AZD9496: An Oral Estrogen Receptor Inhibitor That Blocks the Growth of ER-Positive and <i>ESR1</i> -Mutant Breast Tumors in Preclinical Models

Hazel M. Weir, Robert H. Bradbury, Mandy Lawson, +26

Cancer Research

Optimization of a Novel Binding Motif to (<i>E</i>)-3-(3,5-Difluoro-4-((1<i>R</i>,3<i>R</i>)-2-(2-fluoro-2-methylpropyl)-3-methyl-2,3,4,9-tetrahydro-1<i>H</i>-pyrido[3,4-<i>b</i>]indol-1-yl)phenyl)acrylic Acid (AZD9496), a Potent and Orally Bioavailable Selective Estrogen Receptor Downregulator and Antagonist

Chris De Savi, Robert H. Bradbury, Alfred A. Rabow, +23

Journal of Medicinal Chemistry

Pharmaceutical SciencePharmacotherapyPositive Breast CancerPharmaceutical ChemistryMolecular Pharmacology +16

AZD5153: A Novel Bivalent BET Bromodomain Inhibitor Highly Active against Hematologic Malignancies

Garrett W. Rhyasen, Maureen M. Hattersley, Yi Yao, +26

Molecular Cancer Therapeutics

Azd5153 ExposurePathologyPharmacotherapyTumor BiologyMyeloid Neoplasia +15

Mining the National Cancer Institute's Tumor-Screening Database:  Identification of Compounds with Similar Cellular Activities

Alfred A. Rabow, Robert H. Shoemaker, Edward A. Sausville, +1

Journal of Medicinal Chemistry

Drug TargetHit IdentificationSimilar Cellular ActivitiesTumor BiologyCompound Selectivity +18

Potent and selective bivalent inhibitors of BET bromodomains

Michael J. Waring, Huawei Chen, Alfred A. Rabow, +27

Nature Chemical Biology

Medicinal ChemistrySelective Bivalent InhibitorsMedicineDrug DevelopmentPharmacology +1

Molecular classification of cancer: unsupervised self-organizing map analysis of gene expression microarray data.

David G. Covell, Anders Wallqvist, Alfred A. Rabow, +1

PubMed

EngineeringPathologyGene Expression FingerprintGene Expression ProfilingTumor Biology +16

Optimization of a Series of Bivalent Triazolopyridazine Based Bromodomain and Extraterminal Inhibitors: The Discovery of (3<i>R</i>)-4-[2-[4-[1-(3-Methoxy-[1,2,4]triazolo[4,3-<i>b</i>]pyridazin-6-yl)-4-piperidyl]phenoxy]ethyl]-1,3-dimethyl-piperazin-2-one (AZD5153)

Robert H. Bradbury, Rowena Callis, Gregory R. Carr, +21

Journal of Medicinal Chemistry

Pharmaceutical ScienceChemoprevention StrategyOrganic ChemistryPharmacotherapyPharmaceutical Chemistry +19

AZD3514: A Small Molecule That Modulates Androgen Receptor Signaling and Function <i>In Vitro</i> and <i>In Vivo</i>

Sarah A. Loddick, Sarah J. Ross, Andrew Thomason, +22

Molecular Cancer Therapeutics

Improved genetic algorithm for the protein folding problem by use of a Cartesian combination operator

Alfred A. Rabow, Harold A. Scheraga

Protein Science

Establishing connections between microarray expression data and chemotherapeutic cancer pharmacology.

Anders Wallqvist, Alfred A. Rabow, Robert H. Shoemaker, +2

PubMed

Cancer BiologyGene Expression ProfilingTumor BiologyK Gene ExpressionsTumor Heterogeneity +17