In 2022,Zhang, Hongquan; Wen, Chunxi; Li, Bingting; Yan, Xinlin; Xu, Yangrong; Guo, Jialin; Hou, Shi; Chang, Jiajia; Li, Song; Xiao, Junhai published an article in Molecules. The title of the article was 《Phenoxyaromatic Acid Analogues as Novel Radiotherapy Sensitizers: Design, Synthesis and Biological Evaluation》.Formula: C6H5Br2N The author mentioned the following in the article:
Radiotherapy is a vital approach for brain tumor treatment. The standard treatment for glioblastoma (GB) is maximal surgical resection combined with radiotherapy and chemotherapy. However, the non-sensitivity of tumor cells in the hypoxic area of solid tumors to radiotherapy may cause radioresistance. Therefore, radiotherapy sensitizers that increase the oxygen concentration within the tumor are promising for increasing the effectiveness of radiation. Inspired by Hb allosteric oxygen release regulators, a series of novel phenoxyacetic acid analogs were designed and synthesized. A numerical method was applied to determine the activity and safety of newly synthesized compounds In vitro studies on the evaluation of red blood cells revealed that compounds 19c (ΔP50 = 45.50 mmHg) and 19t (ΔP50 = 44.38 mmHg) improve the oxygen-releasing property effectively compared to pos. control efaproxiral (ΔP50 = 36.40 mmHg). Preliminary safety evaluation revealed that 19c exhibited no cytotoxicity towards HEK293 and U87MG cells, while 19t was cytotoxic toward both cells with no selectivity. An in vivo activity assay confirmed that 19c exhibited a radiosensitization effect on orthotopically transplanted GB in mouse brains. Moreover, a pharmacokinetic study in rats showed that 19c was orally available. In the part of experimental materials, we found many familiar compounds, such as 3,5-Dibromoaniline(cas: 626-40-4Formula: C6H5Br2N)
3,5-Dibromoaniline(cas: 626-40-4) belongs to anime. To avoid the problem of multiple alkylation, methods have been devised for “blocking” substitution so that only one alkyl group is introduced. The Gabriel synthesis is one such method; it utilizes phthalimide, C6H4(CO)2NH, whose one acidic hydrogen atom has been removed upon the addition of a base such as KOH to form a salt.Formula: C6H5Br2N
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary