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 a Potent and Selective BCL-X _L Inhibitor with <i>in Vivo</i> Activity

Zhi‐Fu Tao, Lisa Hasvold, Le Wang, +36

ACS Medicinal Chemistry Letters

Palladium(II)-Catalyzed Cyclization of Olefinic Tosylamides

Richard C. Larock, Timothy R. Hightower, Lisa Hasvold, +1

The Journal of Organic Chemistry

EngineeringHeterocyclicAlkene MetathesisDonut IconAltmetric Attention Score +7

Structure-Guided Design of a Series of MCL-1 Inhibitors with High Affinity and Selectivity

Milan Bruncko, Le Wang, George S. Sheppard, +26

Journal of Medicinal Chemistry

Drug TargetMcl-1 InhibitorsHigh ThroughputExcellent SelectivityCancer Biology +21

Therapeutic Implications for the Induced Levels of Chk1 in Myc-Expressing Cancer Cells

Andreas Höglund, Lisa M. Nilsson, Somsundar Veppil Muralidharan, +6

Clinical Cancer Research

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

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

Discovery of 3<i>H</i>-Benzo[4,5]thieno[3,2-<i>d</i>]pyrimidin-4-ones as Potent, Highly Selective, and Orally Bioavailable Inhibitors of the Human Protooncogene Proviral Insertion Site in Moloney Murine Leukemia Virus (PIM) Kinases

Zhi‐Fu Tao, Lisa Hasvold, Edward K. Han, +13

Journal of Medicinal Chemistry

Synthesis and Structure−Activity Relationships of 2-Pyridones:  A Novel Series of Potent DNA Gyrase Inhibitors as Antibacterial Agents

Qun Li, Daniel T. W. Chu, Akiyo Claiborne, +27

Journal of Medicinal Chemistry

Antibacterial AgentsAntibiotic AdjuvantAntimicrobial ChemotherapyChemical BiologyPharmaceutical Chemistry +19