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Updated: Jan 20, 2026

Synthesis and Evaluation of a Ruthenium-based Mitochondrial Calcium Uptake Inhibitor
Published on: October 26, 2017
[Synthesis and evaluation of N-alkynylaminosteroids as potential CYP450 17A1 inhibitors]
J U Panada1, Y V Faletrov1, N S Frolova2
1Faculty of Chemistry, Belarusian State University, Minsk, Belarus.
Abstract:
Four isomeric dehydroepiandrosterone- and pregnenolone-based N-alkynylaminosteroids were synthesized and tested in vitro for inhibition of heterologously expressed CYP17A1. The highest inhibitory activity was observed when the optimal number of side chain atoms was met. The conjugate based on pregnenolone containing an N-propynyl moiety was found to interefere with enzymatic activity most effectively and consistently in the micromolar range.
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