Design, Synthesis, and Biological Evaluation of Androgen Receptor Degrading and Antagonizing Bifunctional Steroidal Analogs for the Treatment of Advanced Prostate Cancer

In vitro, 67-b exhibited excellent antiproliferative activity and potent androgen receptor (AR) degradation activity in different PCa cells, as well as outstanding antagonistic activity against wild-type and mutant ARs.
[Journal of Medicinal Chemistry]
AbstractGraphical Abstract