Synthesis of Benzo[d]imidazo[2,1-b]thiazole-Propenone Conjugates as Cytotoxic and Apoptotic Inducing Agents.

Background: Cancer can be considered as a disease in which normal cells start behaving badly, multiplying uncontrollably, ignoring signals to stop and accumulating to form a mass that is generally termed as a tumor. Apoptosis or programmed cell death is a physiological process that enables organisms to control their cell numbers in many developmental and physiological settings and to eliminate unwanted cells and it plays essential role in chemotherapy-induced tumor-cell killing. The correct balance between apoptosis and inhibition of apoptosis is important in animal development as well as in tissue homeostasis.

Solvent-Assisted Tuning of the Size and Shape of CsPbBr Nanocrystals via Redispersion Process at Ambient Condition.

All-inorganic CsPbBr perovskite nanocrystals are emerging as a new class of semiconductors with outstanding optoelectronic properties and great potential for various applications, such as, lasing, photon detection, photovoltaics, etc. This article provides the effect of solvents on the reprecipitation of CsPbBr perovskite at room temperature. The results observed for CsPbBr perovskite in various antisolvents showed various cubes (nano- to microsized), self-assembly of nanocubes and nanorods.

Aurora kinase B siRNA-loaded lactoferrin nanoparticles potentiate the efficacy of temozolomide in treating glioblastoma.

Aim: To investigate the efficacy of lactoferrin nanoparticles (LfNPs) in delivering siRNA across the blood-brain barrier to treat glioblastoma multiforme (GBM) and with an additional objective of potentiation of conventional temozolomide (TMZ) chemotherapy.

Methods: Aurora kinase B (AKB) siRNA-loaded nanoparticles (AKB-LfNPs) were prepared with milk protein, lactoferrin, by water in oil emulsion method. AKB-LfNPs were tested in cell lines and in GBM orthotopic mouse model with and without TMZ treatment.

Stipulating Low Production Cost Solar Cells All Set to Retail…!

Today's solar cells are exceptionally in demand whilst excess exploitation of natural fossil fuels. In this context, the first and second generation solar cells commercially available in market for more than decades however limitations in production cost and large-scale applications insist to generate inexpensive materials for fabrication. Thereby, organic materials based solar cells explored and emerging as third generation solar cells which possess flexibility, low cost and large-scale applications.

Biotransformation of Artemisinin to 14-Hydroxydeoxyartemisinin: C-14 Hydroxylation by Aspergillus flavus.

The biotransformation of the front-line antimalarial drug, artemisinin (1) by the filamentous fungus Aspergillus flavus MTCC-9167 was investigated. Incubation of compound 1 with A. flavus afforded a new hydroxy derivative (2) along with three known metabolites (3-5).

Operational strategy of high rate anaerobic digester with mixed organic wastes: effect of co-digestion on biogas yield at full scale.

The present research work is aimed at providing an economically feasible solution for the farmers to exploit the mixed organic wastes (MOW) as resources for the generation of biogas based electrical power and utilize the same for irrigation purpose to reduce the dependence on electricity board. A full scale biomethanation plant has been installed based on anaerobic gas lift reactor (AGR) technology to analyse, understand the operational parameters of anaerobic digestion and assess the performance of a high rate biomethanation plant by co-digesting the MOW such as poultry litter (PL), cattle manure (CM) and napier grass (NG) at ambient temperature. The biomethanation plant was incorporated with inline pre and post-processing unit assembly.

IITZ-01, a novel potent lysosomotropic autophagy inhibitor, has single-agent antitumor efficacy in triple-negative breast cancer in vitro and in vivo.

Autophagy is a homeostatic process that recycles damaged organelles and long-lived proteins by delivering them in double-membrane vesicles to lysosomes for degradation. Autophagy has a prominent role in survival, proliferation, and resistance of tumors in metabolic and chemotherapeutic stress conditions. Clinical trials with chloroquine-a known autophagy inhibitor-were unable to achieve complete autophagy inhibition in vivo, warranting the search for more potent autophagy inhibitors.

High Affinity Neutral Bodipy Fluorophores for Mitochondrial Tracking.

We report the first high affinity neutral Bodipy fluorophores for selective imaging of mitochondria with notable sensitivity (∼100 nM) and insignificant cytotoxicity even at very high concentration (∼100 μM), when tested against HeLa cells. Further, these fluorophores are chemically robust and require no special conditions for storage.

What Has Come out from Phytomedicines and Herbal Edibles for the Treatment of Cancer?

Several modern treatment strategies have been adopted to combat cancer with the aim of minimizing toxicity. Medicinal plant-based compounds with the potential to treat cancer have been widely studied in preclinical research and have elicited many innovations in cutting-edge clinical research. In parallel, researchers have eagerly tried to decrease the toxicity of current chemotherapeutic agents either by combining them with herbals or in using herbals alone.

Supplementation of oat (Avena sativa L.) extract abates alcohol-induced acute liver injury in a mouse model.

Dietary supplementation of oats has been associated with reduced risk of cardiovascular disease, diabetes, and gastrointestinal disorders. The role of oat extract as prophylactic in treating acute liver injury is not thoroughly established. We, therefore, hypothesized that oat extract would exert protective effect against alcohol-induced acute liver injury in a mouse model.

Zinc Dependent Histone Deacetylase Inhibitors in Cancer Therapeutics: Recent Update.

Background: Histone deacetylases (HDAC) are an important class of enzymes that play a pivotal role in epigenetic regulation of gene expression that modifies the terminal of core histones leading to remodelling of chromatin topology and thereby controlling gene expression. HDAC inhibitors (HDACi) counter this action and can result in hyperacetylation of histones, thereby inducing an array of cellular consequences such as activation of apoptotic pathways, generation of reactive oxygen species (ROS), cell cycle arrest and autophagy. Hence, there is a growing interest in the potential clinical use of HDAC inhibitors as a new class of targeted cancer therapeutics.

Interleukin-6 induced overexpression of valosin-containing protein (VCP)/p97 is associated with androgen-independent prostate cancer (AIPC) progression.

Though Androgen deprivation therapy (ADT) is effective initially, numerous patients become resistant to it and develop castration resistant PCa (CRPC). Cytokines promotes ligand independent activation of AR. Interleukin-6 (IL-6) levels are elevated in CRPC patients and regulate AR activity.

A fluorene-core-based electron acceptor for fullerene-free BHJ organic solar cells-towards power conversion efficiencies over 10.

A small molecule non-fullerene electron acceptor (SMNFEA), bearing a furan π-spacer and dicyano-n-hexyl rhodanine as flanking groups, was designed and synthesized for organic solar cell applications. Organic photovoltaic devices based on FRdCN2 and PTB7-Th polymer donors exhibited a highly improved efficient power conversion efficiency of 10.7%, which is the highest so far for OSCs fabricated from fluorene-core-based SMNFEAs.

Molecular interaction of novel benzothiazolyl triazolium analogues with calf thymus DNA and HSA-their biological investigation as potent antimicrobial agents.

The binding behaviour between calf thymus DNA and synthesized benzothiazolyl triazolium derivatives as potent antimicrobial agents was explored by means of spectroscopic applications together with molecular docking study at the sub-domain IIA, binding site I of human serum albumin (HSA). Most of the synthesized derivatives presented significant antimicrobial inhibition when compared with the clinical Norfloxacin, Chloromycin, and Fluconazole. In particular, compound 5q presented efficient anti-Bacillus subtilis, anti-Escherichia coli, anti-Salmonella typhi, and anti-Psuedomonas aeruginosa activity with low MIC values of 2-8 μg/mL which were relatively superior to the reference drugs.

Synthesis and biological evaluation of imidazo[2,1-b]thiazole-benzimidazole conjugates as microtubule-targeting agents.

A series of imidazo[2,1-b]thiazole-benzimidazole conjugates were synthesized and evaluated for their antiproliferative activity against four human cancer cell lines i.e.; HeLa (cervical), A549 (lung), MCF-7 (breast) and DU-145 (prostate) along with normal HEK-293 cell line.

Ferulic acid protects lipopolysaccharide-induced acute kidney injury by suppressing inflammatory events and upregulating antioxidant defenses in Balb/c mice.

Sepsis-induced acute kidney injury (AKI) is responsible for 70-80% mortality in intensive care patients due to elevated levels of endotoxin, Lipopolysaccharide (LPS) caused by gram-negative infections. Ferulic acid (FA), a phenolic phytochemical is known for its renal protection on various induced models of nephrotoxicity. However, the curative effect of FA in LPS-induced AKI is not well studied.

Dry anaerobic co-digestion of food waste and cattle manure: Impact of total solids, substrate ratio and thermal pre treatment on methane yield and quality of biomanure.

The objective of the present study is to assess the impact of TS concentration, substrate mixing ratio (co digestion) and thermal pretreatment on biogas production, methane yield, VS reduction (%) and quality of biomanure through dry anaerobic digestion (DAD) of food waste (FW) and cattle manure (CM). Results divulged that the optimum methane yield and biomanure of 0.18 and 0.

Iodine mediated oxidative cross-coupling of unprotected anilines and heteroarylation of benzothiazoles with 2-methylquinoline.

Iodine-promoted oxidative C-H/C-H cross-coupling of unprotected anilines and 2-methylquinoline to furnish C4-carbonylated aniline (4-aminophenyl)(quinoline-2-yl) methanones in moderate to good yields has been demonstrated. This work provides the first site-selective approach for the synthesis of free amino groups containing methanones including unprecedented C-H functionalization rather than the N-H functionalization of unprotected anilines via the Kornblum oxidation of 2-methylquinoline. Furthermore, we noticed that the incorporation of KOH under standard conditions provides 2-heteroarylbenzothiazoles from benzothiazoles and 2-methylquinoline in good to excellent yields.

Evaluation of single and two stage anaerobic digestion of landfill leachate: Effect of pH and initial organic loading rate on volatile fatty acid (VFA) and biogas production.

This work aims to evaluate the impact of pH and initial organic load (IOL) in terms of Chemical Oxygen Demand (COD) of landfill leachate for the production of value added products during single and two stage anaerobic digestion (AD). It was observed that at an optimal IOL of 48 g/L, acetic acid was dominant at pH 5.5 whereas it was butyric acid at pH of 5.

4β-amidotriazole linked podophyllotoxin congeners: DNA topoisomerase-IIα inhibition and potential anticancer agents for prostate cancer.

Topoisomerases (topo-I and topo-II) have occupied a significant role in DNA replication, transcription, and are a promising set of antitumor targets. In the present approach, a series of new 4β-amidotriazole linked podophyllotoxin derivatives (10a-i and 11a-k) were designed, synthesized by employing the click chemistry and their biological activities were evaluated. The majority of derivatives showed promising antiproliferative activity with IC values ranging from 1 to 10 μM on the six human cancer cell lines; cervical (HeLa), breast (MCF-7), prostate (DU-145), lung (A549), liver (HepG2) and colon (HT-29).

Design, synthesis and biological evaluation of 1, 4-dihydro indeno[1,2-c] pyrazole linked oxindole analogues as potential anticancer agents targeting tubulin and inducing p53 dependent apoptosis.

A series of 1, 4-dihydroindeno-[1,2-c] pyrazole linked oxindole conjugates have been synthesized by using Knoevenagel condensation method and further evaluated for their antiproliferative activity against HeLa, A549 and MDA-MB-231 human cancer cell lines along with HEK-293 (normal human embryonic kidney cells). Among the derivatives, compounds 12a, 12b, and 12d showed excellent cytotoxicity with IC values ranging between 1.33 to 4.

Synthesis of benzo[d]imidazo[2,1-b]thiazole-chalcone conjugates as microtubule targeting and apoptosis inducing agents.

A series of benzo[d]imidazo[2,1-b]thiazole-chalcone conjugates (5a-aa) were designed, synthesized and evaluated for their cytotoxic potency against a panel of human cancer cell lines like lung (A-549), breast (MDA MB-231), prostrate (DU-145) and colon cancer (HT-29). Preliminary results revealed that some of these conjugates like 5d and 5u exhibited significant antiproliferative effect against human breast cancer (MDA MB-231) with IC values of 1.3 and 1.

Light induced oxidation of an indoline derived system triggered spherical aggregates.

Indoline based donor-acceptor system (InBT) exhibits a colour transition from pink to orange to yellow in chloroform facilitated by the photo-oxidation of the N,N-dimethyl indoline of InBT and neutralized by chloride counter ions upon light irradiation at short and long range excitation wavelengths of 320 and 500 nm, which leads to spherical aggregates when subjected to methanol vapour diffusion (MVD).

Role of Co-Sensitizers in Dye-Sensitized Solar Cells.

Co-sensitization is a popular route towards improved efficiency and stability of dye-sensitized solar cells (DSSCs). In this context, the power conversion efficiency (PCE) values of DSSCs incorporating Ru- and porphyrin-based dyes can be improved from 8-11 % to 11-14 % after the addition of additives, co-adsorbents, and co-sensitizers that reduce aggregation and charge recombination in the device. Among the three supporting material types, co-sensitizers play a major role to enhance the performance and stability of DSSCs, which is requried for commercialization.

Regioselective oxidative cross-coupling of benzo[d]imidazo[2,1-b]thiazoles with styrenes: a novel route to C3-dicarbonylation.

A novel I promoted, highly efficient metal-free and peroxide-free greener domino protocol for the C3-dicarbonylation of benzo[d]imidazo[2,1-b]thiazoles (IBTs) with styrenes has been developed via oxidative cleavage of the C(sp)-H bond, followed by C3-nucleophilic attack of IBT and oxidation. Interestingly, under these conditions 2-(benzo[d]imidazo[2,1-b]thiazol-2-yl)aniline gave the benzo[4',5']thiazolo[2',3':2,3]imidazo[4,5-c]quinoline derivative via oxidative cleavage of the C(sp)-H bond, followed by Pictet-Spengler cyclization and aromatization. This method offers the advantages of broad substrate scope, ecofriendly feature and high atom economy apart from higher yields.