Discovery of novel dual-target CDK12/PARP1 inhibitors for the treatment of triple-negative breast cancer.
The dual-target CDK12/PARP1 inhibitor 20b developed herein represents a novel lead molecule for TNBC drug development and exhibited markedly superior antiproliferative effects compared with single-target inhibitors and effectively reduced pSer2-CTD and PAR levels in TNBC cells.