Most of the natural products isolated at present are heterocyclic compounds, so heterocyclic compounds occupy an important position in the research of organic chemistry. A compound: 562074-59-3, is researched, SMILESS is N#CC1=CN=CC(CCl)=C1, Molecular C7H5ClN2Journal, Article, Research Support, Non-U.S. Gov’t, Journal of Medicinal Chemistry called 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, Author is Guo, Jialin; Luo, Longlong; Wang, Zhihong; Hu, Naijing; Wang, Wei; Xie, Fei; Liang, Erguang; Yan, Xinlin; Xiao, Junhai; Li, Song, the main research direction is linear aliphatic amine linked triaryl preparation; programmed cell death 1 ligand SAR antitumor pharmacokinetics.Product Details of 562074-59-3.
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.
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Reference:
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics