1162-60-3Relevant articles and documents
7α-Methy-17α-(E-2′[ 125l]iodvinyl)-19-nortestosterone: A new radioligand for the detection of androgen receptor
Hoyte, Robert M.,Brown, Theodore J.,MacLusky, Neil J.,Hochberg, Richard B.
, p. 13 - 23 (1993)
We have synthesized two γ-emitting, 125I-labeled steroids, E- and Z-7α-methyl-17α-((2′-[ 125I]iodovinyl)-19-nortestosterone [125I](E- and Z-MIVNT) for specific labeling of androgen receptors. [125I]E- and [125I]Z-MIVNTwere synthesized stereospecifically from E- and Z-7α-methyl- 17α-(2′-tri-n-butylstannylvinyl)-19-nortestosterone. The tin adducts were prepared by addition of tri-n-butyltin hydride to 7α-methyl-17α-ethynyl-19-nortestosterone, and after purification they were converted in high yield to the [125I]MIVNT isomers by reaction with 125I (generated in situ by oxidation of [125I] iodide with chloramine T). The 125I-labeledproducts were purified by high-performance liquid chromatography, and their mass determined with an ultraviolet detector (specific activity of both, approximately 2,200 Ci/mmol). In rat prostate cytosol, [125I]E-MIVNT bound with high affinity to a single class of binding sites. Nonspecific binding in the presence of 5α-dihydrotestosterone was relatively low, and compared favorably with that obtained in parallel studies with [3H]methyltrienolone (R1881). The E-isomer bound prostate cytosol with at least twice the affinity of the Z-isomer; therefore, the interaction of the E-isomer with the androgen receptor as well as other steroid receptors was studied in greater detail. Complexes of the androgen receptor with [125I]E-MIVNT as well as [3H]R1881 dissociate very slowly at 4C (kdiss for BOTH = 0.04 h-1). Displacement studies showed that the interaction of[125I]E-MIVNTwith the androgen receptor is highly specific. Competition studies showed that unlabeled E-MIVNT binds poorly to other steroid receptors in rat tissue cytosols. These binding properties make [125I]E-MIVNT a promising ligand for study of the androgen receptor, and [1325I]E-MIVNT a potential imaging agent for the detection of androgen-dependent tumors, such as prostate cancer. (Steroids 58:13-23, 1993).
COMPOUNDS FOR TARGETED THERAPIES OF CASTRATION RESISTANT PROSTATE CANCER
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Paragraph 00126; 00127, (2020/09/12)
The present invention generally relates to new compounds for therapeutic uses. In particular, this disclosure relates to novel tetracyclic compounds useful for treatment of cancer, especially castration resistant prostate cancer. Pharmaceutical composition matters and methods for treating a cancer patient by administering therapeutically effective amounts of such compound alone or together with other therapeutics are within the scope of this disclosure.
Method of producing tibolone metabolites by fermentation with Rhizopus stolonifer
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Page/Page column 10, (2012/04/10)
A new method of producing metabolites of tibolone comprising fermenting tibolone with Rhizopus stolonifer (ATCC 12938) resulting in the formation of Δ4-Tibolone (C21H28O2), 6β-Hydroxytibolone, and 15β-Hydroxytibolone (C21H28O3) is reported.
