Small-molecule inhibitors of ferrochelatase are antiangiogenic agents was written by Sishtla, Kamakshi;Lambert-Cheatham, Nathan;Lee, Bit;Han, Duk Hee;Park, Jaehui;Sardar Pasha, Sheik Pran Babu;Lee, Sanha;Kwon, Sangil;Muniyandi, Anbukkarasi;Park, Bomina;Odell, Noa;Waller, Sydney;Park, Il Yeong;Lee, Soo Jae;Seo, Seung-Yong;Corson, Timothy W.. And the article was included in Cell Chemical Biology in 2022.SDS of cas: 638-07-3 The following contents are mentioned in the article:
Activity of the heme synthesis enzyme ferrochelatase (FECH) is implicated in multiple diseases. In particular, it is a mediator of neovascularization in the eye and thus an appealing therapeutic target for preventing blindness. However, no drug-like direct FECH inhibitors are known. Here, we set out to identify small-mol. inhibitors of FECH as potential therapeutic leads using a high-throughput screening approach to identify potent inhibitors of FECH activity. A structure-activity relationship study of a class of triazolopyrimidinone hits yielded drug-like FECH inhibitors. These compounds inhibit FECH in cells, bind the active site in cocrystal structures, and are antiangiogenic in multiple in vitro assays. One of these promising compounds was antiangiogenic in vivo in a mouse model of choroidal neovascularization. This foundational work may be the basis for new therapeutic agents to combat not only ocular neovascularization but also other diseases characterized by FECH activity. This study involved multiple reactions and reactants, such as Ethyl 4-chloro-3-oxobutanoate (cas: 638-07-3SDS of cas: 638-07-3).
Ethyl 4-chloro-3-oxobutanoate (cas: 638-07-3) belongs to organic chlorides. Chlorinated organic compounds are found in nearly every class of biomolecules and natural products including alkaloids, terpenes, amino acids, flavonoids, steroids, and fatty acids. Alkyl chlorides readily react with amines to give substituted amines. Alkyl chlorides are substituted by softer halides such as the iodide in the Finkelstein reaction.SDS of cas: 638-07-3
Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics