On November 25, 2020, Guo, Jialin; Luo, Longlong; Wang, Zhihong; Hu, Naijing; Wang, Wei; Xie, Fei; Liang, Erguang; Yan, Xinlin; Xiao, Junhai; Li, Song published an article.Quality Control of 2-Amino-4-chlorobenzoic acid The title of the article was Design, Synthesis, and Biological Evaluation of Linear Aliphatic Amine-Linked Triaryl Derivatives as Potent Small-Molecule Inhibitors of the Programmed Cell Death-1/Programmed Cell Death-Ligand 1 Interaction with Promising Antitumor Effects In Vivo. And the article contained the following:
A series of novel linear aliphatic amine-linked triaryl derivatives as inhibitors of PD-1/PD-L1 were designed, synthesized, and evaluated in vitro and in vivo. In this chem. series, compound I showed the most potent inhibitory activity and binding affinity with hPD-L1, with an IC50 value of 12 nM and a KD value of 16.2 pM, showing a binding potency approx. 2000-fold that of hPD-1. Compound I could bind with hPD-L1 on the cellular surface and competitively block the interaction of hPD-1 with hPD-L1. In a T cell function assay, I restored the T cell function, leading to increased IFN-γ secretion. Moreover, in a humanized mouse model, compound I significantly inhibited tumor growth without obvious toxicity and showed moderate PK properties after i.v. injection. These results indicated that I is a promising lead for further development of small-mol. PD-1/PD-L1 inhibitors for cancer therapy. The experimental process involved the reaction of 2-Amino-4-chlorobenzoic acid(cas: 89-77-0).Quality Control of 2-Amino-4-chlorobenzoic acid
The Article related to linear aliphatic amine linked triaryl preparation, programmed cell death 1 ligand sar antitumor pharmacokinetics, Benzene, Its Derivatives, and Condensed Benzenoid Compounds: Amines, Amine Oxides, Imines, and Quaternary Ammonium Compounds and other aspects.Quality Control of 2-Amino-4-chlorobenzoic acid
Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics