Abstract
Four isomeric N-alkynylaminosteroids of the androstane and pregnane series were synthesized and tested in vitro for inhibition of CYP450 17A1 heterologously expressed in transgenic yeast Yarrowia lipolytica. The highest inhibitory activity was observed in the case of steroids containing a side chain of five atoms. At equal concentrations of the substrate and the inhibitor (50 μM), the pregnenolone derivative containing the N-propynyl fragment caused a 5-fold decrease of reduced the progesterone conversion.
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