Small-Molecule Dual PLK1 and BRD4 Inhibitors are Active Against Preclinical Models of Pediatric Solid Tumors
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DOI: 10.1016/j.tranon.2019.09.013
Abstract: Simultaneous inhibition of multiple molecular targets is an established strategy to improve the continuance of clinical response to therapy. Here, we screened 49 molecules with dual nanomolar inhibitory activity against BRD4 and PLK1, best classified… read more here.
Keywords: plk1; plk1 brd4; dual plk1; small molecule ... See more keywords
Design, synthesis and biological evaluation of novel pteridinone derivatives as potent dual inhibitors of PLK1 and BRD4
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DOI: 10.1039/d0nj03477k
Abstract: To develop novel simultaneous inhibition of PLK1 and BRD4 bromodomain by a single molecule, three series of novel pteridinone derivatives were designed, synthesized and evaluated for their biological activity. Most compounds exhibited moderate to excellent… read more here.
Keywords: design synthesis; cell lines; plk1 brd4; pteridinone derivatives ... See more keywords