98653-71-5Relevant articles and documents
Synthesis and evaluation of potential radioligands for the progesterone receptor
Hoyte,Rosner,Johnson,Zielinski,Hochberg
, p. 1695 - 1699 (1985)
Several steroidal analogues were synthesized as potential γ-emitting radioligands for the progesterone receptor. Each of these compounds was tested as an inhibitor of the specific binding of [3H]-17α, 21-dimethyl-19-nor-4,9-pregnadiene-3,20-dione (R5020) to the progesterone receptor in rabbit uterine cytosol. R5020 is a well-known progestin with high affinity for the receptor. Of the compounds synthesized, aromatic N-substituted C-17 steroidal carboxamides inhibited the binding only poorly. Three compounds, 16α-iodo-4-estren-17β-ol-3-one, 17α-[2(E)-iodovinyl]-4-estren-17β-ol-3-one, and 17α-[2(Z)-iodovinyl]-4-estren-17β-ol-3-one were excellent competitors, each having a K(i) less than or equal to that of the natural progestin, progesterone. Since similar iodinated analogues of estrogens have been shown to be extremely stable both in vivo and in vitro, these compounds are potentially useful ligands for the progesterone receptor.
Design, synthesis and evaluation of progesterone-adenine hybrids as bivalent inhibitors of P-glycoprotein-mediated multidrug efflux
Zeinyeh, Wa?l,Alameh, Ghina,Radix, Sylvie,Grenot, Catherine,Dumontet, Charles,Walchshofer, Nadia
scheme or table, p. 3165 - 3168 (2010/09/05)
Steroidal bivalent ligands were designed on the basis of the described closer proximity of the ATP-site and the putative steroid-binding site of P-glycoprotein (ABCB1). The syntheses of seven progesterone-adenine hybrids were described. Their abilities to inhibit P-glycoprotein-mediated daunorubicin efflux in K562/R7 human leukemic cells overexpressing P-glycoprotein were evaluated versus progesterone.
