N-Conjugate prodrugs of galiellalactone
Research output: Contribution to journal › Article
A series of amine adducts of the fungal metabolite galiellalactone (1) were prepared by reacting galiellalactone with different secondary amines via a Lewis acid catalyzed Michael addition. The adducts were assayed for in vitro effects toward prostate cancer cell lines and found to possess a similar ability to inhibit cell proliferation as galiellalactone itself. It was found that the Michael addition of amines to 1 is a reversible reaction, releasing 1 at different rates depending on the conditions, and that the adducts are potential prodrugs of galiellalactone. The chemical stability of the amine adducts is especially sensitive to pH, increasing at a lower pH.
|Research areas and keywords||
Subject classification (UKÄ) – MANDATORY
|Number of pages||4|
|Publication status||Published - 2016 Sep 7|