In 2019,European Journal of Medicinal Chemistry included an article by Zhu, Yan; Sun, Nannan; Yu, Mingcheng; Guo, Huimin; Xie, Qiong; Wang, Yonghui. Recommanded Product: 3395-91-3. The article was titled 《Discovery of aryl-substituted indole and indoline derivatives as RORγt agonists》. The information in the text is summarized as follows:
A series of aryl-substituted indole and indoline derivatives were discovered as novel RORγt agonists by a scaffold-based hybridization of the reported RORγt 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 RORγt agonists with improved drug-like properties. Compound 14 represented a high potency lead with an EC50 of 20.8 ± 1.5 nM, the (S)-enantiomer (EC50 = 16.1 ± 4.5 nM) of which was 17 times more potent than the (R) counterpart (EC50 = 286 ± 30.4 nM) in RORγ dual FRET assay. The cell-based GAL4 reporter gene assay also suggested 14 as the most active compound which exhibited an EC50 of 247 ± 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 RORγt agonist for cancer immunotherapy. In the experimental materials used by the author, we found Methyl 3-bromopropanoate(cas: 3395-91-3Recommanded Product: 3395-91-3)
Methyl 3-bromopropanoate(cas: 3395-91-3) belongs to bromides. Most organobromine compounds, like most organohalide compounds, are relatively nonpolar. Bromine is more electronegative than carbon (2.9 vs 2.5). Consequently, the carbon in a carbon–bromine bond is electrophilic, i.e. alkyl bromides are alkylating agents.Recommanded Product: 3395-91-3
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary