Current Drug Discovery Technologies - Volume 23, Issue 1, 2026
Volume 23, Issue 1, 2026
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Anti-cancer Potential of Scopoletin Derivatives Across Diverse Cancer Cell Lines: A Comprehensive Review
More LessAuthors: Manvi Karayat, Niranjan Kaushik, Deepika Paliwal and Sachin ChaudharyScopoletin, a naturally occurring coumarin derivative, has garnered significant attention for its diverse pharmacological properties, including potent anticancer activity. This review provides a comprehensive examination of scopoletin's anticancer effects across a wide range of tumor cell lines. The paper explores its modulation of apoptotic pathways, inhibition concentration (IC50) of cancer cell proliferation, and suppression of metastasis and angiogenesis. Additionally, the review discusses the role of scopoletin in regulating oxidative stress, inflammation, and cell cycle arrest in cancer cells. A detailed analysis of in vitro and in vivo studies highlights its efficacy, specificity, and potential for synergistic effects when used in combination with conventional chemotherapeutics. Hence, this comprehensive review aims to provide a foundation for future research and development of scopoletin as a promising anticancer agent.
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Challenges and Countermeasures for Ensuring Health and Drug Stability During Long-term Space Missions
More LessMicrogravity, space radiation, and pharmaceutical degradation are all long-term challenges for astronauts traveling through space. Radiation exposure is one of the greatest health risks to astronauts in space. Associated with these conditions are acute radiation syndromes, degenerative tissue effects, damage to the central nervous system (CNS), and carcinogenesis. Microgravity and the stress people experience as astronauts cause immunological dysregulation. This study explores strategies to counteract the problems of microgravity and its related health risks, including protection against space radiation, prevention of pharmaceutical degradation, and advancements in the emerging field of astropharmacy.
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Exploring Herbal Remedies as Adjunctive Therapies in Managing Inflammation and Rheumatoid Arthritis
More LessAuthors: Vijay Raghav, Swati Arya, Rubina Bhutani, Arti Kumari and Farah AnjumHabitual inflammation is defined as the persistent activation of the body's susceptible system in response to harmful events. This ongoing inflammatory process can sometimes harm normal organs & tissues. Crucially, chronic inflammation has been linked to the emergence and advancement of a variety of disorders, including cardiovascular diseases, respiratory issues, metabolic illnesses, neurological disorders, and cancer. These diseases are classified as chronic-degenerative conditions due to the sustained and persistent nature of the underlying chronic inflammatory processes. Treating patient’s inflammation creates new therapeutic opportunities for these related illnesses. In this review, we will study the role of inflammation during the onset of rheumatoid arthritis. Furthermore, we will explore diseases associated with chronic inflammation. Rheumatoid Arthritis (RA) is a persistent autoimmune condition causing joint inflammation. It commonly affects joints of hands, wrists, fingers, elbows, shoulders, neck, back, hips, knees, ankles, and toes. We will discuss various herbal drug therapies that help in treating and providing relief from joint pain in rheumatoid arthritis. Herbal medicines are preferable since they are safer and have fewer adverse effects than the synthetic ones. However, they are not completely safe, and therefore, toxicity studies are being conducted. . Herbal medications' phytochemicals are generally beneficial in the treatment of infectious, autoimmune, and seditious disorders; they are especially helpful in the management of arthritis. Arthritis is one of the leading causes of impairment in the quality of life for millions of people globally. The purpose of this review is to explore the role of inflammation in rheumatoid arthritis and its association with chronic inflammation. This article highlights the importance of herbal medicine as one of the treatment options for rheumatoid arthritis.
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Breaking Boundaries in Cancer Therapy: Harnessing Chromothripsisinduced Mutations for Targeted Bcl-2 Protein Destabilization
More LessAuthors: Sergey Shityakov, Michael Nosonovsky, Ekaterina V. Skorb and Viacheslav KravtsovChromothripsis, a phenomenon of massive genomic rearrangements, introduces extensive mutations in critical genes, affecting cell survival and apoptosis. Among these genes, the BCL-2 (B-cell lymphoma 2) gene, which plays a crucial antiapoptotic role in cancer cells, is often subjected to significant alterations. Here, we present a computational pipeline to model and analyze the structural and functional impacts of chromothripsis-induced Single-Nucleotide Polymorphisms (SNPs) within the BCL-2 gene. This pipeline integrates mutation simulation, homology modeling, and protein interaction analysis to evaluate the stability and apoptotic potential of BCL-2 mutations. These results indicate that chromothripsis-induced mutations can destabilize the BCL-2 protein, thereby disrupting its binding affinity with apoptotic regulators, such as Bax. These findings support the potential of ergodic anticancer therapy to exploit such mutations, facilitating the apoptosis of cancer cells. Our computational model offers a novel in silico approach for understanding mutation-driven alterations in cancer biology, aiding the development of therapeutic strategies targeting apoptotic pathways.
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Exploring Novel Oxazole Derivatives for Cancer Therapy: Design, Synthesis, and Mechanistic Insights
More LessIntroductionThe search for potent anticancer agents has accelerated the evaluation of a wide variety of pharmacological scaffolds, including oxazole derivatives. Although they are currently underexplored, they are promising as anticancer agents. This research covers the synthesis and structure-activity relationships of oxazole-based compounds.
MethodsThe authors designed and synthesized new oxazole derivatives and screened them for their anticancer activity using both computational and experimental methods. Molecular docking studies were performed to identify possible targets based on literature and the interaction of these molecules with anticancer targets like c-Kit tyrosine kinase (TRK) and Murine double minute 2 homolog (MDM2). The compounds were tested using the MTT assay on a cancer cell lines, MCF-7, to evaluate their potential effectiveness.
Results and DiscussionRobust synthetic procedures were developed and optimized for oxazole-based Schiff bases, with their structures confirmed through spectral analyses. Four compounds demonstrated significantly higher anticancer efficacy, while one has lesser potency, suggesting some Structure-Activity Relationship (SAR) nuances within the series. The biological activities (IC50) were determined to be in the range of 80-100 µg/mL, while molecular docking indicated that compound 4c could serve as a potential lead for c-Kit Tyrosine Kinase (TRK) inhibition.
ConclusionThe results obtained from the present study corroborate the hypothesis that oxazole derivatives are potent anticancer agents, consistent with predictions from molecular docking studies. These findings highlight the significance of the oxazole scaffold in anticancer drug discovery and encourage further exploration of structure-activity relationships to enhance therapeutic potential. Although compound 4c showed better interactions in docking studies it turned out to be less effective in biological screening, this suggests that pharmacokinetic issues should be addressed. Future studies are likely to include in vivo models and detailed mechanistic evaluations to validate these findings and support the development of oxazole-derived anticancer compounds.
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Pharmacological Insights on USFDA-approved Novel Drug Therapies in the Year 2023
More LessAuthors: Parveen Kumar Goyal, Vipasha Sharma and Kavita SangwanIntroductionThis study, aimed to prepare a scientific report, underscores the pharmacotherapeutic aspects, including therapeutic indications, mechanisms of therapeutic action, pharmacokinetics, adverse reactions, safety in special cases, approximate costs, etc., of USFDA-approved novel drugs in the year 2023 and serve as a treasured resource for academia, researchers, patients, and clinicians.
MethodsThis comprehensive report was prepared by reviewing the pre-clinical and clinical data of the USFDA-approved novel drugs available in the public domain, especially on the website of the USFDA, National Library of Medicine, Clinical Trials, other online resources, and cross-references.
Results and DiscussionThe USFDA has approved 55 novel drug therapies in the year 2023 and identified 38 drugs as new chemical entities (29 small molecules, 5 peptides, and 4 oligonucleotides) and 17 new biologicals. About 51% (28 out of 55) of drugs were recommended for rare diseases and designated as orphan drugs. In addition to the therapeutic aspects and general description, the approximate cost or price and safety studies in special cases such as lactating and pregnant women, pediatrics, and geriatrics of all novel drug therapies are meticulously presented in this study.
ConclusionThe novel drug therapies approved by the USFDA hold significant potential to enhance the patient’s care by providing advanced treatment modalities. This study, reporting the comprehensive description of therapeutic aspects of the mentioned new drug therapies, underscores the commitment of the pharmaceutical sector to address the unmet medical needs and reshape the landscape of the healthcare service system by instilling optimism among patients and healthcare providers.
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Unlocking the Potential of Alginate Polymers: A Review of Recent Advances in Physicochemical Modulation for Versatile Biomaterials
More LessAuthors: Shiom Mane, Poournima Sankpal, Sachinkumar Patil, Rashmi Pathak and Himanshu SharmaAlginate, a naturally occurring polysaccharide, exhibits immense potential for diverse applications due to its ability to undergo chemical modifications and blend with other constituents. These modifications enable the creation of alginate derivatives that are not only biocompatible for biomedical and tissue engineering applications but also crucial for the thriving field of bioelectronics. Alginate derivatives serve multiple functions, including their use in wound dressings, scaffolds for drug delivery and tissue engineering, as well as key components in hydrogel formulations. Recent studies highlight the immunomodulatory properties of alginate and its derivatives, including porphyrans, fucoidan, and chitin. These materials enhance the innate immune system, rebalance the Th1/Th2 ratio towards Th1, reduce IgE synthesis, and inhibit mast cell degranulation, alleviating allergic symptoms. In pharmaceuticals, alginate-based materials are utilised as substitutes and bio-linkers in 3D bioprinting, demonstrating their potential for creating complex tissue constructs. This review underscores the fundamental characteristics of alginates, outlines various chemical modification methodologies, and discusses recent developments in the fabrication of functional alginate-based composites. By presenting this synthesis of relevant information, we aim to inspire further scientific breakthroughs in the development of biocompatible electronic devices and intelligent materials.
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Therapeutic Potential of Flavonoids in Diabetes Mellitus Management: Molecular Insights and the Future Directions for Drug Design
More LessDiabetes mellitus (DM) is a prevalent metabolic disorder with a rapidly rising global incidence, presenting a significant burden to healthcare systems worldwide. Flavonoids, a class of naturally occurring polyphenolic compounds, are well-documented for their diverse pharmacological activities, particularly their anti-diabetic and anti-inflammatory effects. These secondary metabolites are commonly found in fruits, vegetables, and fungi and are classified into six main subclasses: flavanols, flavones, flavanones, isoflavones, anthocyanidins, and chalcones. The interplay between hyperglycemia, inflammation, and vascular complications in diabetes is now well recognized. Flavonoids with anti-diabetic properties may help mitigate inflammation by reducing hyperglycemia through various mechanisms. This review explores the antidiabetic potential and molecular mechanisms of citrus flavonoids, drawing on updated evidence from in vitro and in vivo studies. Flavonoids are shown to regulate biomarkers of glycemic control, lipid metabolism, renal function, hepatic enzymes, and antioxidant defenses. They also modulate signaling pathways implicated in glucose uptake and insulin sensitivity, which are central to the development of diabetes and its complications. Furthermore, this review synthesizes current knowledge on the antidiabetic effects of dietary flavonoids, emphasizing their molecular mechanisms in modulating key pathways such as glucose transporters, hepatic enzymes, tyrosine kinase inhibitors, AMP-activated protein kinase (AMPK), peroxisome proliferator-activated receptors (PPARs), and nuclear factor kappa B (NF-κβ). Further research is essential to deepen our understanding of flavonoids' therapeutic mechanisms in managing diabetes.
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Formulation, Optimization and Design of Capecitabine Nanosuspension to Enhance the Anti-gastric Cancer Efficacy using Box-Behnken Quality-based Design Study
More LessAuthors: Mayank Kumar Khede, Bhabani Shankar Nayak, Harekrishna Roy and Sisir NandiIntroductionCapecitabine is an anticancer antimetabolite of fluorouracil that inhibits cell proliferation and impairs DNA repair in cancer cells. It is given specifically to treat metastatic breast, gastric and colorectal cancers.
ObjectiveTo design, formulate, optimize and evaluate Capecitabine Nanosuspension using the QbD Box-Behnken model.
MethodsDeploying the Box-Behnken Design (BBD) model, Capecitabine nanosuspension was formulated with seventeen runs; the independent variables selected are Pullulan concentration, Poloxamer F407 concentration, and sonication time. The developed nanosuspension was evaluated for particle size, zeta potential, entrapment efficiency, in vitro drug release, and anti-cancer effectiveness. Drug-excipient compatibility was assessed using the Fourier transform infrared spectroscopy method. X-ray diffraction studies and differential scanning calorimetry were used to perform and assess the crystalline nature. Additionally, characteristics of the developed nanosuspension were assessed by performing a scanning electron microscopy study.
Results and DiscussionThe effect of various factors on key responses, namely particle size, entrapment efficiency, and drug release up to 8 hours, was assessed. A polynomial equation was employed through the analysis to optimize the formulation, considering the significance levels indicated by the p-values. Notably, these variables demonstrated a substantial influence on the responses. The comparison between observed and predicted values revealed a relatively minor variance (85.90, 69.57, and 76.34 for particle size, entrapment efficiency, and percentage drug release at 8 hours, respectively), indicating the model's suitability. The prepared nanosuspension exhibited compatibility with the used excipients, with capecitabine-entrapped nanoparticles uniformly dispersed within the suspending medium.
ConclusionDeveloped capecitabine nanosuspension demonstrated better efficacy and effectiveness against gastric cancer, with independent variables like pullulan and poloxamer F207 concentration, along with sonication time, influencing particle size, entrapment efficiency, and drug release.
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Advances in Periodontal Therapy: A Comprehensive Review of In-situ Forming Dental Cements for Effective Pocket Filling
More LessAuthors: Anuj Kumar, Anurag Verma, Phool Chandra and Vaibhav RastogiFifty percent of people worldwide suffer from periodontitis, a chronic inflammation of the soft tissue that surrounds the teeth. Effective filling of dental pockets is paramount for successful treatment outcomes in periodontal therapy. This review examines all the important aspects of in situ-forming dental cement for filling dental pockets. It focuses on the effectiveness of in-situ forming dental cement in filling periodontal pockets, the conditions necessary for their retention, their interaction with the periodontal environment and their potential performance in clinical practice. Through an in-depth analysis of current literature and clinical evidence, this review highlights the promising role of in-situ forming dental cement in enhancing periodontal therapy outcomes. The effectiveness of various filling systems, such as thermosensitive hydrogels, in-situ gel systems, microparticulate systems, and in-situ forming implants, is critically examined in this study. The advantages and disadvantages of each system are thoroughly examined, with a focus on their clinical uses and efficacy in the treatment of periodontitis. It explains the essential requirements for these cements in the periodontal environment, such as low viscosity for simple administration, the right setting time for stability, and regulated drug release mechanisms to sustain therapeutic concentrations over time. Alongside issues with formulation stability and biocompatibility, the suitability of these materials for the unique conditions present in periodontal pockets is assessed. In order to optimize these materials for better therapeutic effects and enhanced outcomes for patients in periodontal therapy, this study outlines potential directions for future research. It highlights the potential of in-situ forming dental cement to transform periodontal treatment by combining recent research findings with practical applications.
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Volumes & issues
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Volume 23 (2026)
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Volume 22 (2025)
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Volume 21 (2024)
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Volume 20 (2023)
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Volume 19 (2022)
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Volume 18 (2021)
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Volume 17 (2020)
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Volume 16 (2019)
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Volume 15 (2018)
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Volume 14 (2017)
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Volume 13 (2016)
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Volume 12 (2015)
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Volume 11 (2014)
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Volume 10 (2013)
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Volume 9 (2012)
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Volume 8 (2011)
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Volume 7 (2010)
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Volume 6 (2009)
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Volume 5 (2008)
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Volume 4 (2007)
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Volume 3 (2006)
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Volume 2 (2005)
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Volume 1 (2004)
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