Zhang, Zhimin published the artcileDiscovery of novel coumarin derivatives as potent and orally bioavailable BRD4 inhibitors based on scaffold hopping, COA of Formula: C9H5ClO4S, the publication is Journal of Enzyme Inhibition and Medicinal Chemistry (2019), 34(1), 808-817, database is CAplus and MEDLINE.
The bromodomain and extra-terminal (BET) bromodomains, particularly BRD4, have been identified as promising therapeutic targets in the treatment of many human disorders such as cancer, inflammation, obesity, and cardiovascular disease. Recently, the discovery of novel BRD4 inhibitors has garnered substantial interest. Starting from scaffold hopping of the reported compound dihydroquinazolinone (PFI-1), a series of coumarin derivatives were designed and synthesized as a new chemotype of BRD4 inhibitors. Interestingly, the representative compounds exhibited potent BRD4 binding affinity and cell proliferation inhibitory activity, and especially displayed a favorable PK profile with high oral bioavailability (F = 49.38%) and metabolic stability (T1/2 = 4.2 h), meaningfully making it as a promising lead compound for further drug development.
Journal of Enzyme Inhibition and Medicinal Chemistry published new progress about 10543-42-7. 10543-42-7 belongs to chlorides-buliding-blocks, auxiliary class Other Aromatic Heterocyclic,Chloride,Sulfonyl chlorides,Ester, name is Coumarin-6-sulfonyl chloride, and the molecular formula is C28H41N7O4, COA of Formula: C9H5ClO4S.
Referemce:
https://en.wikipedia.org/wiki/Chloride,
Chlorides – an overview | ScienceDirect Topics