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  • Synthesis and structure-activity relationships of 2- and/or 4-halogenated 13[beta]- and 13[alpha]-estrone derivatives as enzyme inhibitors of estrogen biosynthesis
    Bacsa, Ildikó ...
    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.
    Source: Journal of enzyme inhibition and medicinal chemistry. - ISSN 1475-6366 (Vol. 33, iss. 1, 2018, str. 1271-1282)
    Type of material - article, component part
    Publish date - 2018
    Language - english
    COBISS.SI-ID - 33949401