87165-41-1Relevant articles and documents
Benzopyridone heterocyclic compound and application thereof
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Paragraph 0096; 0099; 0104-0106, (2020/08/18)
The invention relates to a benzopyridone heterocyclic compound and an application thereof. The compound is a compound represented by a formula I, or a pharmaceutically acceptable salt thereof, or a stereoisomer thereof, or a tautomer thereof, or a hydrate thereof, or a solvate thereof, or a metabolite thereof, or a prodrug thereof, and R1, R2, R3, R4 and R5 and an A group are as defined in the specification. The compound disclosed by the invention can be used for preparing a medicine for treating and/or preventing cancers.
Low molecular weight amidoximes that act as potent inhibitors of lysine-specific demethylase 1
Hazeldine, Stuart,Pachaiyappan, Boobalan,Steinbergs, Nora,Nowotarski, Shannon,Hanson, Allison S.,Casero, Robert A.,Woster, Patrick M.
, p. 7378 - 7391 (2012/10/29)
The recently discovered enzyme lysine-specific demethylase 1 (LSD1) plays an important role in the epigenetic control of gene expression, and aberrant gene silencing secondary to LSD1 dysregulation is thought to contribute to the development of cancer. We reported that (bis)guanidines, (bis)biguanides, and their urea- and thiourea isosteres are potent inhibitors of LSD1 and induce the re-expression of aberrantly silenced tumor suppressor genes in tumor cells in vitro. We now report a series of small molecule amidoximes that are moderate inhibitors of recombinant LSD1 but that produce dramatic changes in methylation at the histone 3 lysine 4 (H3K4) chromatin mark, a specific target of LSD1, in Calu-6 lung carcinoma cells. In addition, these analogues increase cellular levels of secreted frizzle-related protein (SFRP) 2, H-cadherin (HCAD), and the transcription factor GATA4. These compounds represent leads for an important new series of drug-like epigenetic modulators with the potential for use as antitumor agents.