A Phenotypic Screen Identifies a Compound Series That Induces Differentiation of Acute Myeloid Leukemia Cells <i>In Vitro</i> and Shows Antitumor Effe...
Basic Information
ID: ALA4840350
Journal: J Med Chem
Title: A Phenotypic Screen Identifies a Compound Series That Induces Differentiation of Acute Myeloid Leukemia Cells In Vitro and Shows Antitumor Effects In Vivo.
Authors: Josa-Culleré L, Madden KS, Cogswell TJ, Jackson TR, Carter TS, Zhang D, Trevitt G, Davies SG, Vyas P, Wynne GM, Milne TA, Russell AJ.
Abstract: Induction of differentiation is a promising therapeutic strategy against acute myeloid leukemia. However, current differentiation therapies are effective only to specific patient populations. To identify novel differentiation agents with wider efficacy, we developed a phenotypic high-throughput screen with a range of genetically diverse cell lines. From the resulting hits, one chemical scaffold was optimized in terms of activity and physicochemical properties to yield OXS007417, a proof-of-concept tool compound, which was also able to decrease tumor volume in a murine in vivo xenograft model.
CiteXplore: 34672555
DOI: 10.1021/acs.jmedchem.1c00574
Patent ID: ┄