60121-79-1Relevant 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.
Synthesis and serotonergic activity of arylpiperazide derivatives of serotonin: Potent agonists for 5-HT(1D) receptors
Perez,Fourrier,Sigogneau,Pauwels,Palmier,John,Valentin,Halazy
, p. 3602 - 3607 (2007/10/03)
A series of new arylpiperazide derivatives of serotonin has been prepared and evaluated as 5-HT(1D) receptor agonists. Binding experiments at cloned human 5-HT(1Dα), 5-HT(1Dβ), and 5-HT(1A) receptors show that all the compounds are very potent and selecti
