Yang, Yang; Wang, Ke; Chen, Hao; Feng, Zhiqiang published an article in 2021. The article was titled 《Design, synthesis, evaluation, and SAR of 4-phenylindoline derivatives, a novel class of small-molecule inhibitors of the programmed cell death-1/ programmed cell death-ligand 1 (PD-1/PD-L1) interaction》, and you may find the article in European Journal of Medicinal Chemistry.Safety of 2-Aminopropane-1,3-diol The information in the text is summarized as follows:
The blockade of the PD-1/PD-L1 immune checkpoint pathway with small mols. is an emerging immunotherapeutic approach. A novel series of 4-phenylindoline derivatives were synthesized, and their inhibitory activity against the PD-1/PD-L1 protein-protein interaction (PPI) was evaluated through a homogenous time-resolved fluorescence (HTRF) assay. Among them, I and II exhibited potent activity with IC50 values of 17 nM and 12 nM, resp. Furthermore, I showed the promising inhibitory activity against the PD-1/PD-L1 interaction with the EC50 value of 0.43μM in a co-culture model of PD-L1/TCR Activator-expressing CHO cells and PD-1-expressing Jurkat cells. Besides, the structure-activity relationships (SAR) of the novel synthesized 4-phenylindoline derivatives was concluded, and the binding mode of II with the PD-L1 dimer was analyzed by mol. simulation and docking, demonstrating that the N-atom in the side chain of indoline fragment could interact with the amino acid residue of the PD-L1 protein to lead to the potent inhibitory activity. This study provided a new insight for further drug design.2-Aminopropane-1,3-diol(cas: 534-03-2Safety of 2-Aminopropane-1,3-diol) was used in this study.
2-Aminopropane-1,3-diol(cas: 534-03-2) belongs to anime. Large quantities of aliphatic amines are made synthetically. The most widely used industrial method is the reaction of alcohols with ammonia at a high temperature, catalyzed by metals or metal oxide catalysts (e.g., nickel or copper). Mixtures of primary, secondary, and tertiary amines are thereby produced.Safety of 2-Aminopropane-1,3-diol
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