10589-28-3

Upstream product

• 80171-33-1 5-(4-hydroxybenzylidene)imidazolidine-2,4-dione 
• 123-08-0 4-hydroxy-benzaldehyde 

Downstream Products

• 154722-74-4 methyl 2-oxo-3-(4-hydroxyphenyl)propionate 
• 56401-28-6 [2-hydroxyimino-3-(4-hydroxyphenyl)]propionic acid 
• 862252-61-7 methyl (4-hydroxyphenyl)pyruvate, enol form 
• 87414-44-6 α-oxo-β-(p-hydroxyphenyl)-γ-(p-hydroxybenzyl)-γ-methoxycarbonyl-γ-lactone 

Relevant academic research and scientific papers

Furanone compound and preparation method and application thereof

The invention discloses a furanone compound and a preparation method and application thereof. P-hydroxybenzaldehyde is used as a raw material, condensed with hydantoin and then subjected to alkaline hydrolysis and esterification to obtain a p-hydroxyphenylpyruvate intermediate; p-hydroxy benzaldehyde and halogenated isopentene are subjected to alkylation, and then benzyl protection is performed toobtain a benzaldehyde derivative intermediate; a benzaldehyde derivative intermediate and a phenylpyruvate intermediate are subjected to aldol condensation and intramolecular esterification under thecatalysis of a condensing agent to synthesize novel furanone compounds BL5 and BL10. The furanone derivative has H1N1 virus inhibition activity, and can be used for preparing medicines for treating H1N1 virus infection.

CARBONIC ANHYDRASE INHIBITORS

Compounds are provided which are inhibitors of the CAXII enzyme. Due to the interaction between CAXII and Pgp, such compounds may be useful in lowering the chemoresistance of a cancer allowing for co-administration with existing anti-cancer agents.

Design, synthesis, and biological evaluation of substrate-competitive inhibitors of C-terminal Binding Protein (CtBP)

C-terminal Binding Protein (CtBP) is a transcriptional co-regulator that downregulates the expression of many tumor-suppressor genes. Utilizing a crystal structure of CtBP with its substrate 4-methylthio-2-oxobutyric acid (MTOB) and NAD+ as a guide, we have designed, synthesized, and tested a series of small molecule inhibitors of CtBP. From our first round of compounds, we identified 2-(hydroxyimino)-3-phenylpropanoic acid as a potent CtBP inhibitor (IC50 = 0.24 μM). A structure-activity relationship study of this compound further identified the 4-chloro- (IC50 = 0.18 μM) and 3-chloro- (IC50 = 0.17 μM) analogues as additional potent CtBP inhibitors. Evaluation of the hydroxyimine analogues in a short-term cell growth/viability assay showed that the 4-chloro- and 3-chloro-analogues are 2-fold and 4-fold more potent, respectively, than the MTOB control. A functional cellular assay using a CtBP-specific transcriptional readout revealed that the 4-chloro- and 3-chloro-hydroxyimine analogues were able to block CtBP transcriptional repression activity. This data suggests that substrate-competitive inhibition of CtBP dehydrogenase activity is a potential mechanism to reactivate tumor-suppressor gene expression as a therapeutic strategy for cancer.