《Development of pyrazolo[3,4-d]pyrimidine-6-amine-based TRAP1 inhibitors that demonstrate in vivo anticancer activity in mouse xenograft models》 was written by Kim, Darong; Kim, So-Yeon; Kim, Dongyoung; Yoon, Nam Gu; Yun, Jisu; Hong, Ki Bum; Lee, Changwook; Lee, Ji Hoon; Kang, Byoung Heon; Kang, Soosung. Quality Control of 4-Bromo-1-(bromomethyl)-2-fluorobenzene And the article was included in Bioorganic Chemistry on August 31 ,2020. The article conveys some information:
TNF Receptor Associated Protein 1 (TRAP1) is a mitochondrial paralog of Hsp90 related to the promotion of tumorigenesis in various cancers via maintaining mitochondrial integrity, reducing the production of reactive oxygen species, and reprogramming cellular metabolism Consequently, Hsp90 and TRAP1 have been targeted to develop cancer therapeutics. Herein, we report a series of pyrazolo[3,4-d]pyrimidine derivatives that are mitochondria-permeable TRAP1 inhibitors. Structure-based drug design guided the optimization of potency, leading to the identification of compounds 47 and 48 as potent TRAP1 and Hsp90 inhibitors with good metabolic and plasma stability as well as acceptable CYP and hERG inhibition. X-ray co-crystallization studies confirmed both 47 and 48 interact with the ATP binding pocket in the TRAP1 protein. Compounds 47 and 48 demonstrated excellent anticancer efficiency in various cancer cells, with limited toxicity over normal hepatocyte and prostate cells. Mouse PC3 xenograft studies showed 47 and 48 significantly reduced tumor growth. The experimental process involved the reaction of 4-Bromo-1-(bromomethyl)-2-fluorobenzene(cas: 76283-09-5Quality Control of 4-Bromo-1-(bromomethyl)-2-fluorobenzene)
4-Bromo-1-(bromomethyl)-2-fluorobenzene(cas: 76283-09-5) 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. Quality Control of 4-Bromo-1-(bromomethyl)-2-fluorobenzene
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary