Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10588193 | Bioorganic & Medicinal Chemistry Letters | 2012 | 6 Pages |
Abstract
Structure-based optimisation of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1)-directed high-throughput screening hit led to 7-azaindole-derivatives displaying single digit nanomolar IC50, selective against 11β-HSD2 and exhibiting good inhibition of 11β-HSD1 (IC50 < 1 μM) in 3T3L1 adipocytes.
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Eric Valeur, Serge Christmann-Franck, Franck Lepifre, Denis Carniato, Daniel Cravo, Christine Charon, Sophie Bozec, Djordje Musil, Per Hillertz, Liliane Doare, Fabien Schmidlin, Marc Lecomte, Melanie Schultz, Didier Roche,