OuYang, Yiqiang; Gao, Jian; Zhao, Lei; Lu, Junfeng; Zhong, Haiqing; Tang, Hua; Jin, Shuanglong; Yue, Lu; Li, Yuezhen; Guo, Wenjie; Xu, Qiang; Lai, Yisheng published their research in Journal of Medicinal Chemistry in 2021. The article was titled 《Design, Synthesis, and Evaluation of o-(Biphenyl-3-ylmethoxy)nitrophenyl Derivatives as PD-1/PD-L1 Inhibitors with Potent Anticancer Efficacy In Vivo》.Product Details of 76006-33-2 The article contains the following contents:
Two series of novel o-(biphenyl-3-ylmethoxy)nitrophenyl compounds I (R1 = 2-hydroxyethylamino, furan-ylmethylamino, (2-acetamidoethyl)aminyl, etc.; R2 = H, Me, Br) and II (R3 = 3-cyanobenzyloxy, 3-pyridinylmethoxy, 2-cyanopyridin-4-ylmethoxy) were designed as programmed cell death protein 1 (PD-1)/PD-ligand 1 (PD-L1) inhibitors. All compounds showed significant inhibitory activity with IC50 values ranging from 2.7 to 87.4 nM except compound I (R1 = (2S)-2-aminyl-3-hydroxybutanoic acid), and compound II (III, R1 = (2S)-2-aminyl-3-hydroxybutanoic acid; R3 = 3-cyanobenzyloxy) displayed the best activity. Further experiments showed that III bound to the PD-L1 protein without obvious toxicity in Lewis lung carcinoma (LLC) cells. Furthermore, III significantly promoted interferon-gamma secretion in a dose-dependent manner in vitro and in vivo. Especially, III exhibited potent in vivo anticancer efficacy in an LLC-bearing allograft mouse model at a low dose of 5 mg/kg, which was more active than BMS-1018 (tumor growth inhibition rate: 48.5% vs 17.8%). A panel of immunohistochem. and flow cytometry assays demonstrated that III effectively counteracted PD-1-induced immunosuppression in the tumor microenvironment, thereby triggering antitumor immunity. These results indicate that III is a promising PD-1/PD-L1 inhibitor worthy of further development. After reading the article, we found that the author used 3-Bromo-2-methylbenzoic acid(cas: 76006-33-2Product Details of 76006-33-2)
3-Bromo-2-methylbenzoic acid(cas: 76006-33-2) belongs to organobromine compounds.Organobromine chemicals are produced naturally by an array of biological and other chemical processes in our environment. Organobromine compounds are produced naturally by marine creatures (sponges, corals, sea slugs, tunicates, sea fans) and seaweed, plants, fungi, lichen, algae, bacteria, microbes, and some mammals. Product Details of 76006-33-2
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary