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Matches in SemOpenAlex for { <https://semopenalex.org/work/W2053819908> ?p ?o ?g. }

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• W2053819908 abstract "Indole-pyrrolidines were identified as inhibitors of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) by high-throughput screening. Optimisation of the initial hit through structure-based design led to 7-azaindole-derivatives, with the best analogues displaying single digit nanomolar IC50 potency. The modeling hypotheses were confirmed by solving the X-ray co-crystal structure of one of the lead compounds. These compounds were selective against 11β-hydroxysteroid dehydrogenase type 2 (selectivity ratio >200) and exhibited good inhibition of 11β-HSD1 (IC50 < 1 μM) in a cellular model (3T3L1 adipocytes)" @default.
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• W2053819908 date "2012-09-01" @default.
• W2053819908 modified "2023-09-23" @default.
• W2053819908 title "Structure-based design of 7-azaindole-pyrrolidine amides as inhibitors of 11β-hydroxysteroid dehydrogenase type I" @default.
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• W2053819908 doi "https://doi.org/10.1016/j.bmcl.2012.07.070" @default.
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