Nanoparticles of a Pyrazolo-Pyridazine Derivative as Potential EGFR and CDK-2 Inhibitors: Design, Structure Determination, Anticancer Evaluation and In Silico Studies.

The strategic planning of this study is based upon using the nanoformulation method to prepare nanoparticles and of the previously prepared 4,5-diphenyl-1-pyrazolo[3,4-]pyridazin-3-amine () after confirming its structure with single crystal X-ray analysis. These nanoparticles exhibited promising cytotoxic activity against HepG-2, HCT-116 and MCF-7 cancer cell lines in comparison with the reference doxorubicin and the original derivative . Moreover, their inhibitory assessment against EGFR and CDK-2/cyclin A2 displayed improved and more favorable impact than the parent and the references.

Effective screen-printed potentiometric devices modified with carbon nanotubes for the detection of chlorogenic acid: application to food quality monitoring.

All-solid state screen-printed electrodes were fabricated for chlorogenic acid (CGA) detection. The screen-printed platforms were modified with multi-walled carbon nanotubes (MWCNTs) to work as a lipophilic solid-contact transducer. The sensing-membrane was plasticized with a suitable solvent mediator and incorporating [Ni(bathophenanthroline)][CGA] complex as a sensory material.

Low-cost potentiometric paper-based analytical device based on newly synthesized macrocyclic pyrido-pentapeptide derivatives as novel ionophores for point-of-care copper(ii) determination.

A simple, cost-effective, portable and disposable paper-based analytical device is designed and fabricated for copper(ii) determination. All solid-state ion-selective electrodes (ISEs) for copper and a Ag/AgCl reference electrode were constructed and optimized on the paper substrate. The copper electrodes were built using carbon nano-tube ink as a conductive substrate and an ion-to electron transducer.

Correction: Integrated all-solid-state sulfite sensors modified with two different ion-to-electron transducers: rapid assessment of sulfite in beverages.

[This corrects the article DOI: 10.1039/D0RA09903A.].

Antiproliferative Activity of Some Newly Synthesized Substituted Nicotinamides Candidates Using Pyridine-2(1) thione Derivatives as Synthon.

Some new pyridinethione and thienopyridine derivatives have been synthesized and evaluated for their antiproliferative activity using the MTT assay. Nicotinamide derivatives have been synthesized and used for the preparation of new condensed thieno [2,3-]pyridines by their reactions with active halo compounds. Finally the synthesized thienopyridine underwent ring closure whenever possible through boiling in a solution of sodium ethoxide.

New Benzimidazole-, 1,2,4-Triazole-, and 1,3,5-Triazine-Based Derivatives as Potential EGFR and EGFR Inhibitors: Microwave-Assisted Synthesis, Anticancer Evaluation, and Molecular Docking Study.

A new series of benzimidazole, 1,2,4-triazole, and 1,3,5-triazine derivatives were designed and synthesized using a microwave irradiation synthetic approach utilizing 2-phenylacetyl isothiocyanate as a key starting material. All the new analogues were evaluated as anticancer agents against a panel of cancer cell lines utilizing doxorubicin as a standard drug. Most of the tested derivatives exhibited selective cytotoxic activity against MCF-7 and A-549 cancer cell lines.

Paper-Based Potentiometric Device for Rapid and Selective Determination of Salicylhydroxamate as a Urinary Struvite Stone Inhibitor.

Novel paper-based potentiometric platforms for rapid, cost-effective, and simple determination of the salicylhydroxamic acid (SHAM) drug are presented. Both the SHAM sensor and the reference Ag/AgCl electrode were integrated together on the miniaturized paper platforms. The ion-sensing membrane for the presented sensor is based on the use of Sn-tetraphenylporphyrin (SnTPP) as a charged carrier within a plasticized poly(vinyl chloride) (PVC) matrix.

Paper-Based Potentiometric Sensors for Nicotine Determination in Smokers' Sweat.

Herein, we describe for the first time, the design and fabrication of a novel nicotine paper-based sensor, in which a miniaturized paper reference electrode is integrated for potentiometric measurements. The paper-based sensors were designed using printed wax barriers to define the electrochemical cell and the sample zones. The electrodes were based on the use of the ion association complexes of the nicotinium cation (Nic) with either tetraphenylborate (TPB) or 5-nitrobarbiturate (NB) counter anions as sensing materials for nicotine recognition.

All-Solid-State Potentiometric Ion-Sensors Based on Tailored Imprinted Polymers for Pholcodine Determination.

In recent times, the application of the use of ion-selective electrodes has expanded in the field of pharmaceutical analyses due to their distinction from other sensors in their high selectivity and low cost of measurement, in addition to their high measurement sensitivity. Cost-effective, reliable, and robust all-solid-state potentiometric selective electrodes were designed, characterized, and successfully used for pholcodine determination. The design of the sensor device was based on the use of a screen-printed electrode modified with multiwalled carbon nanotubes (MWCNTs) as a solid-contact transducer.

Design, synthesis and molecular docking of new pyrazole-thiazolidinones as potent anti-inflammatory and analgesic agents with TNF-α inhibitory activity.

A new set of derivatives bearing pyrazole-methylenehydrazono-thiazolidinone scaffold 4-23 was designed, synthesized and confirmed by different spectroscopic means and elemental analyses. In-vivo anti-inflammatory and ulcerogenic evaluation was performed for all the newly synthesized derivatives using indomethacin, celecoxib and diclofenac as standard drugs. The compounds 5, 10, 15, 17, 21, 22 appeared to be the most promising candidates producing rapid onset and long duration of anti-inflammatory activity as well as promising GIT safety profile.

Paper-based potentiometric sensing devices modified with chemically reduced graphene oxide (CRGO) for trace level determination of pholcodine (opiate derivative drug).

Robust, reliable and cost-effective paper-based analytical device for potentiometric pholcodine (opiate derivative drug) ion sensing has been prepared and characterized. A printed pholcodinium (PHL)/5-nitrobarbiturate (NB) ion-association complex as a sensory material-based all-solid-state ion-selective electrode (ISE) on a chemically reduced graphene oxide (CRGO) solid-contact, and a printed all-solid-state Ag/AgCl reference electrode, has been combined on a hydrophobic paper substrate coated with fluorinated alkyl silane (CF(CF)CHCHSiCl, C ). The sensors revealed a potentiometric slope of 28.

Antiproliferative Activity of Some Newly Synthesized Substituted Pyridine Candidates Using 4-(Aaryl)-6-(naphthalen-1-yl)-2-oxo-1,2-dihydropyridine-3-carbonitrile as Synthon.

Herein, we used nicotinonitrile derivatives , as scaffolds to build novel and active antineoplastic agents. The reaction of nicotinonitrile derivatives , with POCl/PCl and/or hydrazine hydrate afforded 2-chloropyridones , and 2-hydrazinyl nicotinonitrile derivatives ,, respectively, as building blocks for various heterocyclic compounds. The structures of all of the synthesized heterocycles were elucidated from their spectral and elemental analyses.

Synthesis and Characterization of Macrocyclic Chiral Tröger's Base Phenhomazine Candidates as Anticancer Agent.

1,4,7,10-Tetraoxa[10](2,8)trögerophane was synthesized from its corresponding precursors. Heating of with p-nitrophenoxide afforded bis(p-nitrophenyl)ether , which was treated with hydrazine hydrate to give bis(p-aminophenyl)ether . Treatment of with paraformaldehyde and triflouroacetic anhydride gave trögerophane .

An all-solid-state potentiometric sensor modified with multi-walled carbon nanotubes (MWCNTs) for silicate assessment and water-quality testing.

A simple and cost-effective approach is proposed for silicate ion determination. The approach is based on designing an all-solid-state potentiometric sensor. The plasticized polyvinyl chloride (PVC) membrane sensor is based on the ion-association complex [Ni(bphen)][SiO] as a sensory recognition material.

Synthesis and Characterization of New Dihydronaphthalene Candidates as Potent Cytotoxic Agents against MCF-7 Human Cancer Cells.

In the present work, a new series of dihydronaphthalene derivatives were synthesized starting with 6-methoxy-1-tetralone , and the corresponding hydrazine derivative . Reaction of compound with aryl isothiocyanates produced thiosemicarbazides , which were reacted with ethyl chloroacetate to give thiazolidinone derivatives . Pyrano thiazolecarbonitrile derivatives - were prepared by heating a mixture of compounds or , aryl aldehydes, and malononitrile utilizing distilled water in the presence of catalytic amount of potassium hydrogen phthalate.

Solid-State Membrane Sensors Based on Man-Tailored Biomimetic Receptors for Selective Recognition of Isoproturon and Diuron Herbicides.

Solid-contact ion-selective electrodes (SC-ISEs) have shown great potential for routine and portable ion detection. The introduction of nanomaterials as ion-to-electron transducers and the adoption of different performance-enhancement strategies have significantly promoted the development of SC-ISEs. Herein, new solid-contact ion-selective electrodes, along with the implementation of multiwalled carbon nanotubes (MWCNTs) as ion-to-electron transducers and potassium tetrakis (p-chlorophenyl) borate (KTpClB) as lipophilic ionic additives, were presented for the detection of isoproturon (IPU) and diuron (DU) herbicides.

Validated Reversed-Phase Liquid Chromatographic Method with Gradient Elution for Simultaneous Determination of the Antiviral Agents: Sofosbuvir, Ledipasvir, Daclatasvir, and Simeprevir in Their Dosage Forms.

A simple, rapid, sensitive, and precise reversed-phase liquid chromatographic method was developed and validated for the simultaneous determination of four direct-acting antivirals, sofosbuvir (SF), ledipasvir (LD), declatasvir (DC), and simeprevir (SM), in their respective pharmaceutical formulations. Effective chromatographic separation was achieved on an Agilent Eclipse plus C8 column (250 mm × 4.6 mm, 5 µm) at 40 °C with gradient elution using a mobile phase composed of acetonitrile:phosphate buffer (pH 6.

Novel Validated Analytical Method Based on Potentiometric Transduction for the Determination of Citicoline Psychostimulant/Nootropic Agent.

Herein, a novel validated potentiometric method is presented for the first time for citicoline determination. The method is based on measuring the potential using new constructed citicoline electrodes. The electrodes are based on the use of citicolinium/phosphomolybdate [Cit][PM] (sensor I) and citicolinium/tetraphenylborate [Cit][TPB] (sensor II) ion association complexes.

Novel heterocyclic hybrids of pyrazole targeting dihydrofolate reductase: design, biological evaluation and studies.

A novel series of pyrazole analogues including hydrazones, pyrazolo[4,3-]-pyridazines, pyrazolo[3,4-][1,2,4]triazine and pyrazolo[3,4-][1,2,3]triazoles was designed, synthesised and screened for their antimicrobial and DHFR inhibition activity. Compounds bearing benzenesulphonamide moiety incorporated with 3-methyl-5-oxo-1-pyrazol-4(5)-ylidene) hydrazine or 6-amino-7-cyano-3-methyl-5-pyrazolo[4,3-]pyridazine revealed excellent and broad spectrum antimicrobial activity comparable to ciprofloxacin and amphotericin B as positive antibiotic and antifungal controls, respectively. Furthermore, these derivatives proved to be the most active DHFR inhibitors with IC values 0.

Liquid Contact-Selective Potentiometric Sensor Based on Imprinted Polymeric Beads Towards 17β-Estradiol Determination.

Novel potentiometric devices "ion-selective electrodes (ISEs)" were designed and characterized for the detection of 17β-estradiol (EST) hormone. The selective membranes were based on the use of man-tailored biomimics (i.e.

A New Validated Potentiometric Method for Sulfite Assay in Beverages Using Cobalt(II) Phthalocyanine as a Sensory Recognition Element.

A simple potentiometric sensor is described for accurate, precise, and rapid determination of sulfite additives in beverages. The sensor is based on the use of cobalt phthalocyanine as a recognition material, dispersed in a plasticized poly(vinyl chloride) matrix membrane. -Nitrophenyl octyl ether (-NPOE) as a membrane solvent and tri-dodecylmethyl- ammonium chloride (TDMAC) as ion discriminators are used as membrane additives.

Solid-Contact Potentiometric Sensors Based on Stimulus-Responsive Imprinted Polymers for Reversible Detection of Neutral Dopamine.

Herein, we present for the first time a novel potentiometric sensor based on the stimulus-responsive molecularly imprinted polymer (MIP) as a selective receptor for neutral dopamine determination. This smart receptor can change its capabilities to recognize according to external environmental stimuli. Therefore, MIP-binding sites can be regenerated in the polymeric membrane by stimulating with stimulus after each measurement.

Synthesis, Antimicrobial Activity and Molecular Docking of Novel Thiourea Derivatives Tagged with Thiadiazole, Imidazole and Triazine Moieties as Potential DNA Gyrase and Topoisomerase IV Inhibitors.

To develop new antimicrobial agents, a series of novel thiourea derivatives incorporated with different moieties was designed and synthesized and their biological activities were evaluated. Compounds , and exhibited excellent antimicrobial activity against all Gram-positive and Gram-negative bacteria, and the fungal with minimum inhibitory concentration (MIC) values ranged from 0.95 ± 0.