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Deoxycholic acid derivatives were designed as P-glycoprotein (Pgp, ABCB1) inhibitors. Thus the synthesis and the biological activity of methyl deoxycholate derivatives 5–10 and their ether analogs 15–20 have been reported. The potency of these compounds to modulate Pgp-mediated MDR was evaluated through daunorubicin accumulation and potentiation of doxorubicin cytotoxicity in K562/R7 multidrug resistant...
Bisphenol A (BPA), is one of the most abundant endocrine disruptors that are present in our environment, and has been repeatedly detected in most human biological samples. As it has been suggested that part of the BPA measured in human samples is due to contamination during samples collection or laboratory measurements, we have developed a specific radioimmunoassay for the measurement of BPA-glucuronide...
Bisphenol A (BPA) is widely used in the manufacturing of polycarbonate plastic food and drink packaging. Possessing a weak estrogenic activity, BPA is listed among a growing list of endocrine disrupting compounds.In this study, a polyclonal anti-BPA antibody was obtained by immunization with BPA-monocarboxymethylether covalently linked to BSA. The antibody demonstrates negligible cross-reactivity...
The photoactivable aryl azide reagents, N-(5-azido-2-nitrobenzoyl)oxysuccinimide, 4-azido-1-fluoro-2-nitrobenzene, and 4-azido-1-nitro-2,4,5,6-tetrafluorobenzene have been condensed at the extremity of three 17α-aminomethyl, 17α-aminoethyl, and 17α-aminopropyl side-chains introduced on (17S)-spiro-(3,3-dimethoxy)-5α-androstan-17β,2'-oxirane either directly, by ammonolysis, in the first case, or by...
17α-Aminomethyl, 17α-acetamidomethyl, and 17α-hemiglutaramidomethyl derivatives of dihydrotestosterone and testosterone have been prepared by hydrocyanation of 3,3 -(ethylenedioxy)-5α-androstan-17-one and 3,3 -ethylenedioxyandrost-5-en-17-one, reduction of the corresponding acetylated 17α-cyanohydrins with lithium aluminium hydride, and acylation of the resulting 17α-aminomethyl derivatives with...
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