Chacon Simon, Selena published the artcileDiscovery of WD Repeat-Containing Protein 5 (WDR5)-MYC Inhibitors Using Fragment-Based Methods and Structure-Based Design, COA of Formula: C8H5F3N4, the publication is Journal of Medicinal Chemistry (2020), 63(8), 4315-4333, database is CAplus and MEDLINE.
The frequent deregulation of MYC and its elevated expression via multiple mechanisms drives cells to a tumorigenic state. Indeed, MYC is overexpressed in up to ~50% of human cancers and is considered a highly validated anticancer target. Recently, we discovered that WD repeat-containing protein 5 (WDR5) binds to MYC and is a critical cofactor required for the recruitment of MYC to its target genes and reported the first small mol. inhibitors of the WDR5-MYC interaction using structure-based design. These compounds display high binding affinity, but have poor physicochem. properties and are hence not suitable for in vivo studies. Herein, we conducted an NMR-based fragment screening to identify addnl. chem. matter and, using a structure-based approach, we merged a fragment hit with the previously reported sulfonamide series. Compounds in this series can disrupt the WDR5-MYC interaction in cells, and as a consequence, we observed a reduction of MYC localization to chromatin.
Journal of Medicinal Chemistry published new progress about 2251-79-8. 2251-79-8 belongs to isoxazole, auxiliary class Trifluoromethyl,Fluoride,Benzene, name is 5-(4-(Trifluoromethyl)phenyl)-1H-tetrazole, and the molecular formula is C8H5F3N4, COA of Formula: C8H5F3N4.
Referemce:
https://en.wikipedia.org/wiki/Isoxazole,
Isoxazole | C3H3NO – PubChem