Ionic-liquid-supported copper-promoted synthesis of 3,5-disubstituted-1,2,4-triazoles.

The synthesis of triazoles plays an important role in drug discovery research. 1,2,4-triazoles are considered significant scaffolds among several bioactive heterocycles due to their extensive use in the pharmaceutical and agrochemical sectors. Consequently, the importance of the synthesis of 1,2,4-triazoles a sustainable method has increased.

A microwave assisted tandem synthesis of quinazolinones using ionic liquid supported copper(II) catalyst with mechanistic insights.

Quinazolinone is a preferred structural motif with notable pharmacological activity that is present in a wide range of naturally occurring compounds. A microwave assisted tandem cyclooxidative method has been developed to afford quinazolinones a recyclable ionic liquid supported copper catalyst. This sustainable method exhibits operational simplicity through a rapid, clean, and energy-efficient route and a variety of 2-substituted quinazolinones are obtained in excellent yields.

Synthesis and Anticancer Evaluation of Disubstituted Benzimidazoles via One-Pot Telescopic Grinding Approach.

Benzimidazole compounds are known for their broad spectrum therapeutic potentials. A small library of benzimidazole derivatives were designed and synthesized via a one-pot telescopic grinding approach. The ability of these molecules as proposed anticancer agents were evaluated by their potential to bind to two important cancer pathway protein targets, human estrogen receptors and cyclin dependant kinases, 3ERT and 5FGK respectively.

Novel neuroprotective 5,6-dihydropyrido[2',1':2,3]imidazo[4,5-c]quinoline derivatives acting through cholinesterase inhibition and CB2 signaling modulation.

A novel group of 5,6-dihydropyrido [2',1':2,3]imidazo [4,5-c]quinolines was prepared via a microwave assisted one-pot telescopic approach. The synthetic sequence involves the formation of an amine precursor of imidazo [1,2-a]pyridine via condensation and reduction under microwave irradiation. Subsequently, the Pictet-Spengler cyclisation reaction occurs with ketones (cyclic or acyclic) to obtain substituted 5,6-dihydropyrido [2',1':2,3]imidazo [4,5-c]quinolines in excellent yields.

Anti-cancer property and DNA binding interaction of first row transition metal complexes: A decade update.

Metal ions carry out a wide variety of functions, including acid-base/redox catalysis, structural functions, signaling, and electron transport. Understanding the interactions of transition metal complexes with biomacromolecules is essential for biology, medicinal chemistry, and the production of synthetic metalloenzymes. After the coincidental discovery of cisplatin, importance of the metal complexes in biochemistry became a top priority for inquiry.

Synthetic access to diverse thiazetidines a one-pot microwave assisted telescopic approach and their interaction with biomolecules.

A one-pot microwave assisted telescopic approach is reported for the chemo-selective synthesis of substituted 1,3-thiazetidines using readily available 2-aminopyridines/pyrazines/pyrimidine, substituted isothiocyanates and 1,2-dihalomethanes. The procedure involves thiourea formation from 2-aminopyridines/pyrazines/pyrimidine with the substituted isothiocyanates followed by a base catalysed nucleophilic attack of the CS bond on the 1,2-dihalomethane. Subsequently, a cyclization reaction occurs to yield substituted 1,3-thiazetidines.

Synaptically-targeted long non-coding RNA SLAMR promotes structural plasticity by increasing translation and CaMKII activity.

Long noncoding RNAs (lncRNAs) play crucial roles in maintaining cell homeostasis and function. However, it remains largely unknown whether and how neuronal activity impacts the transcriptional regulation of lncRNAs, or if this leads to synapse-related changes and contributes to the formation of long-term memories. Here, we report the identification of a lncRNA, SLAMR, which becomes enriched in CA1-hippocampal neurons upon contextual fear conditioning but not in CA3 neurons.

Imaging and Assay of the Dynamics of Cytotoxic Huntingtin (HTT) Protein Aggregates Regulated by lncRNAs.

Huntington's disease (HD) pathogenesis involves deregulation of coding and noncoding RNA transcripts of which the involvement of long noncoding RNAs (lncRNA) has been realized recently. Of these, Meg3, Neat1, and Xist showed a consistent and significant increase in HD cell and animal models. In the present study, we formulate a methodology to visualize and quantify intracellular aggregates formed by mutant HTT protein.

Quantitative Investigation of Neuroprotective Role of ROR1 in a Cell Culture Model of Alzheimer's Disease.

Cytoskeletal and microtubule atrophy are major hallmarks of Alzheimer's disease (AD). A method to investigate endogenous proteins that can interact/stabilize the cytoskeleton (under pathological cues) is rare. Here, we describe how receptor tyrosine kinase-like orphan receptor 1 (ROR1), a receptor tyrosine kinase (RTK), can act as a neuroprotective molecule by promoting neurite outgrowth, stabilizing cytoskeletal components, and altering the dynamics of actin assembly in a cell culture model of AD.

Gynaecologic oncology surgical cancellations in Zambia.

Introduction: Cancellations of elective surgery in low-and middle-income countries (LMIC) are common and a major hindrance for patients who are in need of surgical therapeutic modalities. This is especially important in the context of scaling up needed surgical interventions for gynaecological cancer care. There is a knowledge gap in the literature related to cancellation of gynaecologic oncology surgeries in LMIC, where there is enormous need for this specific cancer surgical capacity.

An in silico approach to investigate the theranostic potential of coumarin-derived self-immolative luminescent probes.

Till date the challenge exists in the treatments of cancer for various reasons. Most importantly, the available diagnostics are expensive with research gap for enhancing the cancer detection sensitivity. Herein, a series of coumarin-derived fluorescent theranostic probes are reported that can serve as potent anticancer agents as well as in the detection of cancer cells.

Recent Advancements of Aptamers in Cancer Therapy.

Aptamers are chemical antibodies possessing the capability of overcoming the limitations posed by conventional antibodies, particularly for diagnostic, therapeutic, and theranostic applications in cancer. The ease of chemical modifications or functionalization, including conjugations with nucleic acids, drug molecules, and nanoparticles, has made these aptamers to gain priorities in research. In this Mini-review, various reports on therapeutics with aptamer-functionalized nanomaterials for controlled or multistep drug release, targeted delivery, stimuli-responsive drug release, are discussed.

Click-derived multifunctional metal complexes for diverse applications.

The Click reaction that involves Cu(I)-catalyzed azide-alkyne cycloaddition (CuAAC) serves as the most potent and highly dependable tool for the development of many complex architectures. It has paved the way for the synthesis of numerous drug molecules with enhanced synthetic flexibility, reliability, specificity and modularity. It is all about bringing two different molecular entities together to achieve the required molecular properties.

Copper Catalyzed Synthesis of Heterocyclic Molecules via C-N and C-O Bond Formation under Microwaves: A Mini-Review.

Heterocyclic moieties play a significant role in the field of drug discovery. C-N and C-O bond formation reactions are the primary synthetic sequence for the generation of heterocyclic molecules. The generation of C-N and C-O bonds involves the use of mostly Pd or Cu catalysts although other transition metal catalyst's are also involved.

Giant cyst in heterotopic pregnancy: A case report.

Background: The coexistence of a heterotopic pregnancy with a giant ovarian cyst is an incredibly rare abnormal pregnancy in cases of natural conception. The incidence of this condition has increased significantly as a result of the continuous development of assisted reproductive technologies. When this type of pregnancy occurs, both the continuation of intrauterine pregnancy and the life of the pregnant woman are severely threatened.

Recent Advancement in the Inhibition of Triple-negative Breast Cancer by -heterocycles.

Despite the substantial progress that has been made in cancer therapy over the past few decades, there has been a discernible rise in the number of reported instances of carcinoma over the past few decades. Breast cancer especially triple-negative breast cancer (TNBC), being the most common cancer found in females account for extensive research. This type of cancer, which is responsible for more than 15% to 20% of all breast cancers, is particularly interesting for research since it is difficult to treat due to its poor response to treatment and extremely aggressive nature.

Biodiversity assessment using passive acoustic recordings from off-reef location-Unsupervised learning to classify fish vocalization.

We present the quantitative characterization of Grande Island's off-reef acoustic environment within the Zuari estuary during the pre-monsoon period. Passive acoustic recordings reveal prominent fish choruses. Detailed characteristics of the call employing oscillograms and individual fish call parameters of the segmented data include vocal groups such as Sciaenidae, Terapon theraps, and planktivorous as well as invertebrate sounds, e.

, a synaptically targeted lncRNA, facilitates the consolidation of contextual fear memory.

LncRNAs are involved in critical processes for cell homeostasis and function. However, it remains largely unknown whether and how the transcriptional regulation of long noncoding RNAs results in activity-dependent changes at the synapse and facilitate formation of long-term memories. Here, we report the identification of a novel lncRNA, SLAMR, that becomes enriched in CA1- but not in CA3-hippocampal neurons upon contextual fear conditioning.

Comparison of a U.S. and Zambian Ob/Gyn Residency Training Programme.

Introduction: The major objective of the study was to compare and contrast a U.S. and Zambian Ob/Gyn residency programme, using uniform metrics, as the basis for an initial exploration of perceived inequities in post-graduate medical education between low- and high-income countries.

In Silico Design and Investigation of Novel Thiazetidine Derivatives as Potent Inhibitors of PrpR in Mycobacterium tuberculosis.

Tuberculosis is one of the most life-threatening acute infectious diseases diagnosed in humans. In the present investigation, a series of 16 new disubstituted 1,3-thiazetidines derivatives is designed, and investigated via various in silico methods for their potential as anti-tubercular agent by evaluating their ability to block the active site of PrpR transcription factor protein of Mycobacterium tuberculosis. The efficacy of the molecules was initially assessed with the help of AutoDock Vina algorithm.

Insights on Chemical Crosslinking Strategies for Proteins.

Crosslinking of proteins has gained immense significance in the fabrication of biomaterials for various health care applications. Various novel chemical-based strategies are being continuously developed for intra-/inter-molecular crosslinking of proteins to create a network/matrix with desired mechanical/functional properties without imparting toxicity to the host system. Many materials that are used in biomedical and food packaging industries are prepared by chemical means of crosslinking the proteins, besides the physical or enzymatic means of crosslinking.

Synthetic approaches to potent heterocyclic inhibitors of tuberculosis: A decade review.

Tuberculosis (TB) continues to be a significant global health concern with about 1.5 million deaths annually. Despite efforts to develop more efficient vaccines, reliable diagnostics, and chemotherapeutics, tuberculosis has become a concern to world health due to HIV, the rapid growth of bacteria that are resistant to treatment, and the recently introduced COVID-19 pandemic.

Photophysical evaluation on the electronic properties of synthesized biologically significant pyrido fused imidazo[4,5-c]quinolines.

A single pot microwave assisted method was employed to synthesize a series of novel pyrido fused imidazo[4,5-c]quinolines. The electronic properties of these derivatives were investigated by following their photophysical behaviour under isolated and solvated conditions via computational and experimental approaches. The solvatochromic effect of these derivatives was investigated in the ground and excited singlet states by following the absorption and fluorescence emission and excitation spectra.

molecular modelling, MM/GBSA binding free energy and molecular dynamics simulation study of novel pyrido fused imidazo[4,5-]quinolines as potential anti-tumor agents.

With an alarming increase in the number of cancer patients and a variety of tumors, it is high time for intensive investigation on more efficient and potent anti-tumor agents. Though numerous agents have enriched the literature, still there exist challenges, with the availability of different targets and possible cross-reactivity. Herein we have chosen the phosphoinositide 3-kinase (PI3K) as the target of interest and investigated the potential of pyrido fused imidazo[4,5-]quinoline derivatives to bind strongly to the active site, thereby inhibiting the progression of various types of tumors.