Oxo-Sulfonylation of 1,7-Enynes via a Multicomponent Oxidative Radical Polar Crossover Approach.

Diastereoselective synthesis of -3,4-difunctionalized tetrahydroquinoline and chromane derivatives via the oxo-sulfonylation of 1,7-enynes is demonstrated. The reaction involves a three-component oxidative radical polar crossover (ORPC) approach wherein a vinyl carbocation intermediate undergoes nucleophilic substitution to afford the corresponding keto functional group. Deprotection of the N-Ts group, gram-scale synthesis, and other synthetic applications were illustrated.

A Review on zerumbone and its semisynthetic Analogs: Synthesis and Implications in Medicinal chemistry.

Natural products and their semisynthetic analogs have long standing history in generating and identifying lead and drug candidates for various therapeutic areas. Zerumbone 1, a unique 11 membered monocyclic sesquiterpene natural product is isolated from Zingiber zerumbet (L. Smith) and related species.

Spatio-temporal localization of P21-activated kinase in endometrial cancer.

Endometrial cancer is the sixth most common gynecologic cancer, and has been reported as a malignancy arising due to the idiopathic effects of certain anticancer agents. Tamoxifen is the drug of choice in ER-positive breast cancer, and several studies have shown better disease-free survival in these patients. However, the long-term usage of tamoxifen has been associated with resistance and risk for endometrial malignancy.

Protective Effect of Sulfur-Containing Heterocyclic Analogs Against Acrylamide-Induced Behavioral and Biochemical Alterations in Zebrafish.

Acrylamide (ACR) is a water-soluble monomer with broad consumer applications, even in foods due to thermal processes. Acute exposure to ACR may lead to neurotoxic effects such as ataxia and skeletal muscle weakness in humans and experimental animals. Oxidative stress is the primary pathway in ACR toxicity; therefore, this study aimed to evaluate the possible protective effect of benzo[b]thiophene analogs as an antioxidant drug for ACR poisoning.

Connected to the cloud at time of death: a case report.

Background: Our case report provides the first clinical evaluation of autopsy practices for a patient death that occurs on the cloud. We question how autopsy practices may require adaptation for a death that presents via the 'Internet of Things', examining how existing guidelines capture data related to death which is no longer confined to the patient's body.

Case Presentation: The patient was a British man in his 50s, who came to the attention of the medical team via an alert on the cloud-based platform that monitored his implanted cardioverter defibrillator (ICD).

Tailoring the Molecular Structure of 6-Gingerol for Targeting the Phase Separation in Human Lysozyme.

Human lysozyme undergoes a phase-separation process to form insoluble amyloid-architects that cause several pathologies including systemic amyloidosis. Here we have tailored 6-gingerol by extending its molecular framework with active functional groups to specifically target lysozyme phase-transition events. Aggregation assay revealed that tailored 6-gingerol with 4-aromatic moieties (MTV4) substantially suppressed the conversion of the lysozyme low-density liquid phase (LDLP) to solid-phase structured amyloids.

Global DNA and RNA Methylation Signature in Response to Antipsychotic Treatment in First-Episode Schizophrenia Patients.

Background: Schizophrenia is a heterogeneous chronic psychiatric disorder influenced by genetic and environmental factors. Environmental factors can alter epigenetic marks, which regulate gene expression and cause an array of systemic changes. Several studies have demonstrated the association of epigenetic modulations in schizophrenia, which can influence clinical course, symptoms, and even treatment.

A Case of Metastatic Melanoma Post Orthotopic Liver Transplantation.

With the rising prevalence of organ transplantation, clinicians must be aware of the many potential complications that may arise. One such complication is post-transplantation melanoma. Herein, we present a case of advanced metastatic melanoma following orthotopic liver transplantation (OLT).

A meta-analysis of ferric carboxymaltose versus other intravenous iron preparations for the management of iron deficiency anemia during pregnancy.

Objective: We conducted a meta-analysis of randomized clinical trials evaluating the clinical effects of ferric carboxymaltose therapy compared to other intravenous iron in improving hemoglobin and serum ferritin in pregnant women. We also assessed the safety of ferric carboxymaltose vs. other intravenous iron.

Finite element analysis (FEA) of stress distribution in platform-switched short dental implants.

The distribution of stress on short platform switched dental implants is of interest. Hence, the mandibular posterior molar area was modelled using a three-dimensional finite element method (FEM) with a continuous 1.5 mm cortical bone thickness and an inner cancellous bone core.

Eggs for Improving Nutrition, cognitive development and reducing linear growth retardation among Infants and young Children (ENRICH): protocol of an egg supplementation trial among children aged 9-18 months in Hyderabad, India.

Introduction: Evidence on the impact of nutrient-rich animal source foods such as eggs for improving child growth and cognition is inconsistent. This study aims to examine the impact of an egg intervention in children, along with behaviour change communication (BCC) to the mother, on linear growth and cognition, and nutritional status in children aged 9-18 months.

Methods And Analysis: A 9-month open-labelled randomised controlled trial will be conducted in three urban slums in Hyderabad, India, as a substudy of an observational cohort study (n=350) following pregnant women and their children until 18 months of age in a population at risk of stunting.

Double Philadelphia chromosome: a rare and sole abnormality in pediatric B-acute lymphoblastic leukemia.

The present study describes a 7-year-old male child who had attended the Pediatric Oncology Clinic of the Regional Cancer Centre, Thiruvananthapuram, Kerala, India, and was pathologically confirmed to have B-Acute Lymphoblastic Leukemia (B-ALL). Conventional cytogenetics analysis at diagnosis showed the presence of a double Philadelphia chromosome and the karyotype of the case was 47, , (9;22)(q34;q11.2), + der(22)t(9;22).

Substituent-controlled regioselective arylation of carbazoles using dual catalysis.

Regioselective arylation of carbazoles is reported using dual palladium-photoredox catalysis. Controlled monoarylation and diarylation of symmetrical and unsymmetrical carbazoles were achieved under mild reaction conditions with a broad substrate scope and functional group tolerance. Steric and electronic control the regioselectivity of the arylation of unsymmetrical carbazoles.

Deacetylepoxyazadiradione ameliorates diabesity in in-vivo zebrafish larval model by influencing the level of regulatory adipokines and oxidative stress.

Obesity and diabetes constitute significant global health issues associated with one another. In contrast to diabetes, which is characterised by oxidative stress that enhances cellular damage and the following complications. Obesity dynamics involve chronic inflammation that promotes insulin resistance and metabolic disruptions.

Rh(III) Catalyzed Redox-Neutral C-H Activation/[5 + 2] Annulation of Aroyl Hydrazides and Sulfoxonium Ylides: Synthesis of Benzodiazepinones.

We herein report the Rh(III) catalyzed redox-neutral C-H activation/[5 + 2] annulation of aroyl hydrazides with sulfoxonium ylides as safe carbene precursors. The reaction shows excellent functional group tolerance, broad substrate scope, and scalability. We demonstrated the synthetic utility of the protocol via the synthesis of various diazepam drug analogues, late-stage functionalization of probenecid drug, and large scale synthesis.

Tragacanth gum-based nano-nutraceuticals synthesis by encapsulation of beetroot juice and Ocimum basilicum leaves for micronutrient deficient population.

Micronutrient deficiencies, such as iron, folic acid, and vitamins C and D, are currently prevalent due to inadequate consumption of natural food sources, namely raw vegetables and fruits. This deficiency is compounded by the growing reliance on synthetic nutraceuticals and processed food, which exhibit poor absorbency within the gastrointestinal tract. Scientific studies consistently indicate that naturally prepared whole foods are superior in terms of nutrient absorption compared to processed and synthetic supplements.

Dual Palladium-Photoredox-Mediated Regioselective Acylation of Carbazoles and Indolines.

We have described a dual palladium-photoredox-catalyzed highly regioselective acylation of carbazoles and indolines using molecular oxygen as the green oxidant. The reaction shows a broad substrate scope and good functional group tolerance. Late-stage functionalization of a carprofen drug derivative, further manipulation of products, and gram-scale synthesis of the acylated products were illustrated to show the versatility of the method.

Oestrogen receptor-independent actions of oestrogen in cancer.

Oestrogen, the primary female sex hormone, plays a significant role in tumourigenesis. The major pathway for oestrogen is via binding to its receptor [oestrogen receptor (ERα or β)], followed by nuclear translocation and transcriptional regulation of target genes. Almost 70% of breast tumours are ER + , and endocrine therapies with selective ER modulators (tamoxifen) have been successfully applied.

Analysis of Inhibition Potential of Nimbin and its Analogs against NF-κB Subunits p50 and p65: A Molecular Docking and Molecular Dynamics Study.

Background: Cancer remains the major cause of morbidity and mortality. The nuclear factor kappa-B (NF- κB) plays an indispensable role in cancer cell proliferation and drug resistance. The role of NF-κB is not only limited to tumor cell proliferation and suppression of apoptotic genes but it also induces EMT transition responsible for metastasis.

Molecular dynamics simulation approach of hybrid chalcone-thiazole complex derivatives for DNA gyrase B inhibition: lead generation.

Compounds bearing thiazole and chalcone groups have been reported to be excellent leads for antibacterial, antitubercular and anticancer activities. In view of this, we performed quantitative structure-activity relationship studies using QSARINS for dataset preparation and for developing validated QSAR models that can predict novel series of thiazole-chalcone hybrids and further evaluate them for bioactivities. The molecular descriptors AATS8i, AVP-1, MoRSEE17 and GATSe7 were found to be active in predicting the structure-activity relationship.

Nimbin analogs stimulate glucose uptake and glycogen storage in the insulin signalling cascade by enhancing the IRTK, PI3K and Glut-4 mechanism in myotubes.

Background: Diabetes Mellitus is a metabolic disorder characterized by insulin dysfunction or failure of the pancreatic β-cells to produce insulin resulting in hyperglycemia. Adverse effects of hyperglycemic conditions continue to be common, reducing treatment adherence. Intensified therapies are required for the constant loss of endogenous islet reserve.