N-doped carbon nanodots@UiO-66-NH2 as novel nanoparticles for releasing of the bioactive drug, rosmarinic acid and fluorescence imaging.

BACKGROUND AND THE PURPOSE OF THE STUDY: The purpose of the present research was to synthesize affordable nanoparticles for simultaneous drug release and cell fluorescence imaging to decrease the costs associated with conventional treatments. METHODS: In the present study, N-doped carbon nanodots@UiO-66-NH2 nanoparticles were simply synthesized in few steps and were used as a novel carrier for rosmarinic acid (RA). Nano particles were characterized by FT-IR spectroscopy, X-ray powder diffraction (XRD), Dynamic Light Scattering (DLS) and field emission scanning electron microscopy (FE-SEM). UV/vis spectroscopy was used to study the release profile of RA drug from this novel carrier. Methylthiazolyl tetrazolium (MTT) assay was to evaluate the effect of irradiation with a (UV) lamp. Confocal laser scanning microscopy was used for fluorescence imaging of cancer cells. RESULTS: Results of the MTT assay revealed that UiO-66-NH2@N-CNDs nanoparticles as a drug carrier for RA, have an excellent therapeutic effect due to their high quantum yield under irradiation of UV light. On the contrary, the observed therapeutic effect was decreased under ambient light. CONCLUSIONS: UiO-66-NH2@N-CNDs nanoparticles can be considered as promising vehicles for drug delivery due to their cost effectiveness in cancer treatment, based on the results of MTT assay. It should be emphasized that this nanocarrier can be as potential platforms for coincident drug delivery system and cell fluorescence imaging due to possessing green fluorescence and microporosity features. Graphical abstract Graphical abstract.

Simultaneous determination of 6-mercaptopruine, 6-thioguanine and dasatinib as three important anticancer drugs using nanostructure voltammetric sensor employing Pt/MWCNTs and 1-butyl-3-methylimidazolium hexafluoro phosphate.

6-Mercaptopurine, 6-thioguanine and dasatinib are three important anticancer drugs with high adverse effects in human body. In this study, a Pt/MWCNTs-1-butyl-3-methylimidazolium hexafluoro phosphate-modified carbon paste electrode was developed for the simultaneously determination of 6-mercaptopurine, 6-thioguanine and dasatinib for the first time. The Pt/MWCNTs synthesized by polyol method and have been characterized by transmission electron microscopy and X-ray diffraction methods. The obtained data revealed that the electro-oxidation of 6-mercaptopurine, 6-thioguanine and dasatinib is facilitated as a novel voltammetric sensor. After optimization of electrochemical parameters employing this sensor at pH 8.0, the oxidation peak currents for 6-mercaptopurine, 6-thioguanine and dasatinib were found to vary linearly with their concentrations in the range of 0.05-550µM; 0.1-500µM and 5.0-500µM with detection limits of 0.009µM, 0.05µM and 1.0µM respectively using square wave voltammetric method. The modified electrode has been applied for the selective and precise analysis of 6-mercaptopurine, 6-thioguanine and dasatinib in pharmaceutical formulations and urine samples.

Ultrasound-promoted one-pot five-components synthesis of biologically active novel bis((6-alkyl or phenyl-2-phenylpyrimidine-4-yl) oxy) alkane or methyl benzene derivatives.

We have described a synthesis of novel five-component reaction (5-CR) of bis((6-alkyl or phenyl-2-phenylpyrimidine-4-yl) oxy) alkane or methyl benzene derivatives under ultrasound irradiation. A useful ultrasound effect was observed and title products were obtained with high yields after 25-40 min sonication. Structural confirmation and characterization of the products based on the analytical, chemical, and spectral analysis. The results show obviously, that to reach a high efficiency of ultrasonic systems in synthetic chemical processes. Our procedure compared to the conventional heating method has the benefit of higher reaction yields and shorter reaction times. The in vitro antibacterial tests show that some of the target compounds have promising activities. Structure-activity relationships (SAR) were established for the substitutions on the pyrimidine rings and related length of linear chain linker.

A rapid one-pot synthesis of pyrido[2,3-d]pyrimidine derivatives using Brønsted-acidic ionic liquid as catalyst.

Pyrido[2,3-d]pyrimidine derivatives were synthesized regioselectivly in good to high yields by one-pot three-component condensation of 6-amino-2-(methylthio)pyrimidin-4(3H)-one, aromatic aldehydes and ethylcyanoacetate or meldrum's acid using 1,2-dimethyl-N-butanesulfonic acid imidazolium hydrogen sulfate ([DMBSI]HSO4) Brønsted-acidic ionic liquid as catalyst. Solvent-free mild reaction conditions, short reaction times, easy work-up, and reusability of the catalyst are the main advantages of this protocol.

Facile regioselective synthesis of novel bioactive thiazolyl-pyrazoline derivatives via a three-component reaction and their antimicrobial activity.

A series of novel 2-(3,5-diphenyl-4,5-dihydro-1H-pyrazol-1-yl)-4-phenylthiazoles have been prepared by a three-component cyclo-condensation of various chalcones, thiosemicarbazide and phenacyl bromide. The easy work-up of the products, rapid reaction, and mild conditions are notable features of this protocol. The reaction was efficiently catalyzed in one-pot by a few drops of HCl in EtOH under reflux conditions providing the title compounds in moderate to high yields. The antibacterial activity of the selected products was examined. Some products exhibit promising activities.

An expeditious regioselective synthesis of novel bioactive indole-substituted chromene derivatives via one-pot three-component reaction.

Novel fused 1H-benzo[f]chromen-indole derivatives were synthesized regioselectivly in good to high yields by triethyl amine catalyzed condensation of 3-cyanoacetylindoles, ß-naphthol and aryl aldehydes in methanol under ultrasounic irradiations and conventional conditions. The easy work-up of the products, rapidity, and mild reaction conditions are notable features of this protocol. The antibacterial activity of the selected products was examined. Some products showed promising activities.

A convenient ultrasound-promoted regioselective synthesis of fused polycyclic 4-aryl-3-methyl-4,7-dihydro-1H-pyrazolo[3,4-b]pyridines.

Fused polycyclic 4-aryl-3-methyl-4,7-dihydro-1H-pyrazolo[3,4-b]pyridines were obtained in a three-component regioselective reaction of 5-amino-3-methyl-1H-pyrazole, 2H-indene-1,3-dione and arylaldehydes in ethanol under ultrasound irradiation. This rapid method produced the products in short reaction times (4-5min) and excellent yields (88-97%).

An efficient one-pot three-component synthesis of fused 1,4-dihydropyridines using HY-zeolite.

A facile and convenient protocol was developed for the fast (2.5-3.5 h) and high yielding (70-90%) synthesis of fused 1,4-dihydropyridines from dimedone in the presence of HY-zeolite as an efficient recyclable heterogeneous catalyst.

KSF: an efficient catalyst for the regioselective synthesis of 1,5-diaryl pyrazoles using Baylis-Hillman adducts.

A facile and convenient protocol was developed for the regioselective synthesis of 1,5-diarylpyrazoles using Baylis-Hillman adducts over KSF catalyst in high yields (70-90%) and low reaction times.