Comprehensive Insight into Green Synthesis Approaches, Structural Activity Relationship, and Therapeutic Potential of Pyrazolic Chalcone Derivative.

Pyrazolic chalcone exhibits diverse therapeutic activities, including anti-inflammatory, antioxidant, antimicrobial, antitumor, and anti-diabetic properties. Structural activity relationship (SAR) studies play a crucial role in understanding the molecular aspects governing their biological effects, guiding the rational design of derivatives with enhanced efficacy and reduced side effects. This review provides an overview of pyrazolic chalcone derivatives, emphasizing their synthesis through both conventional and green methods.

A Significant Prospective on Nanorobotics in Precision Medicine and Therapeutic Interventions.

Nanorobotics, situated at the intersection of nanotechnology and robotics, holds the potential for revolutionary impact on precision medicine and medical interventions. This review explores the design, navigation, drug delivery, and applications of nanorobots. Architectural intricacies, sensor integration, and navigation strategies, both active and passive, are discussed.

Dysregulated gene subnetworks in breast invasive carcinoma reveal novel tumor suppressor genes.

Breast invasive carcinoma (BRCA) is the most malignant and leading cause of death in women. Global efforts are ongoing for improvement in early detection, prevention, and treatment. In this milieu, a comprehensive analysis of RNA-sequencing data of 1097 BRCA samples and 114 normal adjacent tissues is done to identify dysregulated genes in major molecular classes of BRCA in various clinical stages.

Cationic nanocarriers: A potential approach for targeting negatively charged cancer cell.

Cancer, a widespread and lethal disease, necessitates precise therapeutic interventions to mitigate its devastating impact. While conventional chemotherapy remains a cornerstone of cancer treatment, its lack of specificity towards cancer cells results in collateral damage to healthy tissues, leading to adverse effects. Thus, the quest for targeted strategies has emerged as a critical focus in cancer research.

Cell-Penetrating Peptides as Keys to Endosomal Escape and Intracellular Trafficking in Nanomedicine Delivery.

This review article discusses the challenges of delivering cargoes to the cytoplasm, for example, proteins, peptides, and nucleic acids, and the mechanisms involved in endosomal escape. Endocytosis, endosomal maturation, and exocytosis pose significant barriers to effective cytoplasmic delivery. The article explores various endosomal escape mechanisms, such as the proton sponge effect, osmotic lysis, membrane fusion, pore formation, membrane destabilization/ disruption, and vesicle budding and collapse.

A Comprehensive Review on Nanoparticles as a Targeted Delivery System for the Treatment of Lung Cancer.

The second most common type of cancer is lung cancer, impacting the human population. Lung cancer is treated with a number of surgical and non-surgical therapies, including radiation, chemotherapy, and photodynamic treatment. However, the bulk of these procedures are costly, difficult, and hostile to patients.

Drug Delivery System Approaches for Rheumatoid Arthritis Treatment: A Review.

Rheumatoid arthritis (RA) is a chronic autoimmune disease that has traditionally been treated using a variety of pharmacological compounds. However, the effectiveness of these treatments is often limited due to challenges associated with their administration. Oral and parenteral routes of drug delivery are often restricted due to issues such as low bioavailability, rapid metabolism, poor absorption, first-pass effect, and severe side effects.

Targeted intracellular delivery of antitubercular bioactive(s) to Mtb infected macrophages via transferrin functionalized nanoliposomes.

The packaging of antimicrobials/chemotherapeutics into nanoliposomes can enhance their activity while minimizing toxicity. However, their use is still limited owing to inefficient/inadequate loading strategies. Several bioactive(s) which are non ionizable, and poorly aqueous soluble cannot be easily encapsulated into aqueous core of liposomes by using conventional means.

Curcumin and its Derivatives Targeting Multiple Signaling Pathways to Elicit Anticancer Activity: A Comprehensive Perspective.

The uncontrolled growth and spread of aberrant cells characterize the group of disorders known as cancer. According to GLOBOCAN 2022 analysis of cancer patients in either developed countries or developing countries the main concern cancers are breast cancer, lung cancer, and liver cancer which may rise eventually. Natural substances with dietary origins have gained interest for their low toxicity, anti-inflammatory, and antioxidant effects.

Structural Insights into N-heterocyclic Moieties as an Anticancer Agent against Hepatocellular Carcinoma: An Exhaustive Perspective.

Hepatocellular carcinoma (HCC) is rapidly spreading around the world with a high mortality rate. In the low- and middle-income nations most impacted by HCV and HBV infections, HCC places a significant strain on the healthcare system and leaches productive capability. An extensive study on HCC to create novel therapeutic approaches was motivated by the lack of adequate preventive or curative therapy methods.

Multiple Protein Biomarkers and Different Treatment Strategies for Colorectal Carcinoma: A Comprehensive Prospective.

In this review, we emphasized important biomarkers, pathogenesis, and newly developed therapeutic approaches in the treatment of colorectal cancer (CRC). This includes a complete description of small-molecule inhibitors, phytopharmaceuticals with antiproliferative potential, monoclonal antibodies for targeted therapy, vaccinations as immunotherapeutic agents, and many innovative strategies to intervene in the interaction of oncogenic proteins. Many factors combine to determine the clinical behavior of colorectal cancer and it is still difficult to comprehend the molecular causes of a person's vulnerability to CRC.

Structural Insight on GPR119 Agonist as Potential Therapy for Type II Diabetes: A Comprehensive Review.

Diabetes Mellitus (DM) is a long-term metabolic condition that is characterized by excessive blood glucose. DM is the third most death-causing disease, leading to retinopathy, nephropathy, loss of vision, stroke, and cardiac arrest. Around 90% of the total cases of diabetic patients have Type II Diabetes Mellitus (T2DM).

Advances in Nanogel as Drug Delivery System for Cancer Therapeutics: An Overview.

Nanogels have gotten much attention as nanoscopic drug carriers, especially for delivering bioactive mediators to specific sites or at certain times. The versatility of polymer systems and the ease with which their physicochemical properties can be changed have resulted in versatile nano gel formulations. Nanogels offer exceptional stability, drug-loading capacity, biological consistency, strong penetration ability, and the ability to respond to environmental stimuli.

Structural Perspective of Benzophenones Targeting Tubulin as Anticancer Agents.

Cancer is the leading cause of death and the most significant determinant of life expectancy in almost every country in this twenty-first century. According to the World Health Organization (WHO), cancer is responsible for the leading cause of death globally. Benzophenone derivatives are found in a variety of naturally occurring compounds which are known to be pharmacologically efficacious against a variety of diseases, including cancer.

Computational approaches for the design of novel dopamine D and serotonin 5-HT receptor dual antagonist towards schizophrenia.

Piperidine and piperazine derivatives exhibit a diverse range of biological applications, including antipsychotic activity. In this study, a dataset of molecules containing piperidine, piperazine moieties that possess serotonin 5-HT and dopamine D inhibitory activity have been chosen for Pharmacophore modeling, Quantitative Structure-Activity (3D-QSAR) Relationship, Molecular docking, and ADME studies. The pharmacophoric hypothesis was found to be AAHPRRR_1 having seven features as one H-bond acceptor (A), one hydrophobic (H), one positive ion acceptor (P), and three aromatic rings (R), with survival score = 6.

A critical analysis of urea transporter B inhibitors: molecular fingerprints, pharmacophore features for the development of next-generation diuretics.

Urea transporter is a membrane transport protein. It is involved in the transferring of urea across the cell membrane in humans. Along with urea transporter A, urea transporter B (UT-B) is also responsible for the management of urea concentration and blood pressure of human.

Multiple strategies for the treatment of invasive breast carcinoma: A comprehensive prospective.

In this review, we emphasize on evolving therapeutic strategies and advances in the treatment of breast cancer (BC). This includes small-molecule inhibitors under preclinical and clinical investigation, phytoconstituents with antiproliferative potential, targeted therapies as antibodies and antibody-drug conjugates (ADCs), vaccines as immunotherapeutic agents and peptides as a novel approach inhibiting the interaction of oncogenic proteins. We provide an update of molecules under different phases of clinical investigation which aid in the identification of loopholes or shortcomings that can be overcomed with future breast cancer research.

Urea transporter and its specific and nonspecific inhibitors: State of the art and pharmacological perspective.

Hypertension is a major concern for a wide array of patients. The traditional drugs are commonly referred as 'water pills' and these molecules have been successful in alleviating hypertension. However, this comes at the high expense of precious electrolytes in our body.

Synthesis and ex vivo evaluation of PLGA chitosan surface modulated double walled transdermal Pluronic nanogel for the controlled delivery of Temozolomide.

A surface modulated biodegradable transdermal strategy has been exploited for improving the biopharmaceutical properties of Temozolomide augmented in Poly Lactic-co-glycolic acid (PLGA) chitosan double walled nanogel (PCNGL). The PCNGL was synthesized by dual approach methodology showing consistent nanosize particle range of 210 nm and PDI 0.325 ± 0.

Discovery of novel ALK2 inhibitors of pyrazolo-pyrimidines: A computational study.

ALK2 is a serine/threonine kinase, involved in different signaling pathways and associated with cell proliferation and differentiation. The present study includes development of pharmacophore, 3-D QSAR, docking and virtual screening studies on 30 different pyrazolo[1,5-a]pyrimidine derivatives. The pharmacophore study provides ARRR_2 hypothesis with four different features essential for ALK2 kinase inhibitory activity.

Structural and biological aspects of natural bridged macrobicyclic peptides from marine resources.

Among peptide-based drugs, naturally occurring bicyclic compounds have been established as molecules with unique therapeutic potential. The diverse pharmacological activities associated with bicyclic peptides from marine tunicates, sponges, and bacteria render them suitable to be employed as effective surrogate between complex and small therapeutic moieties. Bicyclic peptides possess greater conformational rigidity and higher metabolic stability as compared with linear and monocyclic peptides.

Current Insights into the Chemistry and Antitubercular Potential of Benzimidazole and Imidazole Derivatives.

Tuberculosis is a disease caused by Mycobacterium tuberculosis (Mtb), affecting millions of people worldwide. The emergence of drug resistance is a major problem in the successful treatment of tuberculosis. Due to the commencement of MDR-TB (multi-drug resistance) and XDR-TB (extensively drug resistance), there is a crucial need for the development of novel anti-tubercular agents with improved characteristics such as low toxicity, enhanced inhibitory activity and short duration of treatment.

The Recent Development of Piperazine and Piperidine Derivatives as Antipsychotic Agents.

Schizophrenia is a chronic neuropsychiatric disorder that affects nearly 1% of the global population. There are various anti-psychotic drugs available for the treatment of schizophrenia, but they have certain side effects; therefore, there is a need to explore and develop novel potential lead compounds against schizophrenia. The currently available drugs e.

Exploring siRNA Umpired Nanogels: A Tale of Barrier Combating Carrier.

Potential short interfering RNAs (siRNA) modulating gene expression have emerged as a novel therapeutic arsenal against a wide range of maladies and disorders containing cancer, viral infections, bacterial ailments and metabolic snags at the molecular level. Nanogel, in the current medicinal era, displayed a comprehensive range of significant drug delivery prospects. Biodegradation, swelling and de-swelling tendency, pHsensitive drug release and thermo-sensitivity are some of the renowned associated benefits of nanogel drug delivery system.