Zeng, Qing-Xuan; Wang, Kun; Zhang, Xin; Shi, Yu-Long; Dou, Yue-Ying; Guo, Zhi-Hao; Zhang, Xin-Tong; Zhang, Na; Deng, Hong-Bin; Li, Ying-Hong; Song, Dan-Qing published their research in Bioorganic Chemistry in 2021. The article was titled 《Structure-activity relationship and biological evaluation of 12 N-substituted aloperine derivatives as PD-L1 down-regulatory agents through proteasome pathway》.Reference of 4-Cyanobenzyl bromide The article contains the following contents:
Twenty-nine 12 N-substituted aloperine derivatives were synthesized and screened for suppression on PD-L1 expression in H460 cells, as a continuation of our work. Systematic structural modifications led to the identification of compound I as the most active PD-L1 modulator. Compound I could significantly down-regulate both constitutive and inductive PD-L1 expression in NSCLC cells, and successively enhance the cytotoxicity of co-cultured T cells against tumor cells at the concentration of 20μM. Also, it exhibited a moderate in vivo anticancer efficacy against Lewis tumor xenograft with a stable PK and safety profile. The mechanism study indicated that I mediated the degradation of PD-L1 through a proteasome pathway, rather than a lysosome route. These results provided the powerful information for cancer immunotherapy of aloperine derivatives with unique endocyclic skeleton by targeting PD-L1 to activate immune cells to kill cancer cells. The experimental part of the paper was very detailed, including the reaction process of 4-Cyanobenzyl bromide(cas: 17201-43-3Reference of 4-Cyanobenzyl bromide)
4-Cyanobenzyl bromide(cas: 17201-43-3) is used in the synthesis of ligands containing a chelating pyrazolyl-pyridine group with a pendant aromatic nitrile. It is also useful in the preparation of 4-[(2H-tetra-zol-2-yl)methyl]benzonitrile by reaction with 2H-tetrazole in the presence of potassium hydroxide.Reference of 4-Cyanobenzyl bromide
Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts