67268-42-2

Upstream product

• 93-35-6 7-hydroxy-2H-chromen-2-one 
• 106-96-7 propargyl bromide 
• 38445-24-8 6-hydroxy-4H-1-benzopyran-4-one 
• 107-19-7 propargyl alcohol 

Downstream Products

• 1379521-08-0 7-[(1-phenyl-1H-1,2,3-triazol-4-yl)methoxy]-2H-chromen-2-one 
• 1379521-07-9 7-[(1-phenyl-1H-1,2,3-triazol-4-yl)methoxy]-2H-chromene-2-thione 
• 1379521-26-2 7-((1-(2-fluorophenyl)-1H-1,2,3-triazol-4-yl)methoxy)-2H-chromen-2-one 
• 1379521-25-1 7-[1'-(2-bromophenyl)-1H-1',2',3'-triazol-4'-yl]methoxy-2H-chromen-2-one 
• 1422963-21-0 4β-[(4-(((2-oxo-2H-chromen-7-yl)oxy)methyl)-1H-1,2,3-triazol-1-yl)]-4-desoxypodophyllotoxin 
• 1449232-46-5 C₃₀H₄₁AuN₃O₃P 
• 1449232-48-7 C₃₀H₄₀AuO₃P 
• 1621674-83-6 (E)-7-((1-(3-(3-(3,4-dimethoxyphenyl)acryloyl)phenyl)-1H-1,2,3-triazol-4-yl)methoxy)-2H-chromen-2-one 
• 1621674-84-7 (E)-7-((1-(3-(3-(2,3-dimethoxyphenyl)acryloyl)phenyl)-1H-1,2,3-triazol-4-yl)methoxy)-2H-chromen-2-one 
• 1621674-85-8 (E)-7-((1-(4-(3-(2,3-dimethoxyphenyl)acryloyl)phenyl)-1H-1,2,3-triazol-4-yl)methoxy)-2H-chromen-2-one 
• 1621674-86-9 (E)-7-((1-(3-(3-(2,3,4-trimethoxyphenyl)acryloyl)phenyl)-1H-1,2,3-triazol-4-yl)methoxy)-2H-chromen-2-one 
• 1621674-87-0 (E)-7-((1-(4-(3-(2,3,4-trimethoxyphenyl)acryloyl)phenyl)-1H-1,2,3-triazol-4-yl)methoxy)-2H-chromen-2-one 
• 1621674-88-1 (E)-7-((1-(4-(3-(3,4,5-trimethoxyphenyl)acryloyl)phenyl)-1H-1,2,3-triazol-4-yl)methoxy)-2H-chromen-2-one 

Relevant academic research and scientific papers

Umbelliferone aminoalkyl derivatives, a new class of squalene-hopene cyclase inhibitors

The synthesis is described of several aminoalkyl derivatives of coumarin, obtained in good yields under microwave or high-intensity ultrasound irradiation. These compounds proved uniformly active as inhibitors of squalene-hopene cyclase (SHC) from Alicycl

Synthesis, docking study, and biological evaluation of novel umbellipherone/hymecromone derivatives as acetylcholinesterase/butyrylcholinesterase inhibitors

A novel hybrid series of umbellipherone and benzyl amine scaffolds, linked via triazole ring, was synthesized and evaluated as both acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) inhibitors. Most of the synthesized compounds showed moderate to high activities by using Ellman’s modified assay. Among the target compounds, 6e bearing 3-methoxy substituent on benzyl moiety was the most active one (AChE and BuChE IC50 = 3.4 and 1.1 μM, respectively). Finally, binding modes of the target compound was studied using molecular docking stimulations. The neuroprotectivity evaluation exhibited that this compound efficiently protected PC12 neurons against H2O2-induced cell death.

Amphiphilic block copolymer micelles with fluorescence as nano-carriers for doxorubicin delivery

Well-defined and nontoxic core-shell polymeric micelles, containing fluorescence units, were employed for efficient drug delivery of doxorubicin (DOX). The self-assembled structures were generated from triblock copolymers of poly(ε-caprolactone)-block-poly(glycidyl methacrylate)-block- poly(poly(ethylene glycol)methyl ether methacrylate) (PCL-b-PGMA-b-P(PEGMA)) with fluorescence units. Various experiments like structural characterization, fluorescence properties, cell viability studies, encapsulation studies, measuring cytotoxicity against fibroblasts and bladder cancer cells are performed on these polymeric micelles. All of these results demonstrate that these self-assembled micelles may be promising carriers for intravesical delivery of DOX for bladder cancer therapy.

Synthesis of coumarin-nucleoside conjugates via Huisgen 1,3-dipolar cycloaddition

An efficient synthesis of fluorescent coumarin-nucleoside conjugates via Cu(I) catalysed Huisgen 1,3-dipolar cycloaddition is described. Starting from azidonucleosides and coumarin derivatives, products are obtained in good yields. The fluorescent properties of the newly prepared coumarin-nucleoside conjugates are determined.

Synthesis and Photophysical Studies on N1-(2′-O,4′-C-Methyleneribofurano-nucleoside-3′-yl)-C4-(coumarin-7-oxymethyl)-1,2,3-triazoles

A series of eight N1-(2′-O,4′-C-methylene-β-D-ribofuranonucleoside-3′-yl)-C4-(coumarin-7-oxymethyl)-1,2,3-triazoles have been synthesized by Cu(I)-catalyzed azide-alkyne cycloaddition reaction of 3′-azido-3′-deoxy-2′-O,4′-C-methylene

New fluorescent sensor based on a calix[4]arene bearing two triazole–coumarin units for copper ions: application for Cu2+ detection in human blood serum

A novel fluorescent chemosensor calix[4]arene L, containing two fluorogenic coumarin units at the lower rim has been synthesized via click reaction. The structure of this chemosensor, was characterized by IR, NMR spectra and elemental analysis. Ion-binding properties of L were investigated in acetonitrile with different metal ions and the recognition process was monitored by fluorescence, UV-Vis and 1H NMR spectral changes. In comparison with other metal ions, chemosensor L showed a specific selectivity toward copper ions?. The Job plot analysis revealed that the binding between L with Cu2+ is in 1:1 stoichiometry. The association constant (Ka) for the complex L.Cu2+ was found to be 1.6 × 105?M?1. The limit of detection of the sensor L was determined to be 5.4 × 10?7?M. This sensitive and selective chemosensor was successfully applied for the detection of Cu2+ ions in human blood serum with 90–100% recovery.

Synthesis and pH-responsive self-assembly behavior of a fluorescent amphiphilic triblock copolymer mPEG-b-PCL-b-PDMAEMA-g-PC for the controlled intracellular delivery of doxorubicin

In this work, well-defined pH-responsive methoxy poly(ethylene glycol)-block-poly(ε-caprolactone)-block-poly[2-(dimethylamino)ethyl methacrylate]-g-7-propinyloxy coumarin triblock amphiphilic copolymers (mPEG-b-PCL-b-PDMAEMA-g-PC) were synthesized using a combination of atom transfer radical polymerization (ATRP), ring opening polymerization (ROP) and click chemistry. The chemical structures and compositions of these copolymers were characterized using Fourier transform infrared spectroscopy (FT-IR) and proton nuclear magnetic resonance (1H NMR). The molecular weights of the copolymers were obtained using 1H NMR spectroscopy and gel permeation chromatography (GPC) measurements. Subsequently, the polymers could self-assemble into micelles which were investigated using dynamic light scattering (DLS), transmission electron microscopy (TEM), and fluorescence spectroscopy. The pH-responsive self-assembly behavior of these triblock copolymers in water were investigated at different pH values of 5 and 7.4 for controlled doxorubicin release, the results indicated that the release rate of DOX could be effectively controlled by altering the pH, DOX was sealed in neutral surroundings and DOX release was triggered in acidic surroundings. CCK-8 assays and confocal laser scanning microscopy (CLSM) against HeLa cells indicated that the micelles had no associated cytotoxicity, possessed good biodegradability and biocompatibility, and identified the location of the DOX in HeLa cells. The DOX-loaded micelles possessed high cytotoxicity to HeLa cells and exhibited inhibition of the proliferation of HeLa cells. Moreover, these flexible micelles with an on-off switched drug release may offer a promising pattern to deliver a wide variety of hydrophobic payloads to tumor cells for cancer therapy.

Mitochondria-Targeted Photoactivatable Real-Time Monitoring of a Controlled Drug Delivery Platform

The current anticancer therapies are limited by their lack of controlled spatiotemporal release at the target site of action. We report a novel drug delivery platform that provides on-demand, real-time, organelle-specific drug release and monitoring upon

Novel series of triazole containing coumarin and isatin based hybrid molecules as acetylcholinesterase inhibitors

Novel series of coumarin-triazole and isatin-triazole hybrids were rationally designed, synthesized and biologically evaluated to check their inhibitory potential against acetylcholinesterase enzyme by using in vitro Ellman's method. Most of the hybrid compounds showed significant inhibition against the enzyme. Biological assay revealed that compound B-1 (among 4-hydroxycoumarin-triazole series) and compound AS-8 (from isatin-triazole series) possessed potent inhibitory activity against the AChE with the IC50 values of 110 ± 1.11 nM and 155 ± 1.65 nM, respectively. These active compounds (B-1 and AS-8) exhibited mixed mode of enzyme's inhibition which was confirmed through enzyme kinetic studies. Molecular docking studies were performed to understand the binding modes of these potent compounds within the active pocket of AChE enzyme by using Discovery studio. Furthermore, to predict the stability of the most prominent compound B-1 within the catalytic cavity of AChE, molecular dynamic simulations were performed for 5 ns and was found that ligand and protein complex is stable within their dynamic system. Therefore, these hybrids could be taken as effective lead candidates for further designing, development and optimization of new acetylcholinesterase inhibitors.

Synthesis, antimalarial and antioxidant activity of coumarin appended 1,4-disubstituted 1,2,3-triazoles

A series of coumarin appended triazole hybrids of biotic interest was synthesized through click chemistry approach from the coumarin based terminal alkynes and aromatic azides. All the synthesized triazoles were characterized by FT-IR, 1H NMR,