A novel class of inhibitors for steroid 5alpha-reductase: synthesis and evaluation of umbelliferone derivatives.
A series of umbelliferone derivatives was prepared and their 5alpha-reductase type 1 inhibitory activities were evaluated in cell culture systems. Our studies have identified a new series of potent 5alpha-reductase type 1 inhibitors and provided the basis for further development for the treatment of human endocrine disorders associated with overproduction of DHT by 5alpha-reductase type 1. The preliminary structure-activity relationship was described to elucidate the essential structural requirements.
Fan
G
G
Natural Products Research Institute, Seoul National University, 28 Yungun, Jongro, Seoul 110-460, South Korea.
Mar
W
W
Park
M K
MK
Choi
E W
EW
Kim
K
K
Kim
S
S
D058891:5-alpha Reductase Inhibitors; D003374:Coumarins / Q000737:chemistry* / Q000494:pharmacology*; D015195:Drug Design; D004353:Drug Evaluation, Preclinical; D004791:Enzyme Inhibitors / Q000737:chemistry* / Q000494:pharmacology*; D006801:Humans; D020128:Inhibitory Concentration 50; D008297:Male; D011471:Prostatic Neoplasms / Q000188:drug therapy; D013329:Structure-Activity Relationship; D014407:Tumor Cells, Cultured; D014468:Umbelliferones / Q000737:chemistry*
D058891:5-alpha Reductase Inhibitors; C442391:8-allyl-7-hydroxy-2H-benzopyran-2-one; D003374:Coumarins; D004791:Enzyme Inhibitors; D014468:Umbelliferones; C031477:7-hydroxycoumarin