Kawashita, Seiji; Aoyagi, Koichi; Fukushima, Kyoko; Hantani, Rie; Naruoka, Shiori; Tanimoto, Atsuo; Hori, Yuji; Toyonaga, Yukiyo; Yamanaka, Hiroshi; Miyazaki, Susumu; Hantani, Yoshiji published an article in 2021. The article was titled 《SAR study of small molecule inhibitors of the programmed cell death-1/programmed cell death-ligand 1 interaction》, and you may find the article in Chemical Biology & Drug Design.Related Products of 139115-91-6 The information in the text is summarized as follows:
The development of small mol. inhibitors of programmed cell death-1/programmed cell death-ligand 1 (PD-1/PD-L1) has drawn research interest for the treatment of cancer. Recently, we reported the discovery of a novel dimeric core small mol. PD-1/PD-L1 inhibitor. In an effort to discover more potent inhibitors, we further explored the dimeric core scaffold. Our investigations of the structure-activity-relationship revealed that introduction of lipophilic substituents onto one of the di-alkoxylated Ph rings improved binding affinities to PD-L1, and inhibitory activities of PD-1/PD-L1 in cellular assays. Furthermore, conversion of the ether linker part to an olefin linker not only improved binding affinity but also led to slow dissociation binding kinetics. We also explored more potent, as well as downsized, scaffolds. Compounds bearing a linear chain in place of one of the di-alkoxylated Ph rings exhibited good binding affinity with improved ligand efficiency (LE). Representative compounds demonstrated potent inhibitory activities of PD-1/PD-L1 in the submicromolar range in cellular assays as well as cellular function in the mixed lymphocyte reaction (MLR) assay with efficacy comparable to anti-PD-1 antibody. Our results provide applicable information for the design of more potent inhibitors targeting PD-1/PD-L1 pathway. After reading the article, we found that the author used tert-Butyl (2-(2-hydroxyethoxy)ethyl)carbamate(cas: 139115-91-6Related Products of 139115-91-6)
tert-Butyl (2-(2-hydroxyethoxy)ethyl)carbamate(cas: 139115-91-6) belongs to ethers.Related Products of 139115-91-6Although ethers resist hydrolysis, they are cleaved by hydrobromic acid and hydroiodic acid. Hydrogen chloride cleaves ethers only slowly.
Referemce:
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem