1. Faculty of Chemistry, Belarusian State University, Minsk, Belarus 2. Research Institute for Physical Chemical Problems, Belarusian State University, Minsk, Belarus
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.
Panada J.U., Faletrov Y.V., Frolova N.S., Shkumatov V.M. (2019) Synthesis and evaluation of N-alkynylaminosteroids as potential CYP450 17A1 inhibitors. Biomeditsinskaya Khimiya, 65(4), 324-330.
Panada J.U. et al. Synthesis and evaluation of N-alkynylaminosteroids as potential CYP450 17A1 inhibitors // Biomeditsinskaya Khimiya. - 2019. - V. 65. -N 4. - P. 324-330.
Panada J.U. et al., "Synthesis and evaluation of N-alkynylaminosteroids as potential CYP450 17A1 inhibitors." Biomeditsinskaya Khimiya 65.4 (2019): 324-330.
Panada, J. U., Faletrov, Y. V., Frolova, N. S., Shkumatov, V. M. (2019). Synthesis and evaluation of N-alkynylaminosteroids as potential CYP450 17A1 inhibitors. Biomeditsinskaya Khimiya, 65(4), 324-330.
