Author/Editor     Živec, Matej; Sova, Matej; Brunskole, Mojca; Lenaršič, Roman; Lanišnik-Rižner, Tea; Gobec, Stanislav
Title     New inhibitors of fungal 17beta-hydroxysteroid dehydrogenase based on the (1,5)-benzodiazepine scaffold
Type     članek
Source     J Enzyme Inhib Med Chem
Vol. and No.     Letnik 22, št. 1
Publication year     2007
Volume     str. 29-36
ISSN     1475-6366
Language     eng
Abstract     The synthesis and activity of a new series of non-steroidal inhibitors of 17beta-hydroxysteroid dehydrogenase are based on a 1,5-benzodiazepine scaffold are presented. Their inhibitory potential was screened against 17beta-hydroxysteroid dehydrogenase from the fungus Cochliobolus luuatus (17beta-HSDcI), a model enzyme of the short-chain dehydrogenase/ reductase superfamily. Some of these compounds are potent inhibitors of 17beta-HSDcI activity, with IC50 values in the low micromolar range and represent promising lead compounds that should be further developed and investigated as inhibitors of human 17beta-HSD isoforms, which are the enzymes associated with the development of many hormone-dependent and neuronal diseases.
Descriptors     BENZODIAZEPINES
17-HYDROXYSTEROID DEHYDROGENASES
ASCOMYCETES
ANTINEOPLASTIC AGENTS