期刊
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
卷 33, 期 1, 页码 1271-1282出版社
TAYLOR & FRANCIS LTD
DOI: 10.1080/14756366.2018.1490731
关键词
Estrone; halogenations; aromatase; STS; 17 beta-HSD1
资金
- Janos Bolyai Research Scholarship of the Hungarian Academy of Sciences
- National Research, Development and Innovation Office-NKFIH through project Orszagos Tudomanyos Kutatasi Alapprogramok (OTKA) [SNN 124329]
- [UNKP-17-4]
Ring A halogenated 13 alpha-, 13 beta-, and 17-deoxy-13 alpha-estrone derivatives were synthesised with N-halosuccinimides as electrophile triggers. Substitutions occurred at positions C-2 and/or C-4. The potential inhibitory action of the halogenated estrones on human aromatase, steroid sulfatase, or 17 beta-hydroxysteroid dehydrogenase 1 activity was investigated via in vitro radiosubstrate incubation. Potent submicromolar or low micromolar inhibitors were identified with occasional dual or multiple inhibitory properties. Valuable structure-activity relationships were established from the comparison of the inhibitory data obtained. Kinetic experiments performed with selected compounds revealed competitive reversible inhibition mechanisms against 17 beta-hydroxysteroid dehydrogenase 1 and competitive irreversible manner in the inhibition of the steroid sulfatase enzyme.
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