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

Emily J. Faivre, Keith F. McDaniel, Daniel H. Albert, +31

Nature

Bd2 BromodomainMedicineNatural SciencesMolecular BiologyCancer Biology +7

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

Keith F. McDaniel, Le Wang, Todd Soltwedel, +29

Journal of Medicinal Chemistry

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

David A. DeGoey, John T. Randolph, Dachun Liu, +26

Journal of Medicinal Chemistry

Excellent PotencyMedicinal ChemistryHcv Ns5aMedicineAntiviral Drug Development +9

Mutations Conferring Resistance to a Hepatitis C Virus (HCV) RNA-Dependent RNA Polymerase Inhibitor Alone or in Combination with an HCV Serine Protease Inhibitor In Vitro

Hongmei Mo, Liangjun Lu, Ron Pithawalla, +12

Antimicrobial Agents and Chemotherapy

Viral ReplicationHepatitis C VirusViral HepatitisCompounds A-782759Antiviral Therapy +10

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

Mai H. Bui, Daniel H. Albert, Leiming Li, +21

Cancer Research

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

George S. Sheppard, Le Wang, Steven D. Fidanze, +20

Journal of Medicinal Chemistry

Nonsteroidal Selective Glucocorticoid Modulators:  the Effect of C-5 Alkyl Substitution on the Transcriptional Activation/Repression Profile of 2,5-Dihydro-10-methoxy-2,2,4-trimethyl-1H-[1]benzopyrano[3,4-f]quinolines

Steven W. Elmore, Michael J. Coghlan, David D. Anderson, +10

Journal of Medicinal Chemistry

C-5 Alkyl SubstitutionMedicinal ChemistryBioorganic ChemistryAllergyBiochemistry +13

Nonsteroidal Selective Glucocorticoid Modulators:  The Effect of C-10 Substitution on Receptor Selectivity and Functional Potency of 5-Allyl-2,5-dihydro-2,2,4-trimethyl-1H-[1]benzopyrano[3,4-f]quinolines

Philip R. Kym, Michael E. Kort, Michael J. Coghlan, +17

Journal of Medicinal Chemistry

Functional PotencyMedicinal ChemistryC-10 SubstitutionBiochemistryG Protein-coupled Receptor +12

A new class of potent non-imidazole H3 antagonists: 2-aminoethylbenzofurans

Marlon Cowart, John K. Pratt, Andrew O. Stewart, +3

Bioorganic & Medicinal Chemistry Letters

Medicinal ChemistryMedicinePharmacological AgentNew ClassPharmacotherapy +4

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

Le Wang, John K. Pratt, Todd Soltwedel, +30

Journal of Medicinal Chemistry