In an article, published in an article,authors is Zhu, Yan, once mentioned the application of category: Thiomorpholine, Name is Thiomorpholine 1,1-dioxide,molecular formula is C4H9NO2S, is a conventional compound. this article was the specific content is as follows. category: Thiomorpholine
Discovery of aryl-substituted indole and indoline derivatives as RORgammat agonists
A series of aryl-substituted indole and indoline derivatives were discovered as novel RORgammat agonists by a scaffold-based hybridization of the reported RORgammat agonists 1 and 2. SAR studies on the core structures, the RHS hydrophilic side chains and the LHS hydrophobic aryl groups of a hybrid compound 3 led to the identification of potent RORgammat agonists with improved drug-like properties. Compound 14 represented a high potency lead with an EC50 of 20.8 ¡À 1.5 nM, the (S)-enantiomer (EC50 = 16.1 ¡À 4.5 nM) of which was 17 times more potent than the (R) counterpart (EC50 = 286 ¡À 30.4 nM) in RORgamma dual FRET assay. The cell-based GAL4 reporter gene assay also suggested 14 as the most active compound which exhibited an EC50 of 247 ¡À 33.1 nM and a maximum activation percentage of 133%. Moreover, 14 showed high metabolic stability (t1/2 = 113 min) in mouse liver microsome and had improved aqueous solubility at pH 7.4 compared to the parent compounds. Furthermore, 14 was found to be orally bioavailable and demonstrated excellent in vivo pharmacokinetics in mice. Present studies indicate that 14 deserves further investigation in tumor animal models as a potential candidate of RORgammat agonist for cancer immunotherapy.
The proportionality constant is the rate constant for the particular unimolecular reaction. the reaction rate is directly proportional to the concentration of the reactant. I hope my blog about 39093-93-1 is helpful to your research. category: Thiomorpholine
Reference£º
Thiomorpholine – Wikipedia,
Thiomorpholine | C4H9NS – PubChem