Open AccessSynthesis and evaluation of N-alkynylaminosteroids as potential CYP450 17A1 inhibitors
Author(s) -
Jan Panada,
Yaroslav V. Faletrov,
N. S. Frolova,
V. M. Shkumatov
Publication year - 2019
Publication title -
biomeditsinskaya khimiya
Language(s) - English
Resource type - Journals
eISSN - 2310-6972
pISSN - 2310-6905
DOI - 10.18097/pbmc20196504324
Subject(s) - pregnenolone , cyp17a1 , dehydroepiandrosterone , chemistry , conjugate , moiety , in vitro , enzyme , stereochemistry , aminoglutethimide , pharmacology , steroid , combinatorial chemistry , biochemistry , medicine , biology , mathematical analysis , mathematics , cancer , breast cancer , hormone , aromatase , androgen
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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