Development of small-molecule BRD4 degraders based on pyrrolopyridone derivative.

Bioorganic Chemistry(2020)

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摘要
•Several BRD4 degraders were designed and synthesized based on pyrrolopyridone derivative.•Degraders 32a and 32b effectively inhibited the proliferation of pancreatic cancer cell line BxPC3.•Degrader 32a potently degraded BRD4 protein and inhibited the expression of c-Myc in a time-dependent manner.•Degrader 32a induced the cell cycle arrest and apoptosis of BxPC3 cells.
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small-molecule
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