Authors Kiss, MA; Perina, M; Bazgier, V; May, NV; Baji, A; Jorda, R; Frank, E in PERGAMON-ELSEVIER SCIENCE LTD published article about GALETERONE; DEGRADATION; ABIRATERONE; INHIBITION; CHROMATIN; ESTRONE; BINDING; ACCESS in [Kiss, Marton A.; Baji, Adam; Frank, Eva] Univ Szeged, Dept Organ Chem, Dom Ter 8, H-6720 Szeged, Hungary; [Perina, Miroslav; Jorda, Radek] Palacky Univ Olomouc, Fac Sci, Dept Expt Biol, Slechtitelu 27, Olomouc 78371, Czech Republic; [Bazgier, Vaclav] Palacky Univ Olomouc, Fac Sci, Dept Phys Chem, Slechtitelu 241-27, Olomouc 77900, Czech Republic; [Bazgier, Vaclav] Czech Acad Sci, Lab Growth Regulators, Inst Expt Bot, Slechtitelu 27, Olomouc 78371, Czech Republic; [Bazgier, Vaclav] Palacky Univ, Slechtitelu 27, Olomouc 78371, Czech Republic; [May, Nora V.] Ctr Struct Sci, Res Ctr Nat Sci, Magyar Tudosok Korutja 2, H-1117 Budapest, Hungary in 2021.0, Cited 45.0. Product Details of 61-82-5. The Name is 1H-1,2,4-Triazol-5-amine. Through research, I have a further understanding and discovery of 61-82-5
One of the main directions of steroid research is the preparation of modified derivatives in which, in addition to changes in physicochemical properties, receptor binding is significantly altered, thus a bioactivity different from that of the parent compound predominates. In the frame of this work, 2-arylidene derivatives were first synthesized by regioselective modification of the A-ring of natural sex hormone, 5 alpha-dihydrotestosterone (DHT). After Claisen-Schmidt condensations of DHT with (hetero)aromatic aldehydes in alkaline EtOH, heterocyclizations of the alpha,beta-enones were performed with 3-amino-1,2,4-triazole, 3-aminopyrazole and 3-amino-5-methylpyrazole in the presence of t-BuOK in DMF to afford 7 ‘-epimeric mixtures of A-ring-fused azolo-dihydropyrimidines, respectively. Depending on the electronic demand of the substituents of the arylidene moiety, spontaneous or 2,3-dichloro-5,6-dicyanobenzoquinone (DDQ)-induced oxidation of the heteroring led to triazolo[1,5-a]pyrimidines and pyrazolo[1,5-a]pyrimidines in good yields, while, using the Jones reagent as a strong oxidant, 17oxidation also occurred. The crystal structures of an arylidene and a triazolopyrimidine product have been determined by single crystal X-ray diffraction and both were found to crystallize in the monoclinic crystal system at P21 space group. Most derivatives were found to diminish the transcriptional activity of androgen receptor (AR) in reporter cell line. The candidate compound (17 beta-hydroxy-2-(4-chloro)benzylidene-5 alpha-androstan-3-one, 2f) showed to suppress androgen-mediated AR transactivation in a dose-dependent manner. We confirmed the cellular interaction of 2f with AR, described the binding in AR-binding cavity by the flexible docking and showed the ability of the compound to suppress the expression of AR-regulated genes in two prostate cancer cell lines.
About 1H-1,2,4-Triazol-5-amine, If you have any questions, you can contact Kiss, MA; Perina, M; Bazgier, V; May, NV; Baji, A; Jorda, R; Frank, E or concate me.. Product Details of 61-82-5
Reference:
Article; Safari, Niloufar; Shirini, Farhad; Tajik, Hassan; Journal of Molecular Structure; vol. 1201; (2020);,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics