116089-55-5Relevant academic research and scientific papers
Small Molecule Antagonists of the Nuclear Androgen Receptor for the Treatment of Castration-Resistant Prostate Cancer
Johnson, James K.,Skoda, Erin M.,Zhou, Jianhua,Parrinello, Erica,Wang, Dan,O'Malley, Katherine,Eyer, Benjamin R.,Kazancioglu, Mustafa,Eisermann, Kurtis,Johnston, Paul A.,Nelson, Joel B.,Wang, Zhou,Wipf, Peter
supporting information, p. 785 - 790 (2016/08/24)
After a high-throughput screening campaign identified thioether 1 as an antagonist of the nuclear androgen receptor, a zone model was developed for structure-activity relationship (SAR) purposes and analogues were synthesized and evaluated in a cell-based luciferase assay. A novel thioether isostere, cyclopropane (1S,2R)-27, showed the desired increased potency and structural properties (stereospecific SAR response, absence of a readily oxidized sulfur atom, low molecular weight, reduced number of flexible bonds and polar surface area, and drug-likeness score) in the prostate-specific antigen luciferase assay in C4-2-PSA-rl cells to qualify as a new lead structure for prostate cancer drug development.
Me3SiCl-promoted intramolecular cyclization of aromatic compounds tethered with N,O-acetals leading to the facile preparation of 1,4-benzodiazepine skeletons
Sakai, Norio,Watanabe, Akimasa,Ikeda, Reiko,Nakaike, Yumi,Konakahara, Takeo
experimental part, p. 8837 - 8845 (2010/11/19)
The Me3SiCl-promoted intramolecular aminomethylation of a novel type of N,O-acetals, which were prepared via a facile three-step synthesis from N-alkylaniline derivatives and N-alkyl-2-oxazolidinones that leads to the production of pharmaceutically useful 1,4-benzodiazepine skeletons with a variety of functional groups is described. This method was successfully applied to the facile preparation of both tricyclic benzodiazepine derivatives and a 1,4-benzoxazepine derivative via 7-exo-trig cyclization.
THE REMARKABLE REACTIVITY OF 2-ALKYLIDENE-IMIDAZOLIDINES IN INVERSE DIELS-ALDER REACTIONS
Gruseck, Ursula,Heuschmann, Manfred
, p. 6027 - 6030 (2007/10/02)
The reactivity of 2-alkylidene-imidazolidines 2 in inverse Diels-Alder syntheses with several pyridazines and 1,2,4-triazines is compared with that of acyclic ketene acetals 1.The 2-cyclopropylidene-imidazolidine 2c is particulary suited for less reactive dienes.
