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Biochemical Reconstitution of Steroid Receptor•Hsp90 Protein Complexes and Reactivation of Ligand Binding
Published on: September 21, 2011
Structure-activity relationship study of androstene steroids with respect to local anti-inflammatory activity
Rohini Chaubal1, Arvind M Mujumdar, Ashwini Misar
1T. R. Ingle Research Laboratory, Department of Chemistry, Sir Parshurambhau College, Pune, India.
Abstract:
A sex hormone, 3beta-acetoxy-17beta-hydroxy-androst-5-ene (1) (CAS 1639-43-6), was isolated from aerial parts of Acacia nilotica. This compound is reported to have anti-inflammatory activity. In view of this, considering this molecule as a lead molecule different androstene compounds were synthesized to study their potency and structure-activity relationship with respect to local anti-inflammatory activity. The experiments indicated that 17 ketonic compounds were more active towards inflammation than their oxime analogues. Similarly, for the compounds containing an acetyl group fixed at C-3 position a decreasing trend of activity was observed in the order of ketonic, hydroxyl, oxime and acetyl group, respectively, when these groups are at C-17 position.
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