Terphenyl-Based Small-Molecule Inhibitors of Programmed Cell Death-1/Programmed Death-Ligand 1 Protein-Protein Interaction was written by Muszak, Damian;Surmiak, Ewa;Plewka, Jacek;Magiera-Mularz, Katarzyna;Kocik-Krol, Justyna;Musielak, Bogdan;Sala, Dominik;Kitel, Radoslaw;Stec, Malgorzata;Weglarczyk, Kazimierz;Siedlar, Maciej;Domling, Alexander;Skalniak, Lukasz;Holak, Tad A.. And the article was included in Journal of Medicinal Chemistry in 2021.Safety of 5-Bromo-2-(hydroxymethyl)phenol This article mentions the following:
We describe a new class of potent PD-L1/PD-1 inhibitors based on a terphenyl scaffold that is derived from the rigidified biphenyl-inspired structure. Using in silico docking, we designed and then exptl. demonstrated the effectiveness of the terphenyl-based scaffolds in inhibiting PD-1/PD-L1 complex formation using various biophys. and biochem. techniques. We also present a high-resolution structure of the complex of PD-L1 with one of our most potent inhibitors to identify key PD-L1/inhibitor interactions at the mol. level. In addition, we show the efficacy of our most potent inhibitors in activating the antitumor response using primary human immune cells from healthy donors. In the experiment, the researchers used many compounds, for example, 5-Bromo-2-(hydroxymethyl)phenol (cas: 170434-11-4Safety of 5-Bromo-2-(hydroxymethyl)phenol).
5-Bromo-2-(hydroxymethyl)phenol (cas: 170434-11-4) belongs to organobromine compounds. 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. Many of the alkyl bromine derivatives are excellent alkylating agents since bromides are good leaving groups. Tribromides, like tetrabutylammonium tribromide, are used as a solid source of bromine. N-bromosuccimide (NBS) is used for the selective bromination of allylic bonds.Safety of 5-Bromo-2-(hydroxymethyl)phenol
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary