Discovery of a new class of PROTAC BRD4 degraders based on a dihydroquinazolinone derivative and lenalidomide/pomalidomide.
Bioorganic & Medicinal Chemistry(2020)
摘要
•A new class of BRD4 degraders were designed and synthesized.•All synthesized compounds were evaluated for their ability to inhibit BRD4.•Cell proliferation inhibition was assessed in the HL-60, Raji and THP-1 cell lines.•Compound 21 effectively induced the degradation of BRD4 protein and suppression of c-Myc expression.
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关键词
BRD4 degraders,PROTAC,Protein degradation,Dihydroquinazolinone
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