Novel pyrazole derivatives as inhibitors of Leishmania donovani: an integrated approach combining in vitro analysis and mechanistic insights.

Leishmaniasis is a neglected tropical disease that continues to be a global public health problem, leading to a disastrous impact on poor rural people. The present therapeutic arsenal faces the limitations of drug resistance and toxicity concerns, raising a great need to identify novel chemical scaffolds that are potent, non-toxic, and cost-effective. Heterocycles comprise a distinctive class of molecules exhibiting a wide array of physical, chemical, and biological characteristics and occupy a prominent position in pharmaceutical applications.

Mechanistic Evaluation of Thymoquinone Derivative-Induced Apoptosis in Human Glioblastoma Cells.

Background: Glioblastoma is a highly aggressive brain tumor with limited treatment options, necessitating the development of targeted and effective therapeutics. Thymoquinone (TQ), a natural compound with known anticancer potential, has been modified to enhance its efficacy.

Materials And Methods: A series of TQ derivatives (SS-01 to SS-05) and the parent compound (SS-06) were synthesized and screened for cytotoxic activity using the Sulforhodamine B (SRB) assay against various cancer cell lines-glioblastoma (SNB-19, U251), breast carcinoma (MCF-7, MD-MBA-231), pancreatic carcinoma (MIAPaCa, PANC-1), lung carcinoma (A549), prostate carcinoma (PC3)-and a normal fibroblast cell line (FR2).

Leveraging hybrid model for accurate sentiment analysis of Twitter data.

Sentiment analysis has emerged as a vital tool for gauging public opinion in today's fast-paced digital environment. This study examines the use of advanced artificial intelligence techniques to analyze sentiments derived from Twitter, a leading platform for real-time social media engagement. By utilizing Twitter's vast dataset, the research implements a comprehensive pre-processing pipeline that incorporates natural language processing (NLP) techniques such as tokenization, stop-word removal, and stemming to prepare the textual data for analysis.

Synthesis of benzenesulfonamide tethered pyrazolyl stilbene derivatives: Their anti-proliferative and carbonic anhydrase inhibitory potentials.

A series of twelve benzenesulfonamide tethered pyrazolyl stilbene derivatives (13a- l) were prepared by a two-step synthetic strategy involving the synthesis of dibenzalacetone via Claisen-Schmidt condensation, followed by the tandem one-pot reaction between dibenzalacetone and 4-hydrazine benzene sulphonamide in presence of catalytic iodine. All the synthesized compounds were evaluated for their antiproliferative activity against the NCI panel of 60 human cancer cell lines at a single dose of 10 μM. Among the synthesized compounds, compounds 13e and 13j have demonstrated promising anti-proliferative activity and were further subjected to a comprehensive five-dose assay across an NCI panel of 60 cancer cell lines.

Metabolite profiling and bioactivity of fungal endofauna from Xiphinema nuragicum in the rhizosphere of Withania somnifera.

Gut-associated fungal endofauna confronted with stressful conditions have the potential to secrete diverse bioactive metabolites. In this context, the present study aims to uncover the hidden metabolite profiling of less explored fungal gut parasites associated with rhizosphere nematodes of Withania somnifera. The nematode Xiphinema nuragicum, predominantly found in W.

Cancer odds among Ohio firefighters: data from the Ohio Cancer Incidence Surveillance System (OCISS) 1996-2019.

Objectives: The objective of the current case-control study was to examine the odds of cancer among firefighters in the state of Ohio and compare the odds of being a firefighter versus police or the general population across different cancer types.

Methods: Cancer cases were examined from the Ohio Cancer Incidence Surveillance System (OCISS) between 1996 and 2019. Occupation status was classified as firefighter, police or general population.

A radical approach towards polarity-reversed -substitution of electron-deficient arenes.

We have developed a protocol for polarity-reversed -substitution of electron-deficient arenes. In order to achieve desired reactivity and selectivity for a broad range of substrates, the dual pronged strategy is essential. Furthermore, this approach has also shown promise in perfluoroalkylation of arenes.

Mechanistic Approach into 1,2,3-triazoles-based IIIM(S)-RS98 Mediated Apoptosis in Lung Cancer Cells.

Lung cancer is a major public health problem across the globe, since it is the second most frequent cancer and the leading cause of cancer fatalities. This necessitates careful assessment of current therapies for lung cancer and discovery of novel drug candidates. 1,2,3 triazole compounds have emerged as an important class of prospective chemotherapeutic drugs for the treatment of lung cancer, with promising anti-lung cancer activity shown via a variety of pathways.

Photoinduced stereoselective reactions using pyridinium salts as radical precursors.

Pyridinium salts are amine surrogates that are abundant in nature and the redox active nature of the pyridinium salts allows them to serve as precursors for generating radical species under mild conditions that can be initiated by light, heat or metal catalysis. The stereoselective formation of products has always been a topic of interest for synthetic chemists worldwide. In this context, pyridinium salts can readily undergo single electron reduction to form a neutral radical, and the N-X bond's subsequent fragmentation furnishes the X radical without any harsh reaction conditions.

Discovery of Ring-Annulated Analogues of Cannabidiol as Potential Anticancer Agents: Synthesis and Biological Evaluation.

Cannabidiol (CBD) is a nonpsychoactive cannabinoid derived from and its potential therapeutic effects extend beyond its well-known antiepileptic properties. Exploring CBD and its analogues as anticancer agents has gained significant attention in recent years. In this study, a series of novel ring-annulated analogues of CBD with oxazinyl moiety were synthesized and evaluated for their antiproliferative effect.

Ewing Sarcoma of Temporal bone Presentation as Chronic Otitis Media: A rare Clinical Confusion.

Ewing's Sarcoma is type of malignant round cell neoplasm, representing only 1-4% of all ES cases. Temporal bone ES is often confused with chronic otitis media as clinical picture is quite similar i.e.

Polar-Effect-Directed Control in Site-Selectivity of Radical Substitution Enables C-H Perfluoroalkylation of Coumarins.

A novel Ru-catalyzed protocol for C-7 selective C-H trifluoromethylation of coumarins in the presence of light is presented. This reaction undergoes a radical type nucleophilic substitution instead of a radical type electrophilic substitution owing to the benzocore activation as a result of lowering the lowest unoccupied molecular orbital (LUMO).

Endoscopic ultrasonography-guided coil embolization and cyanoacrylate injection versus cyanoacrylate injection alone for gastric varices: a randomized comparative study.

Background: Bleeding from gastric varices is life-threatening, with significant rebleeding risk despite standard cyanoacrylate glue injection therapy. Our aim was to evaluate the efficacy and safety of endoscopic ultrasonography (EUS)-guided coil embolization with cyanoacrylate injection (Coil+CYA) compared with EUS-guided cyanoacrylate injection alone (CYA) for the treatment of gastric varices.

Methods: The study was conducted at a tertiary referral center in India, using a single-blinded, prospective, and parallel-group randomized design.

Decoding the plant clock: a review of mathematical models for the circadian regulatory network.

Most organisms have evolved specific mechanisms to respond to changes in environmental conditions such as light and temperature over the course of day. These periodic changes in the physiology and behaviour of organisms, referred to as circadian rhythms, are a consequence of intricate molecular mechanisms in the form of transcription and translational feedback loops. The plant circadian regulatory network is a complex web of interconnected feedback loops involving various transcription factors such as CCA1, LHY, PRRs, TOC1, LUX, ELF3, ELF4, RVE8, and more.

Repurposing FDA approved drugs against Sterol C-24 methyltransferase of Leishmania donovani: A dual in silico and in vitro approach.

Leishmaniasis is a disease caused by the parasite Leishmania donovani affecting populations belonging to developing countries. The present study explores drug repurposing as an innovative strategy to identify new uses for approved clinical drugs, reducing the time and cost required for drug discovery. The three-dimensional structure of Leishmania donovani Sterol C-24 methyltransferase (LdSMT) was modeled and 1615 FDA-approved drugs from the ZINC database were computationally screened to identify the potent leads.

Neuroprotective Effects of Cannabispirenone A against NMDA-Induced Excitotoxicity in Differentiated N2a Cells.

The endocannabinoid system is found throughout the central nervous system, and its cannabinoids receptor 1 is critical in preventing neurotoxicity caused by N-methyl-D-aspartate receptor activation (NMDARs). The activity of NMDARs places demands on endogenous cannabinoids to regulate their calcium currents. Endocannabinoids keep NMDAR activity within safe limits, protecting neural cells from excitotoxicity.

Intravenous versus oral 'L-ornithine-L-aspartate' in overt hepatic encephalopathy: a randomized comparative study.

Hepatic encephalopathy (HE), a morbid ordeal affecting chronic liver disease patients always insists for the search of a rational, superior & infallible agent beyond the time-proven standards i.e., Lactulose & Rifaximin.

Photoinduced metal-free trifluoro/perfluoroalkylation of heteroarenes.

A practical and straightforward protocol to access trifluoromethylated/perfluoroalkylated heteroarenes radical-type nucleophilic substitution rather than typical radical-type electrophilic substitution is described here. The substrate scope was observed to be broad and diverse-covering arenes, heteroarenes (containing N, O, S), bioactive cores, and allylic cores. Mechanistic studies confirmed a radical-mediated reaction pathway.

Safety and Efficacy of Ureteroscopic Laser Lithotripsy in the Management of Ureteric Calculi in Pregnancy-Experience of a Tertiary Care Center.

Introduction: Ureteric colic in pregnancy is one of the common non-obstetric reasons for emergency department visits. Ureteric calculi present a significant threat to maternal and fetal health and definitive management often becomes necessary. Our aim is to assess the safety and efficacy of ureteroscopic laser lithotripsy in the management of ureteric stones in pregnancy.

Mini-PCNL - a boon for CKD patients with nephrolithiasis.

Purpose: The prevalence of urinary stone disease in ESRD is 3.2%, leading to renal damage due to obstructive uropathy, infection, and frequent surgical intervention. PCNL, the gold standard for complex renal stone disease, has evolved with smaller access sheaths (14-20 F), improved optics, and fluoroscopic equipments.

Biodiversity and Bioactive Potential of Actinomycetes from Unexplored High Altitude Regions of Kargil, India.

Unlabelled: The effectiveness of currently available antimicrobials and anticancer medications is steadily declining due to the emergence of drug resistance. Since actinobacteria are important producers of bioactive substances, we have isolated them from the soil samples of exotic North-Western Himalayan terrains. Out of 128 isolates, 39 strains were prioritized based on their bioactive potential.

Correction to 1,2,3-Triazole Tethered Hybrid Capsaicinoids as Antiproliferative Agents Active against Lung Cancer Cells (A549).

[This corrects the article DOI: 10.1021/acsomega.2c03325.

Efficacy and Rationale of Endoscopic Ultrasound-Guided Thrombin Injection in Visceral Artery Pseudoaneurysm Not Amenable to Angioembolization.

Background: Pseudoaneurysm usually occurs after vascular injuries or erosions such as in trauma or inflammation like pancreatitis and is associated with high morbidity and mortality.

Aim: The aim of study is to assess efficacy and safety of EUS-guided thrombin injection in pseudoaneurysm.

Materials And Methods: Prospective data collection was done at SMS Hospital, Jaipur, from January 2015 to March 2023.