A novel class of inhibitors for steroid 5α-reductase:: Synthesis and evaluation of umbelliferone derivatives

A series of umbelliferone derivatives was prepared and their 5 alpha -reductase type 1 inhibitory activities were evaluated in cell culture systems. Our studies have identified a new series of potent 5 alpha -reductase type 1 inhibitors and provided the basis for further development for the treatment of human endocrine disorders associated,vith overproduction of DHT by 5 alpha -reductase type 1. The preliminary structure-activity relationship was described to elucidate the essential structural requirements. (C) 2001 Elsevier Science Ltd. All rights reserved.