An Azomethine Derivative, BCS3, Targets XIAP and cIAP1/2 to Arrest Breast Cancer Progression Through MDM2-p53 and Bcl-2-Caspase Signaling Modulation.

: Breast cancer influences more than 2 million women worldwide annually. Since apoptotic dysregulation is a cancer hallmark, targeting apoptotic regulators encompasses strategic drug development for cancer therapy. One such class of apoptotic regulators is inhibitors of apoptosis proteins (IAP) which are a class of E3 ubiquitin ligases that actively function to support cancer growth and survival.

Anticancer and Cyclooxygenase Inhibitory Activity of Benzylidene Derivatives of Fenobam and its Thio Analogues.

Introduction: A series of benzylidene derivatives of fenobam and its thio analogues (1-22) have been evaluated for their cytotoxicity against breast cancer (MCF-7, MDA-MB-231), ovarian cancer (A2780, SKOV-3) and cervical cancer (HELA) cell lines.

Method: These compounds (1-22) exhibited 72-83% inhibition of Erk activity against the ovarian cancer cell line (A2780). Compounds 3 and 20 showed the highest DNA damage effect in Comet Assay against the A2780 cancer cell line as compared to the other tested analogues (4, 8, 11, 12, and 13) by using % Tail DNA and OTM.

Bottom-Up Porous Graphene Synthesis and its Applications.

Incorporation of regular order pores/holes/defects into semimetalic graphene sheets can tune the band gap up to 1 eV or more introducing semiconducting property and therefore exhibiting promising applications for organic electronics such as field-effect transistors (FETs), molecular sieve membranes, gas sensing, catalysis devices, etc. In this mini review, we focused on bottom-up approaches to introduce periodic homogeneous pores into graphene and nanographene and graphene nanoribbons along with their characteristics and potential applications in various fields.

Therapeutic potential of Linn. in systemic lupus erythematosus: Network pharmacology and molecular modeling insights.

Background: Systemic lupus erythematosus is a chronic autoimmune inflammatory disease characterized by multiple symptoms. The phenolic acids and other flavonoids in have anti-oxidants, anti-inflammatory, and immunomodulatory activities that are essential for managing SLE through natural sources. This study employs network pharmacology to unveil the multi-target and multi-pathway mechanisms of as a complementary therapy.

Identification of potent indolizine derivatives against Mycobacterial tuberculosis: In vitro anti-TB properties, in silico target validation, molecular docking and dynamics studies.

In the current study, two sets of compounds: (E)-1-(2-(4-substitutedphenyl)-2-oxoethyl)-4-((hydroxyimino)methyl)pyridinium derivatives (3a-3e); and (E)-3-(substitutedbenzoyl)-7-((hydroxyimino)methyl)-2-substitutedindolizine-1-carboxylate derivatives (5a-5j), were synthesized and biologically evaluated against two strains of Mycobacterial tuberculosis (ATCC 25177) and multi-drug resistant (MDR) strains. Further, they were also tested in vitro against the mycobacterial InhA enzyme. The in vitro results showed excellent inhibitory activities against both MTB strains and compounds 5a-5j were found to be more potent, and their MIC values ranged from 5 to 16 μg/mL and 16-64 μg/mL against the M.

Laser Melting of Mechanically Alloyed FeNi: A Study of the Correlation between Microstructure and Texture with Magnetic and Physical Properties.

The current study attempts to establish the interrelation between microstructure and magnetic properties induced during laser melting of the FeNi alloy. This study demonstrates the optimization of laser parameters for defect-free, uniform, and chemically homogeneous FeNi alloy synthesis. Mechanically alloyed FeNi (50-50 atom %) powders obtained after 12 and 24 h milling, with average particle sizes of 15 and 7 μm, were used as starting materials.

Bottom-Up Synthesis of Twisted Porous Graphene through a Heterogeneous Scholl Reaction and Its Supercapacitor Application.

Anthracene- and pyrene-based twisted porous graphene () with an ordered pore structure has been synthesized through bottom-up solution phase synthesis from a conjugated microporous polymer () via a heterogeneous Scholl cyclization reaction. The regular-ordered pores embedded within the graphene structures were analyzed through a Raman spectrum, different morphological analyses, and theoretical studies. A significant change in surface area from to was observed, from 143 to 640 m/g, respectively.

Synthesis, characterization and larvicidal studies of ethyl 3-benzoyl-7-(piperidin-1-yl)indolizine-1-carboxylate analogues against and cheminformatics approaches.

According to WHO, in 2021, there was an estimation of 247 million malaria cases from 84 malaria-endemic countries. Globally an estimated count of 2 billion malaria cases and 11.7 million deaths due to malaria were recorded in the past two decades.

Easy Access to Sauropunols A-D: Synthesis and Spectroscopy Correlation of Their Natural Methyl and Ethyl Glycosides.

3,6-Anhydro-2-deoxy-hexofuranoside, the natural product core, is present in natural sauropunols (A-D) and in their natural methyl and ethyl glycosides, now, namely, sauropunol H and sauropunol F. The easily synthesized d-glucose-derived 3,6-anhydro-1,2--isopropylidene-5--benzoyl-α-d-glucofuranose was elaborated to final targets employing the TsOH·HO-catalyzed glycosylation reaction with seven different alcohols, subsequent radical deoxygenation, and appropriate deprotection reactions involving mild conditions with excellent functional group tolerance. A short total synthesis of sauropunols (A-D), sauropunol H, and the first total synthesis of sauropunol F are reported herein.

Suppression of mTOR Expression by siRNA Leads to Cell Cycle Arrest and Apoptosis Induction in MDA-MB-231 Breast Cancer Cells.

Background: Mammary carcinogenesis, being ranked second in cancer-related mortality and the inadequacy of existing chemotherapy advocates the development of a novel treatment approach targeting its molecular signalling. Hyperactivation of mammalian target of rapamycin (mTOR) has a critical role in developing invasive mammary cancer and it can be a potential target.

Objective: This experiment was to explore the efficacy of mTOR-specific siRNA on therapeutic targeting of the mTOR gene, assess its proficiency in suppressing in vitro breast cancer and determine underlying molecular mechanisms.

Evaluating the climatic and socio-economic influences on the agricultural drought vulnerability in Jharkhand.

Environmental hazards like drought lead to degrading food production and adversely impact the agro-economy. This study investigates the contributions of different climatic and socio-economic variables to agricultural drought in Jharkhand. The three primary criteria, i.

Therapeutic silencing of mTOR by systemically administered siRNA-loaded neutral liposomal nanoparticles inhibits DMBA-induced mammary carcinogenesis.

Background: Mammary carcinogenesis possesses great challenges due to the lack of effectiveness of the multiple therapeutic options available. Gene therapy-based cancer treatment strategy provides more targeting accuracy, fewer side effects, and higher therapeutic efficiency. Downregulation of the oncogene mTOR by mTOR-siRNA is an encouraging approach to reduce cancer progression.

Structural basis of Omicron immune evasion: A comparative computational study.

Background: The vaccines used against SARS-CoV-2 by now have been able to develop some neutralising antibodies in the vaccinated population and their effectiveness has been challenged by the emergence of the new strains with numerous mutations in the spike protein of SARS-CoV-2. Since S protein is the major immunogenic protein of the virus which contains Receptor Binding Domain (RBD) that interacts with the human Angiotensin-Converting Enzyme 2 (ACE2) receptors, any mutations in this region should affect the neutralisation potential of the antibodies leading to the immune evasion. Several variants of concern of the virus have emerged so far, amongst which the most critical are Delta and recently reported Omicron.

Cascaded adaptive integral backstepping sliding mode and super-twisting controller for twin rotor system using bond graph model.

This work presents a bond graph (BG) model and a robust cascaded controller for a twin-rotor system (TRS). The BG model accounts for all the energetic and dynamical couplings. An adaptive integral backstepping sliding mode (AIBSM) controller is used in the outer loop to control the slow yaw and pitch dynamics of the mechanical sub-system whereas a higher-order sliding mode (HOSM) observer-based super-twisting algorithm (STA) controller is used in the inner loop to control the fast electromechanical actuator dynamics.

Improved NDVI based proxy leaf-fall indicator to assess rainfall sensitivity of deciduousness in the central Indian forests through remote sensing.

Quantifying the leaf-fall dynamics in the tropical deciduous forest will help in modeling regional energy balance and nutrient recycle pattern, but the traditional ground-based leaf-fall enumeration is a tedious and geographically limited approach. Therefore, there is a need for a reliable spatial proxy leaf-fall (i.e.

Molecular Docking and Cognitive Impairment Attenuating Effect of Phenolic Compound Rich Fraction of Trianthema portulacastrum in Scopolamine Induced Alzheimer's Disease Like Condition.

Dementia is considered as the frequent cause of neurodegenerative mental disorder such as Alzheimer's disease (AD) amongst elderly people. Free radicals as well as cholinergic deficit neurons within nucleus basalis magnocellularis demonstrated to attribute with aggregation of β amyloid which further acts as an essential hallmark in AD. Various phenolic phytoconstituents exists in Trianthema portulastrum (TP) leaves have been reported as active against various neurological disorders.

Daphnetin inhibits TNF-α and VEGF-induced angiogenesis through inhibition of the IKKs/IκBα/NF-κB, Src/FAK/ERK1/2 and Akt signalling pathways.

Coumarins, identified as plant secondary metabolites possess diverse biological activities including anti-angiogenic properties. Daphnetin (DAP), a plant derived dihydroxylated derivative of coumarin has shown significant pharmacological properties such as anticancer, anti-arthritic and anti-inflammatory. The present study was performed to investigate the anti-angiogenic potential of DAP, focusing on the mechanism of action.

Characterization of forced degradation products and in silico toxicity prediction of Sofosbuvir: A novel HCV NS5B polymerase inhibitor.

Sofosbuvir is a direct acting antiviral medication used to treat Hepatitis C viral infection. The present study focuses on the degradation behavior of the drug under various stress conditions (hydrolysis, oxidative, thermal and photolytic) as per International Conference on Harmonization (ICH Q1A (R2)) guidelines. A high performance liquid chromatographic system (HPLC) was used to develop a selective, precise and accurate method for separating all the degradation products.

Effect of Dendrophthoe falcata (L.f.) Ettingsh on female reproductive system in Wistar rats: a focus on antifertility efficacy.

Background: This study was designed to assess the effect of one traditionally used antifertility plant, Dendrophthoe falcata (L.f.) Ettingsh (Loranthaceae), on female reproductive system, fertility and safety, by oral administration to adult female Wistar rats.