Discovery and Structure-Based Optimization of Potent and Selective WD Repeat Domain 5 (WDR5) Inhibitors Containing a Dihydroisoquinolinone Bicyclic Core.

Tian J, Teuscher KB, Aho ER, Alvarado JR, Mills JJ, Meyers KM, Gogliotti RD, Han C, Macdonald JD, Sai J, Shaw JG, Sensintaffar JL, Zhao B, Rietz TA, Thomas LR, Payne WG, Moore WJ, Stott GM, Kondo J, Inoue M, Coffey RJ, Tansey WP, Stauffer SR, Lee T, Fesik SW
J Med Chem. 2020 63 (2): 656-675

PMID: 31858797 · PMCID: PMC6986559 · DOI:10.1021/acs.jmedchem.9b01608

MeSH Terms (16)

Antineoplastic Agents Bridged Bicyclo Compounds, Heterocyclic Cell Cycle Cell Line, Tumor Cell Proliferation Chromatin Crystallography, X-Ray Drug Design Drug Discovery Epigenetic Repression Genes, myc Humans Intracellular Signaling Peptides and Proteins Quinolones Structure-Activity Relationship WD40 Repeats

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