Zheng, Peiyuan published the artcileDesign, synthesis and biological evaluation of imidazo[1,5-a]pyrazin-8(7H)-one derivatives as BRD9 inhibitors, Category: piperidines, the publication is Bioorganic & Medicinal Chemistry (2019), 27(7), 1391-1404, database is CAplus and MEDLINE.
BRD9 is the subunit of mammalian SWI/SNF chromatin remodeling complex (BAF). SWI/SNF complex mutations were found in nearly 20% of human cancers. The biol. role played by BRD9 bromodomain remains poorly understood, and it is therefore imperative to identify potent and highly selective inhibitors to effectively explore the biol. of individual bromodomain proteins. In this paper, we synthesized a series of imidazo[1,5-a]pyrazin-8(7H)-one derivatives as potent BRD9 inhibitors and evaluated their BRD9 inhibitory activity in vitro and anti-proliferation effects against tumor cells. Gratifyingly, compound 27(I) and 29(II) exhibited robust potency of BRD9 inhibition with IC50 values of 35 and 103 nM resp. Docking studies were performed to explain the structure-activity relationship. Furthermore, I potently inhibited cell proliferation in cell lines A549 and EOL-1 with an IC50 value of 6.12 μM and 1.76 μM resp. The chem. probe, I, was identified that should prove to be useful in further exploring BRD9 bromodomain biol. in both in vitro and in vivo settings.
Bioorganic & Medicinal Chemistry published new progress about 39546-32-2. 39546-32-2 belongs to piperidines, auxiliary class Piperidine,Amine,Amide, name is Piperidine-4-carboxamide, and the molecular formula is C7H16Cl2Si, Category: piperidines.
Referemce:
https://en.wikipedia.org/wiki/Piperidine,
Piperidine | C5H11N – PubChem