1,2,3-Triazole scaffolds are not obtained in nature, but they are still intensely investigated by synthetic chemists in various fields due to their excellent properties and green synthetic routes. ...This review will provide a library of all synthetic routes used in the past 21 years to synthesize 1,2,3-triazoles and their derivatives using various metal catalysts (such as Cu, Ni, Ru, Ir, Rh, Pd, Au, Ag, Zn, and Sm), organocatalysts, metal-free as well as solvent- and catalyst-free neat syntheses, along with their mechanistic cycles, recyclability studies, solvent systems, and reaction condition effects on regioselectivity. Constant developments indicate that 1,2,3-triazoles will help lead to future organic synthesis and are useful for creating molecular libraries of various functionalized 1,2,3-triazoles.
A novel nanofabrication technique based on 4-beam interference lithography is presented that enables the preparation of large macroscopic areas (>50 mm2) of perfectly periodic and defect-free ...two-dimensional plasmonic arrays of nanoparticles as small as 100 nm. The technique is based on a special interferometer, composed of two mirrors and a sample with photoresist that together form a right-angled corner reflector. In such an interferometer, the incoming expanded laser beam is split into four interfering beams that yield an interference pattern with rectangular symmetry. The interferometer allows setting the periods of the array from about 220 nm to 1500 nm in both directions independently through the rotation of the corner-reflector assembly around horizontal and vertical axes perpendicular to the direction of the incident beam. Using a theoretical model, the implementation of the four-beam interference lithography is discussed in terms of the optimum contrast as well as attainable periods of the array. Several examples of plasmonic arrays (on either glass or polymer substrate layers) fabricated by this technique are presented.
A novel method enabling rapid fabrication of 2D periodic arrays of plasmonic nanoparticles across large areas is presented. This method is based on the interference of multiple coherent beams ...originating from diffraction of large-diameter collimated beam on a transmission phase mask. Mutual orientation of the interfering beams is determined by parameters of the used phase mask. Herein, parameters of the phase mask (periods and modulation depth) are selected to yield an interference pattern with high contrast and narrow well-separated maxima. Finally, multiple beam interference lithography (MBIL)-based fabrication of periodic plasmonic arrays with selected nanomotifs including discs, disc dimers, rods and bowtie antennas is demonstrated.
A series of N-(4-chlorophenyl) substituted pyrano2,3-cpyrazoles was synthesised and screened for their potential to inhibit kinases and exhibit anticancer activity against primary patient-derived ...glioblastoma 2D cells and 3D neurospheres. A collection of 10 compounds was evaluated against glioma cell lines, with compound 4j exhibiting promising glioma growth inhibitory properties. Compound 4j was screened against 139 purified kinases and exhibited low micromolar activity against kinase AKT2/PKBβ. AKT signalling is one of the main oncogenic pathways in glioma and is often targeted for novel therapeutics. Indeed, AKT2 levels correlated with glioma malignancy and poorer patient survival. Compound 4j inhibited the 3D neurosphere formation in primary patient-derived glioma stem cells and exhibited potent EC
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against glioblastoma cell lines. Although exhibiting potency against glioma cells, 4j exhibited significantly less cytotoxicity against non-cancerous cells even at fourfold-fivefold the concentration. Herein we establish a novel biochemical kinase inhibitory function for N-(4-chlorophenyl) substituted pyrano2,3-cpyrazoles and further report their anti-glioma activity in vitro for the first time.
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Anti-glioma pyrano2,3-cpyrazole 4j inhibited the 3D neurosphere formation in primary patient-derived glioma stem cells. 4j also displayed PKBβ/AKT2 inhibitory activity. 4j is nontoxic towards non-cancerous cells.
In September 2018, an epizootic infection caused by canine distemper virus emerged in an Asiatic lion population in India. We detected the virus in samples from 68 lions and 6 leopards by reverse ...transcription PCR. Whole-genome sequencing analysis demonstrated the virus strain is similar to the proposed India-1/Asia-5 strain.
We report a novel prism-coupled surface plasmon resonance (SPR) biosensor based on special surface plasmon (SP) mode referred to as long-range surface plasmon (LRSP). Utilization of LRSP in ...prism-coupled SPR sensor offers several advantages in comparison with SPR sensors with conventional SPs (cSP) such as extended probe depth of LRSP mode into sensed dielectric and higher sensitivity to the bulk refractive index (RI) changes. The LRSP-supporting multilayer structures and prototype of the sensor setup were prepared. Performance of the LRSP-based sensor was compared to that of the cSP-based sensor in model experiments. LRSP-based sensor was determined to be almost 8 times more sensitive to sample RI changes than the cSP-based sensor. In addition, LRSP-based sensor responses were up to 2.5 and 5.5-fold greater than cSP-based sensor responses for latex beads and the bacterium E. coli HB101P, respectively.
The pyranopyrimidine core is a key precursor for medicinal and pharmaceutical industries due to its broader synthetic applications as well as its bioavailability. Among its four possible isomers, we ...found that 5H-pyrano2,3-dpyrimidine scaffolds have a wide range of applicability, and in recent years, they have been intensively investigated, but the development of the main core is found to be more challenging due to its structural existence. In this review article, we cover all of the synthetic pathways that are employed for the development of substituted 4-aryl-octahydropyrano/hexahydrofuro2,3-dpyrimidin-2-one (thiones) and 5-aryl-substituted pyrano2,3-dpyrimidindione (2-thiones) derivatives through a one-pot multicomponent reaction using diversified hybrid catalysts such as organocatalysts, metal catalysts, ionic liquid catalysts, nanocatalysts, green solvents, catalyst-/solvent-free conditions, and miscellaneous catalysts as well as the mechanism and recyclability of the catalysts. This review mainly focuses on the application of hybrid catalysts (from 1992 to 2022) for the synthesis of 5H-pyrano2,3-dpyrimidine scaffolds. This review will definitely attract the world’s leading researchers to utilize broader catalytic applications for the development of lead molecules.
Proteasome-addicted neoplastic malignancies present a considerable refractory and relapsed phenotype with patients exhibiting drug resistance and high mortality rates. To counter this global problem, ...novel proteasome-based therapies are being developed. In the current study, we extensively characterize TIR-199, a syrbactin-class proteasome inhibitor derived from a plant virulence factor of bacterium Pseudomonas syringae pv syringae. We report that TIR-199 is a potent constitutive and immunoproteasome inhibitor, capable of inducing cell death in multiple myeloma, triple-negative breast cancer, (TNBC) and non-small cell lung cancer lines. TIR-199 also effectively inhibits the proteasome in primary myeloma cells of patients, and bypasses the PSMB5 A49T+A50V bortezomib-resistant mutant. TIR-199 treatment leads to accumulation of canonical proteasome substrates in cells, it is specific, and does not inhibit 50 other enzymes tested in vitro. The drug exhibits synergistic cytotoxicity in combination with proteasome-activating kinase DYRK2 inhibitor LDN192960. Furthermore, low-doses of TIR-199 exhibits in vivo activity by delaying myeloma-mediated bone degeneration in a mouse xenograft model. Together, our data indicates that proteasome inhibitor TIR-199 could indeed be a promising next-generation drug within the repertoire of proteasome-based therapeutics.
Emotion recognition is a significant research topic for interactive intelligence system with the wide range of applications in different tasks, like education, social media analysis, and customer ...service. It is the process of perceiving user's emotional response automatically to the multimedia information by means of implicit explanation. With initiation of speech recognition and the computer vision, research on emotion recognition with speech and facial expression modality has gained more popularity in recent decades. Due to non-linear polarity of signals, emotion recognition results a challenging task. To achieve facial emotion recognition using multimodal signals, an effective Bat Rider Optimization Algorithm (BROA)-based deep learning method is proposed in this research. However, the proposed optimization algorithm named BROA is derived by integrating Bat Algorithm (BA) with Rider Optimization Algorithm (ROA), respectively. Here, the multimodal signals include face image, EEG signals, and physiological signals such that the features extracted from these modalities are employed for the process of emotion recognition. The proposed method achieves better performance against exiting methods by acquiring maximum accuracy of 0.8794, and minimum FAR and minimum FRR of 0.1757 and 0.1806.
Cell volume and its regulation are key factors for cellular integrity and also serve as indicators of various cell pathologies. SPR sensors represent an efficient tool for real-time and label-free ...observations of changes in cell volume and shape. Here, we extend this concept by employing the use of long-range surface plasmons (LRSP). Due to the enhanced penetration depth of LRSP (∼1μm, compared to ∼0.4μm of a conventional surface plasmon), the observation of refractive index changes occurring deeper inside the cells is possible. In this work, the responses of a confluent normal rat kidney (NRK) epithelial cell layer to osmotic stress are studied by both conventional and long-range surface plasmons. Experiments are conducted in parallel using cell layers grown and stimulated under the same conditions to enable direct comparison of the results and discrimination of the osmotic stress-induced effects in different parts of the cell.
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