Discovery of Potent Myeloid Cell Leukemia-1 (Mcl-1) Inhibitors That Demonstrate in Vivo Activity in Mouse Xenograft Models of Human Cancer.

Lee T, Christov PP, Shaw S, Tarr JC, Zhao B, Veerasamy N, Jeon KO, Mills JJ, Bian Z, Sensintaffar JL, Arnold AL, Fogarty SA, Perry E, Ramsey HE, Cook RS, Hollingshead M, Davis Millin M, Lee KM, Koss B, Budhraja A, Opferman JT, Kim K, Arteaga CL, Moore WJ, Olejniczak ET, Savona MR, Fesik SW
J Med Chem. 2019 62 (8): 3971-3988

PMID: 30929420 · DOI:10.1021/acs.jmedchem.8b01991

MeSH Terms (20)

Animals Antineoplastic Agents Azepines Binding Sites Cell Line, Tumor Cell Survival Crystallography, X-Ray Drug Evaluation, Preclinical Female Humans Mice Mice, Inbred NOD Mice, SCID Molecular Dynamics Simulation Myeloid Cell Leukemia Sequence 1 Protein Neoplasms Protein Structure, Tertiary Small Molecule Libraries Structure-Activity Relationship Xenograft Model Antitumor Assays

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