrouracil derivatives as palm initiation site inhibitors of HCV NS5B polymerase

Bioorganic & medicinal chemistry letters, 2012-06, Vol.22 (11), p.3747-3750

2012

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Discovery of fluorobenzimidazole HCV NS5A inhibitors

Bioorganic & medicinal chemistry letters, 2016-11, Vol.26 (22), p.5462-5467

2016

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Mechanism of Inhibition of HIV-1 Reverse Transcriptase by Nonnucleoside Inhibitors

Science (American Association for the Advancement of Science), 1995-02, Vol.267 (5200), p.988-993

1995

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Mechanistic Study of HCV Polymerase Inhibitors at Individual Steps of the Polymerization Reaction

Biochemistry (Easton), 2006-09, Vol.45 (38), p.11312-11323

2006

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Antiviral Drug Discovery for the Treatment of COVID-19 Infections

Selective inhibition of the BD2 bromodomain of BET proteins in prostate cancer

Discovery of N‑Ethyl-4-[2-(4-fluoro-2,6-dimethyl-phenoxy)-5-(1-hydroxy-1-methyl-ethyl)phenyl]-6-methyl-7-oxo‑1H‑pyrrolo[2,3‑c]pyridine-2-carboxamide (ABBV-744), a BET Bromodomain Inhibitor with Selectivity for the Second Bromodomain

Exploitation of Castration-Resistant Prostate Cancer Transcription Factor Dependencies by the Novel BET Inhibitor ABBV-075

Discovery of N -Ethyl-4-[2-(4-fluoro-2,6-dimethyl-phenoxy)-5-(1-hydroxy-1-methyl-ethyl)phenyl]-6-methyl-7-oxo-1 H -pyrrolo[2,3- c ]pyridine-2-carboxamide (ABBV-744), a BET Bromodomain Inhibitor with Selectivity for the Second Bromodomain

HEXIM1 as a Robust Pharmacodynamic Marker for Monitoring Target Engagement of BET Family Bromodomain Inhibitors in Tumors and Surrogate Tissues

Preclinical Characterization of BET Family Bromodomain Inhibitor ABBV-075 Suggests Combination Therapeutic Strategies

Discovery of N‑(4-(2,4-Difluorophenoxy)-3-(6-methyl-7-oxo-6,7-dihydro‑1H‑pyrrolo[2,3‑c]pyridin-4-yl)phenyl)ethanesulfonamide (ABBV-075/Mivebresib), a Potent and Orally Available Bromodomain and Extraterminal Domain (BET) Family Bromodomain Inhibitor

Vulnerability of Small-Cell Lung Cancer to Apoptosis Induced by the Combination of BET Bromodomain Proteins and BCL2 Inhibitors

Discovery of a Potent Chloroacetamide GPX4 Inhibitor with Bioavailability to Enable Target Engagement in Mice, a Potential Tool Compound for Inducing Ferroptosis In Vivo

Selective Inhibition of the Second Bromodomain of BET Family Proteins Results in Robust Antitumor Activity in Preclinical Models of Acute Myeloid Leukemia

Highlights of the Structure–Activity Relationships of Benzimidazole Linked Pyrrolidines Leading to the Discovery of the Hepatitis C Virus NS5A Inhibitor Pibrentasvir (ABT-530)

Fragment-Based, Structure-Enabled Discovery of Novel Pyridones and Pyridone Macrocycles as Potent Bromodomain and Extra-Terminal Domain (BET) Family Bromodomain Inhibitors

Discovery of ABT-267, a Pan-Genotypic Inhibitor of HCV NS5A

Abstract DDT01-05: ABBV-744: A first-in-class highly BDII-selective BET bromodomain inhibitor

Co-clinical Modeling of the Activity of the BET Inhibitor Mivebresib (ABBV-075) in AML

Discovery and optimization of novel constrained pyrrolopyridone BET family inhibitors

Synthesis and Biological Characterization of Aryl Uracil Inhibitors of Hepatitis C Virus NS5B Polymerase: Discovery of ABT-072, a trans-Stilbene Analog with Good Oral Bioavailability

Biomarkers for the clinical development of antiviral therapies

Methylpyrrole inhibitors of BET bromodomains

Relative Replication Capacity and Selective Advantage Profiles of Protease Inhibitor-Resistant Hepatitis C Virus (HCV) NS3 Protease Mutants in the HCV Genotype 1b Replicon System

Identification of aryl dihydrouracil derivatives as palm initiation site inhibitors of HCV NS5B polymerase

Discovery of fluorobenzimidazole HCV NS5A inhibitors

Mechanism of Inhibition of HIV-1 Reverse Transcriptase by Nonnucleoside Inhibitors

Mechanistic Study of HCV Polymerase Inhibitors at Individual Steps of the Polymerization Reaction

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