A novel class of inhibitors for steroid 5α-Reductase: synthesis and evaluation of umbelliferone derivatives

A series of umbelliferone derivatives was prepared and their 5α-reductase type 1 inhibitory activities were evaluated in cell culture systems. Our studies have identified a new series of potent 5α-reductase type 1 inhibitors and provided the basis for further development for the treatment of human endocrine disorders associated with overproduction of DHT by 5α-reductase type 1. The preliminary structure–activity relationship was described to elucidate the essential structural requirements.