Contribution of Knoevenagel Condensation Products toward the Development of Anticancer Agents: An Updated Review

Knoevenagel condensation is an entrenched, prevailing, prominent arsenal following greener principles in the generation of α, β-unsaturated ketones/carboxylic acids by involving carbonyl functionalities and active methylenes. This reaction has proved to be a major driving force in many multicomponent reactions indicating the prolific utility toward the development of biologically fascinating molecules. This eminent reaction was acclimatised on different pharmacophoric aldehydes (benzimidazole, β-carboline, phenanthrene, indole, imidazothiadiazole, pyrazole etc.) and active methylenes (oxindole, barbituric acid, Meldrum's acid, thiazolidinedione etc.) to generate the library of chemical compounds. Their potential was also explicit to understand the significance of functionalities involved, which thereby evoke further developments in drug discovery. Furthermore, most of these reaction products exhibited remarkable anticancer activity in nanomolar to micromolar ranges by targeting different cancer targets like DNA, microtubules, Topo-I/II, and kinases (PIM, PARP, NMP, p300/CBP) etc. This review underscores the efficiency of the Knoevenagel condensation explored in the past six-year to generate molecules of pharmacological interest, predominantly toward cancer. The present review also provides the aspects of structure-activity relationships, mode of action and docking study with possible interaction with the target protein.     

Effect of B-site doping on electrical conductivity of YAlO3 based electrolytes for solid oxide fuel cells

Journal of Electroceramics - Solid oxide fuel cells (SOFCs) have emerged as high temperature fuel cell technology operating at temperatures around 1000 °C. Lowering the operating...     

Classification of Foot Pressure Images Using Machine Learning Algorithm

Arthritis is an acute systemic disease of a joint accompanied by pain. In developed countries, it mainly causes disability among people over 50 years of age. Rheumatoid Arthritis is a type of arthritis that occurs commonly among elders. The incidence of arthritis is higher in females than in males. There is no permanent diagnosis method for arthritis, but if it was identified in the early stages based on the foot pressure, it can be diagnosed before attaining the critical stage of Rheumatoid Arthritis. The analysis and study of arthritis patients were done using design thinking methodology. Design thinking is a problem-solving methodology that is used to find a solution for the identification of the early stage of arthritis. This process consists of five stages follows Empathy, Define, Ideate, Prototype, and Testing. To define the problem statement, the Empathy was done with the arthritis patients to know the difficulties faced by them. This paper proposes a measurement technique of early measurement of arthritis using a non-invasive technique. It helps us to detect arthritis using a foot pressure pad that was designed with piezoresistive material and the feature classification was done using Weka.     

Magnetocaloric Effect,Magnetic Interactions and Phase Transition in La1.3Fe11.6-xSi1.4Gax Alloys

Journal of Superconductivity and Novel Magnetism - La1.3Fe11.6-xSi1.4Gax (x?=?0.1, 0.3, 0.5) alloys were prepared by arc-melting. Structural studies show the presence of 1:13 as the...     

Rapid phytochemical microwave-assisted synthesis of zinc oxide nano flakes with excellent electrocatalytic activity for non-enzymatic electrochemical sensing of uric acid

Journal of Materials Science: Materials in Electronics - In the current research work, the author synthesized Zinc oxide (ZnO) NPs using crude black pepper (Piper nigrum) seed extract as a...     

Preparation and characterization of electrospun SiO2 nanofibers

The objective of this study was to prepare and characterize electrospun SiO2 nanofibers for composite (particularly dental composite) applications. We investigated (1) tetraethyl orthosilicate (TEOS) as the alkoxide precursor, (2) polyethylene oxide (PEO) and polyvinyl pyrrolidone (PVP) as the carrying polymers, (3) several solvents for making the spin dopes, and (4) the morphological and structural properties of the electrospun SiO2 nanofibers and their relationship with the pyrolysis temperatures. We also investigated the morphology durability of the prepared SiO2 nanofibers by subjecting them to vigorous ultrasonic vibrations. The results indicated that the uniform (beads-free) amorphous SiO2 nanofibers with an average diameter of approximately 500 nm were successfully prepared. These SiO2 nanofibers also retained their overall fiber morphology when subjected to vigorous ultrasonic vibrations. The electrospun SiO2 nanofibers were, therefore, nano-scaled glass (amorphous SiO2) fibers, and could be used for reinforcement of dental composites.     

Design and Synthesis of DNA‐Interactive β‐Carboline–Oxindole Hybrids as Cytotoxic and Apoptosis‐Inducing Agents

A new series of (E)‐3‐[(1‐aryl‐9H‐pyrido[3,4‐b]indol‐3‐yl)methylene]indolin‐2‐one hybrids were synthesized and evaluated for their in vitro cytotoxic activity against a panel of selected human cancer cell lines, namely, HCT‐15, HCT‐116, A549, NCI‐H460, and MCF‐7, including HFL. Among the tested compounds, (E)‐1‐benzyl‐5‐bromo‐3‐{[1‐(2,5‐dimethoxyphenyl)‐9H‐pyrido[3,4‐b]indol‐3‐yl]methylene}indolin‐2‐one ( 10 s ) showed potent cytotoxicity against HCT‐15 cancer cells with an IC₅₀ value of 1.43±0.26 μm and a GI₅₀ value of 0.89±0.06 μm . Notably, induction of apoptosis by 10 s on the HCT‐15 cell line was characterized by using different staining techniques, such as acridine orange/ethidium bromide (AO/EB) and DAPI. Further, to understand the mechanism of anticancer effects, various assays such as annexin V‐FITC/PI, DCFDA, and JC‐1were performed. The flow cytometric analysis revealed that compound 10 s arrests the HCT‐15 cancer cells at the G0/G1 phase of the cell cycle. Additionally, western blot analysis indicated that treatment of 10 s on HCT‐15 cancer cells led to decreased expression of anti‐apoptotic Bcl‐2 and increased protein expression of both pro‐apoptotic Bax and caspase‐3, ‐8, and ‐9, and cleaved PARP with reference to actin. Next, a clonogenic assay revealed the inhibition of colony formation in HCT‐15 cancer cells by 10 s in a dose‐dependent manner. Moreover, upon testing on normal human lung cells (HFL), the compounds were observed to be safer with a low toxicity profile. In addition, viscosity and molecular‐docking studies showed that compound 10 s has typical intercalation with DNA.     

Mechanical and Thermal Properties Modeling,Sorption Characteristics of Multiscale (Multiwalled Carbon Nanotubes/Glass Fiber) Filler Reinforced Polypropylene Composites

The present work was aimed to investigate the individual and hybrid reinforcement effect of multiscale fillers [glass fibers (GF)/multiwalled carbon nanotubes (MWCNTs)] in polypropylene (PP) matrix. The MWCNT content in the hybrid composites was varied from 0.5 to 5 wt%, and glass fiber fraction was fixed as 20 wt%. The morphology of nano and hybrid composite revealed reasonable dispersion of MWCNTs and glass fibers in the matrix. At a MWCNT content of 3 wt%, the optimum tensile properties for the hybrid composites were achieved and beyond which it declined due to agglomeration effects as revealed by transmission electron microscopy. A comparative study of the experimental and predicted values of moduli of nano, micro, and hybrid composites using various micromechanical models was conducted. The simultaneous incorporation of MWCNTs and glass fibers in PP restricted the mobility of polymer chains as indicated by the increase in storage modulus and rise in glass transition temperature obtained by dynamic mechanical analysis. The differential scanning calorimetry studies indicated that the inclusion of 2 wt% of MWCNTs increased the crystallinity of PP from 58.2 to 69.1% in hybrid composites. The Avrami and Mo models were used to explore nonisothermal crystallization kinetics, and Mo model was in close agreement with the experimental results. The sorption behavior of the composites revealed that the formation of immobilized regions developed by the simultaneous inclusion of micro and nano fillers delayed the transport of the solvent. J. VINYL ADDIT. TECHNOL., 25:E94–E107, 2019. © 2019 Society of Plastics Engineers     

A methodology to estimate source-specific aerosol radiative forcing

This paper presents a novel approach to estimate source-specific radiative forcing by combining source apportionment results for particulate matter mass with satellite (moderate resolution imaging spectroradiometer (MODIS)) derived aerosol optical depth (AOD). Positive matrix factorization (PMF) was applied to particulate matter (PM) mass and its chemical constituents measured during a winter intensive study (December 2004) at Hisar, Haryana, India. The model resolved four factors including carbonate rich dust, combustion rich aerosol, secondary sulfate/nitrate, and an unidentified factor likely to be emission from polymer industries. Carbonate rich dust was the highest contributor to the measured PM mass closely followed by combustion rich aerosol with their average contributions accounting for 34.0% and 33.6%, respectively. Model apportioned species concentrations corresponding to each factor were then used to estimate factor specific optical and radiative properties, and radiative transfer calculations were performed for the shortwave regime. During the study period, although carbonate rich dust and combustion rich aerosol mass contributions were comparable, carbonate rich dust contributed to only 22% of top of the atmosphere forcing while combustion rich aerosol contributed nearly 56%. Overall, the results suggested that the aerosol radiative forcing was primarily governed by the aerosol optical and radiative properties, while the mass concentrations played a secondary role.