Lenstra, Danny C. published the artcileStructure-Activity Relationship Studies on (R)-PFI-2 Analogues as Inhibitors of Histone Lysine Methyltransferase SETD7, Synthetic Route of 61551-49-3, the publication is ChemMedChem (2018), 13(14), 1405-1413, database is CAplus and MEDLINE.
SETD7 is a histone H3K4 lysine methyltransferase involved in human gene regulation. Aberrant expression of SETD7 has been associated with various diseases, including cancer. Therefore, SETD7 is considered a good target for the development of new epigenetic drugs. To date, few selective small-mol. inhibitors have been reported that target SETD7, the most potent being (R)-PFI-2. Herein we report structure-activity relationship studies on (R)-PFI-2 and its analogs. A library of 29 structural analogs of (R)-PFI-2 was synthesized and evaluated for inhibition of recombinantly expressed human SETD7. The key interactions were found to be a salt bridge and a hydrogen bond formed between (R)-PFI-2’s NH2+ group and SETD7’s Asp256 and His252 residue, resp.
ChemMedChem published new progress about 61551-49-3. 61551-49-3 belongs to chlorides-buliding-blocks, auxiliary class Liquid Crystal &OLED Materials, name is 5,6,7,8-Tetrahydronaphthalene-2-sulfonyl chloride, and the molecular formula is C10H11ClO2S, Synthetic Route of 61551-49-3.
Referemce:
https://en.wikipedia.org/wiki/Chloride,
Chlorides – an overview | ScienceDirect Topics