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 | |
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 |