70362-07-1

Usage

Uses

Used in Pharmaceutical Industry:
2-hydroxy-4-Morpholinobenzaldehyde is used as a DNA-PK inhibitor and PI3K isoform inhibitor for its potential role in cancer treatment. Its ability to inhibit DNA-PK and specific PI3K isoforms may contribute to the development of targeted therapies for various types of cancer.
Used in Radiotherapy Enhancement:
2-hydroxy-4-Morpholinobenzaldehyde is used to enhance the radiation-induced cytotoxicity of HCT116 cells, which may improve the effectiveness of radiotherapy in cancer treatment. Its use at a concentration of 100 μM can potentially increase the sensitivity of cancer cells to radiation, leading to more effective tumor control.

Upstream product

• 27292-49-5 3-(4-morpholino)phenol 
• 68-12-2 N,N-dimethyl-formamide 
• 925-90-6 ethylmagnesium bromide 
• 591-27-5 m-Hydroxyaniline 
• 110-91-8 morpholine 
• 348-28-7 4-fluoro-2-hydroxybenzaldehyde 

Downstream Products

• 404009-46-7 AMA₃₇ 
• 404009-40-1 IC₈₆₆₂₁ 

Relevant academic research and scientific papers

A long-wavelength fluorescent probe with a large Stokes shift for lysosome-targeted imaging of Cys and GSH

Biothiols including cysteine (Cys) and glutathione (GSH) are biological signaling molecules responsible for cell detoxification, cell metabolism and neutralization of reactive oxygen species. Here, we synthesized a long-wavelength fluorescent probe, DCIMA

Piperazine-Coumarin based fluorescence probe with enhanced brightness and solubility for bio-thiol detection and esophageal carcinoma diagnosis

The development of novel fluorescent dyes for bio-thiol is of great importance in biological, clinical and pharmaceutical sciences. Given the importance of bio-thiol anticipating in numerous physiological processes, there is a great need to construct fluo

Synthesis and pharmacological evaluation of carboxycoumarins as a new antitumor treatment targeting lactate transport in cancer cells

Under hypoxia, cancer cells consume glucose and release lactate at a high rate. Lactate was recently documented to be recaptured by oxygenated cancer cells to fuel the TCA cycle and thereby to support tumor growth. Monocarboxylate transporters (MCT) are the main lactate carriers and therefore represent potential therapeutic targets to limit cancer progression. In this study, we have developed and implemented a stepwise in vitro screening procedure on human cancer cells to identify new potent MCT inhibitors. Various 7-substituted carboxycoumarins and quinolinone derivatives were synthesized and pharmacologically evaluated. Most active compounds were obtained using a palladium-catalyzed Buchwald-Hartwig type coupling reaction, which proved to be a quick and efficient method to obtain aminocarboxycoumarin derivatives. Inhibition of lactate flux revealed that the most active compound 19 (IC 50 11 nM) was three log orders more active than the CHC reference compound. Comparison with warfarin, a conventional anticoagulant coumarin, further showed that compound 19 did not influence the prothrombin time which, together with a good in vitro ADME profile, supports the potential of this new family of compounds to act as anticancer drugs through inhibition of lactate flux.

Isoform-specific phosphoinositide 3-kinase inhibitors from an arylmorpholine scaffold

Phosphoinositide 3-kinases (PI3-Ks) are an ubiquitous class of signaling enzymes that regulate diverse cellular processes including growth, differentiation, and motility. Physiological roles of PI3-Ks have traditionally been assigned using two pharmacological inhibitors, LY294002 and wortmannin. Although these compounds are broadly specific for the PI3-K family, they show little selectivity among family members, and the development of isoform-specific inhibitors of these enzymes has been long anticipated. Herein, we prepare compounds from two classes of arylmorpholine PI3-K inhibitors and characterize their specificity against a comprehensive panel of targets within the PI3-K family. We identify multiplex inhibitors that potently inhibit distinct subsets of PI3-K isoforms, including the first selective inhibitor of p110β/p110δ (IC50 p110β = 0.13 μM, p110δ = 0.63 μM). We also identify trends that suggest certain PI3-K isoforms may be more sensitive to potent inhibition by arylmorpholines, thereby guiding future drug design based on this pharmacophore.

Benzofurylpyrone derivatives

There is provided benzofuryl-α-pyrone derivative represented by the following structural formula (I): wherein R1represents a hydrogen atom or an alkyl group of 1 to 5 carbons; R2represents hydrogen, —CO—R5or —SO2/sub