Current Topics in Medicinal Chemistry - Online First
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81 - 100 of 106 results
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Multimodal Activity of a Novel Compound against Prostate and Pancreatic Cancer
Authors: Flaviana Alves dos Santos, Joelson Germano Crispim, Eduardo Davi Lima da Silva, Arsênio Rodrigues Oliveira, Aldilane Gonçalves da Fonseca, Telma Maria Araújo Moura Lemos, Ana Cristina Lima Leite, Michelle Melgarejo da Rosa, Maira Galdino da Rocha Pitta, Michelly Cristiny Pereira, Ivan da Rocha Pitta and Moacyr Jesus Barreto de Melo RêgoAvailable online: 19 March 2025More LessBackgroundProstate and pancreatic cancers pose significant global health challenges. This study explored the potential of compound 5b, a novel phthalimido-1,3-thiazole derivative, as an anticancer agent against these malignancies.
MethodsIn vitro, compound 5b exhibited potent cytotoxic activity against both prostate (DU-145 and PC-3) and pancreatic (Panc-1 and Mia Paca-2) cancer cell lines. Notably, it significantly reduced colony formation in PC-3 cells, potentially hindering tumor growth. Furthermore, treatment with compound 5b suppressed cell migration and induced cell cycle arrest in the PC-3 line. Additionally, it triggered cell death through late apoptosis and necrosis at higher concentrations. Safety evaluations in mice revealed no mortality or adverse effects after a 30-day treatment with compound 5b. Key blood parameters (hematology) and biochemical markers of liver and kidney function remained unaltered.
ResultsCompound 5b significantly reduced colony formation, suppressed cell migration, and induced cell cycle arrest and apoptosis/necrosis in prostate cancer cells. In vivo, safety evaluations showed no adverse effects in treated mice, with blood and biochemical markers remaining normal.
ConclusionThese findings suggest that compound 5b holds promise for further development as a therapeutic option for prostate and pancreatic cancers. Its multimodal activity profile, targeting cell viability, migration, cell cycle progression, and cell death, warrants further investigation.
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Antimicrobial Plant Peptides: Structure, Classification, Mechanism And Therapeutic Potential
Authors: Shaina Shahab Khan and Suaib LuqmanAvailable online: 17 March 2025More LessHumans, animals, and plants possess small polypeptides known as antimicrobial peptides (AMPs), which are often positively charged. They are tiny, mostly basic peptides with a molecular weight of 2 to 9 kDa. They are a crucial part of plants' innate defense system, acting as effector molecules that provide a resistance barrier against pests and diseases. Plants have been found to contain antimicrobial peptides belonging to numerous families, including plant defensins, thionins, cyclotides, and others. An increase in pathogen resistance is achieved through the transgenic overexpression of the relevant genes, while pathogen mutants that are susceptible to peptides exhibit decreased pathogenicity. For many organisms, AMPs exhibit a wide range of antimicrobial activity against various pathogens and serve as a crucial line of defense. This review raises awareness about plant antimicrobial peptides (AMPs) as potential therapeutic agents in the pharmaceutical and medical fields, including treating fungal and bacterial diseases. It also provides a broad synopsis of the main AMP families found in plants, their mechanisms of action, and the factors that influence their antimicrobial activities.
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The Impact and Role of Artificial Intelligence (AI) in Healthcare: Systematic Review
Authors: Kavya Singh, Ashish Prabhu and Navjeet KaurAvailable online: 03 March 2025More LessIntroductionHealthcare organizations are complicated and demanding for all stakeholders, but artificial intelligence (AI) has revolutionized several sectors, especially healthcare, with the potential to enhance patient outcomes and standard of life. Quick advancements in AI can transform healthcare by implementing it into clinical procedures. Reporting AI's involvement in clinical settings is vital for its successful adoption by providing medical professionals with the necessary information and tools.
BackgroundThis paper offers a thorough and up-to-date summary of the present condition of AI in medical settings, including its possible uses in patient interaction, treatment suggestions, and disease diagnosis. It also addresses the challenges and limitations, including the necessity for human expertise along with future directions. In doing so, it improves the understanding of AI's relevance in healthcare and supports medical institutions in successfully implementing AI technologies.
MethodsThe structured literature review, with its dependable and reproducible research process, allowed the authors to acquire 337 peer-reviewed publications from indexing databases, such as Scopus and EMBASE, without any time restrictions. The researchers utilized both qualitative and quantitative factors to assess authors, publications, keywords, and collaboration networks.
ResultsAI implementation in healthcare holds enormous potential for enhancing patient outcomes, treatment recommendations, and disease diagnosis. AI technologies can use massive datasets and recognize patterns to beat human performance in various healthcare domains. AI provides improved accuracy, reduced expenses, and time savings. It can transform customized medicine, optimize drug dosages, improve management of population health, set guidelines, offer digital medical assistants, promote mental health services, boost patient knowledge, and maintain patient-clinician trust.
ConclusionAI can be utilized to detect diseases, develop customized therapy plans, and support medical professionals with their clinical decision-making. Instead of just automating jobs, AI focuses on creating technologies that can improve patient care in several healthcare settings. However, challenges such as biasness, data confidentiality, and data quality must be resolved for the appropriate and successful integration of AI in healthcare.
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Chemical Profiling and Antibacterial Potential of Methanol Extract of Solanum xanthocarpum Fruits against Methicillin-Resistant Staphylococcus aureus: Implications for AMR Management
Available online: 03 March 2025More LessAimTo investigate the antimicrobial potential of methanol fruit extract of Solanum xanthocarpum against Methicillin-Resistant Staphylococcus aureus (MRSA) and elucidate its mode of action.
BackgroundThe rise of antimicrobial resistance (AMR) demands the exploration of alternative therapeutic strategies to combat resistant pathogens.
ObjectiveTo evaluate the efficacy of Solanum xanthocarpum methanol extract against MRSA, and identify its active constituents and mechanism of action.
MethodsThe fruits of Solanum xanthocarpum were extracted using various solvents, with hexane and methanol yielding the highest results. Microbroth dilution assays assessed antimicrobial activity, while in vitro assays such as Alamar blue, Scanning Electron Microscopy (SEM), protein, and nucleic acid leakage examined metabolic disruption and cell membrane integrity. Gas Chromatography-Mass Spectrometry (GC-MS) was used to identify active compounds, and molecular docking studies assessed interactions with key MRSA proteins.
ResultsThe methanol extract demonstrated significant antimicrobial activity against MRSA, causing metabolic disruption and leakage of cellular contents as evidenced by various in vitro assays including alarm blue, SEM, and protein and nucleic acid leakage assay. GC-MS analysis identified alpha-linoleic acid and palmitic acid as key active components. Molecular docking studies confirmed their inhibition of beta-lactamase activity, cell wall biosynthesis, efflux pumps, and virulence factors.
ConclusionThe findings suggest that Solanum xanthocarpum methanol fruit extract has promising potential as a natural remedy against AMR associated with MRSA.
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Application of Artificial Intelligence-Based Approaches in the Discovery and Development of Protein Kinase Inhibitors (PKIs) Targeting Anticancer Activity
Available online: 28 February 2025More LessHerein, we present an in-depth review focused on the application of different artificial intelligence (AI) approaches for developing protein kinase inhibitors (PKIs) targeting anticancer activity, focusing on how the AI-based tools are making promising advances in drug design and development, by predicting active compounds for essential targets involved in cancer. In this context, the machine learning (ML) approach performs a critical role by promoting a fast analysis of a thousand potential inhibitors within a small gap of time by processing large datasets of chemical data, putting it at a higher level than other traditionally used methods for screening molecules. In general, AI-based screening of compounds reduces the time of the work and increases the chances of success in the end. Additionally, we have covered recent studies focused on the application of deep neural networks (DNNs) and quantitative structure-activity relationships (QSAR) to identify PKIs. Furthermore, the paper covers new AI-based methodologies for filtering or improving datasets of potential compounds or even targets, such as generative models for the creation of novel compounds and ML-based strategies to collect information from different databases, increasing the efficiency in drug design and development. Finally, this review highlights how AI-based tools are increasing and improving the field of PKIs targeting cancer, making them an alternative for the future in the medicinal chemistry field.
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Diverse Therapeutic Potentials of Hypericin: An In-Depth Review
Authors: Sandeep Kumar Maurya, Sheetal Divakar, Sunny Rathee and Umesh Kumar PatilAvailable online: 27 February 2025More LessBackgroundThis review is delving into determining the content and significance of hypericin, a pharmacologically important constituent commonly known as St. John's Wort (SJW). The paper explores the rich history of Hypericin's traditional use in alternative medicine and the recent surge in scientific interest surrounding its bioactive properties.
ObjectiveThis review aims to provide a comprehensive analysis the therapeutic potentials of hypericin, focusing on its chemistry, extraction, sources, stability, pharmacokinetics, safety profile, and multifunctional applications in drug and medicinal fields as well as advancements in Bioengineering Approaches for Enhanced Hypericin Delivery.
MethodsWe performed a non-systematic search of journals. Literature using computerized methods was conducted, utilizing databases such as Medline (PubMed), ChemSciFinder, China National Knowledge Infrastructure (CNKI) and Scirus Library. To effectively identify the most important and relevant research articles, scientific studies, clinical studies and review articles on hypericin were searched using different keywords: “Hypericum”, “traditional use”, “phytochemistry”, “pharmacology”, “drug delivery” and “bioactivity”. Thus, articles available from 1984 to 2024 were analyzed and collected. The selection process for the review primarily considered the originality of the paper and its clinical applications.
ResultsAlthough hypericin is not a novel compound within the research community, it is gaining renewed recognition and showing great effectiveness as a promising agent in the field of medical diagnostics and has promising applications as a therapeutic.
ConclusionHere, our current comprehensive review of hypericin, its potential and its activities is intended to contribute to this ongoing process actively. Overall, this review provided theoretical direction for future hypericin research. Future studies should, therefore, focus further on the pharmacological processes, pharmacokinetics, and chemistry of hypericin and hypericin-based drug delivery systems. This comprehensive review of hypericin aims to actively contribute to ongoing research and provide a theoretical direction for future studies.
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Therapeutic Potential of Quercetin in Type 2 Diabetes Based on a Network Pharmacology Study
Available online: 13 February 2025More LessIntroductionCurrently, there are pharmacological treatments for type 2 diabetes (T2D), but these are ineffective. Quercetin is a flavonoid with antidiabetic properties.
ObjectiveThis research aimed to identify the molecular mechanism of Quercetin in T2D from network pharmacology.
MethodsWe obtained T2D-related genes from MalaCards and DisGeNET, while potential targets for Quercetin were sourced from SwissTargetPrediction and Comparative Toxicogenomics databases. The overlapping genes were identified and analyzed using ShinyGO 0.77. Subsequently, we constructed a protein-protein interaction network using Cytoscape, conducted molecular docking analyses with SwissDock, and validated the results through molecular dynamics simulation in GROMACS.
ResultsQuercetin is involved in apoptotic processes and in the regulation of insulin activity, estrogen, prolactin and EGFR receptor. The key driver genes AKT1, GSK3B, SRC, IGF1R, MMP9, ESR2, PIK3R1, and MMP2 showed high concordance in the molecular docking study, and molecular dynamics showed stability between Quercetin and ESR2 and PIK3R1.
ConclusionsOur work helps to identify the molecular mechanism and antidiabetic effect of quercetin, which needs to be studied experimentally.
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WISP3/CCN6 Adipocytokine Marker in Patients with Non-alcoholic Fatty Liver Disease (NAFLD) and its Association with Some Risk Factors
Available online: 11 February 2025More LessIntroductionCCN6/WISP3 is a member of the CCN adipokines family that can exert multiple effects on metabolic pathways. So far, the function of CCN6 in the pathogenesis of NAFLD has not been known well. Hence, we aimed to examine CCN6 serum levels in patients with NAFLD compared to healthy individuals and its association with some risk factors for the first time.
MethodThis case-control study measured serum levels of CCN6, TNF-α, IL-6, adiponectin, and fasting insulin using ELISA kits in 88 NAFLD patients and 88 controls. In addition, other biochemical variables, including AST, ALT, lipid profiles, and FBG, were determined using an Auto analyzer instrument.
ResultsA remarkable decrease in CCN6 levels was found in the NAFLD patients (1501.9543 ± 483.414 pg/ml) compared to the healthy group (1899.4856 ± 559.704 pg/ml, P < 0.001). In NAFLD patients, a negatively notable correlation was observed between CCN6 and the levels of insulin (r = -0.278, P = 0.011), HOMA-IR (r = -0.268, P = 0.014), as well as TNF-α (r = -0.343, P = 0.001). A remarkable association was found between CCN6 and the risk factor of NAFLD in the adjusted model for gender, age, and BMI with OR = 0.867 (95% CI, [0.806-0.931], P < 0.001).
ConclusionOur findings showed a significant reduction in CCN6 levels in the NAFLD patients compared to the healthy group, as well as the developing risk of NAFLD enhanced with the decrease of CCN6 levels.
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Therapeutic Potential of Simvastatin: Cellular Mechanism, Binding Energetics, and Resistance Developments
Available online: 30 January 2025More LessStatins are a class of hypolipidemic agents that have been shown to promote osteogenic differentiation through enhanced alveolar bone recovery, inserted osseointegration, and cartilage regeneration. This review uses Molecular Docking (MD) simulations and additional Computer-Aided Drug Design (CADD) methods to present the state of the art in statin therapy. Furthermore, several studies have shown that factors such as limited overall absorption, metabolism in the first pass, and systemic side effects are among those that affect the oral administration of statins. In addition, these variables include susceptibility to efflux mechanisms, drug permeability, dissolution percentage, aqueous solubility, initial metabolism, and pre-systemic metabolism. Additionally examined are the pharmacokinetics of the statin and in vivo mechanisms of action. As a result of the numerous problems associated with the consumption of statins, including their low total bioavailability, first-pass metabolism, low aqueous solubility, and systemic adverse reactions, a non-oral mode of administration was looked into for this crucial and primary class of pharmacokinetic agents. However, to optimize bioavailability and minimize side effects, more research is required.
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A Recent Progress in Biological Activities of 1,3,4-thiadiazole and its Derivatives: A Review
Available online: 30 January 2025More Less1,3,4-thiadiazole can be produced in several ways and has a wide range of possible biological uses. As a result, scientists have created novel procedures for producing 1,3,4-thiadiazole derivatives and their use in medicine. Among the activities are Anticancer, anticonvulsant, antimicrobial, antifungal, antiinflammatory, antiHIV, antidiabetic, antitubercular, antifungal, and other properties. We have compiled different biological activities of 1,3,4-thiadazole in this review study. Many researchers may find the material on this page helpful, which could result in the identification of new medicinal species beneficial to society.
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Roles of C/EBPβ/AEP in Neurodegenerative Diseases
Authors: Jing Guo, Xin-Yi Liu, Sha-Sha Yang, Qiang Li, Yang Duan, Shan-Shan Zhu, Ke Zhou, Yi-Zhi Yan and Peng ZengAvailable online: 27 January 2025More LessIn recent years, an increasing number of studies have shown that increased activation of aspartic endopeptidases (AEPs) is a common symptom in neurodegenerative diseases (NDDs). AEP cleaves amyloid precursor protein (APP), tau (microtubule-associated protein tau), α-synuclein (α-syn), SET (a 39-KDa phosphoprotein widely expressed in various tissues and localizes predominantly in the nucleus), and TAR DNA-binding protein 43 (TDP-43), and promotes their aggregation, contributing to Alzheimer's disease (AD), Parkinson's disease (PD), Huntington's disease, multiple sclerosis (MS), amyotrophic lateral sclerosis (ALS), and frontotemporal dementia (FTD) pathogenesis. Abundant evidence supports the notion that CCAAT/enhancer-binding protein β (C/EBPβ)/AEP may play an important role in NDDs. Developing its small molecule inhibitors is a promising treatment of NDDs. However, current research suggests that the pathophysiological mechanism of the C/EBPβ/AEP pathway is very complex in NDDs. This review summarizes the structure of C/EBPβ and AEP, their major physiological functions, potential pathogenesis, their small molecule inhibitors, and how C/EBPβ/AEP offers a novel pathway for the treatment of NDDs.
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Osseointegration Process Improving via Functionalization of Titanium Dioxide Nanotubes: A Bibliometric Analysis and Systematic Review
Available online: 21 January 2025More LessIntroduction/ObjectivesFailures of osseointegrated implants pose a significant challenge in the medical field, often attributed to prolonged osseointegration periods and bacterial infections. Functionalization of Titanium Dioxide Nanotubes (TNTs) has emerged as a promising strategy to improve osseointegration and mitigate infections. This study aims to conduct a bibliometric analysis and systematic review to identify trends, gaps, and advancements in research on the functionalization of TNTs for osseointegration improvement.
MethodsArticles were retrieved from the Web of Science database using the keywords “osseointegration,” “titanium dioxide nanotubes,” and “functionalization.” The inclusion criteria were studies published between 2014 and 2023, written in English, and focusing on the use of TNTs in implant surface modifications. A total of 126 articles were included after screening. Data extraction and analysis were performed using VOS Viewer, Microsoft Excel, and GraphPad Prism.
ResultsThe review revealed a growing number of publications on TNT functionalization, with China, the United States, and Brazil leading in contributions. Key findings include the effectiveness of TNTs loaded with bioactive agents (e.g., silver, strontium, hydroxyapatite) in promoting osseointegration and antibacterial activity. Collaborative networks among institutions and authors were mapped, highlighting the Sao Paulo State University and Yong Huang as the most prolific contributors.
ConclusionThe findings underscore the potential of TNT functionalization to enhance implant performance. However, a gap remains in translating preclinical findings into clinical trials. Future research should focus on clinical validation to bridge this gap and translate laboratory advancements into therapeutic solutions.
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Advances in the Study of Halogenated Natural Products
Authors: Lijing Zhang, Bing Liu, Ting Zhu, Xue Tian, Ning Chen and Yuxin WangAvailable online: 21 January 2025More LessHalogenated natural products are an important class of secondary metabolites that are widely distributed in nature. The presence of halogen atoms usually enhances the pharmacological activity of the compounds. As a result, halogenated natural products have shown promising pharmacological activities in antibacterial, antitumour, anti-inflammatory and antiplasmodial properties, providing a rich resource for the development of new drugs. To date, more than 62% of halogenated compounds are produced by marine organisms, mainly including marine sponges, algae, corals, fungi and other organisms. In addition, terrestrial microorganisms, including bacteria and fungi, also produce halogenated metabolites, which are equally important sources of halogenated natural products. The biosynthesis of halogenated natural products involves the synergistic action of multiple enzymes that efficiently and selectively bind halogen atoms to organic molecules, a process that enhances the biological activity of the compounds. Halogenated natural products have a wide range of uses as important raw materials in the agricultural, pharmaceutical and chemical industries. This paper reviews the progress of research on halogenated compounds and their biosynthesis in recent years, laying the foundation for further utilisation and development of halogenated compounds.
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Synthesis, X-Ray Structure, Characterization, Antifungal Activity, DFT, and Molecular Simulation of a Novel Pyrazole Carboxylic Acid
Available online: 21 January 2025More LessBackgroundThe search for new antifungal agents is critical due to the rising resistance of fungal pathogens to existing treatments. This study focuses on the synthesis and evaluation of a novel compound, 1-benzyl-5-methyl-1H-pyrazole-3-carboxylic acid (compound L1), as a potential antifungal agent.
MethodsCompound L1 was synthesized and characterized using a range of analytical techniques, including 1H^1H1H NMR, 13C^{13}C13C NMR, FT-IR, GC-MS, and X-ray single crystal diffraction (XRD). The antifungal activity of the compound was assessed in vitro, and its molecular structure was studied using Density Functional Theory (DFT). Molecular docking and dynamics simulations were conducted to evaluate the interaction of the compound with sterol 14-alpha demethylase (CYP51) from Candida albicans. ADME/Tox evaluations were also performed to assess the drug-like properties of compound L1.
ResultsCompound L1 exhibited moderate antifungal activity with an IC50 value of 34.25 µg/mL. DFT studies confirmed the highly stable molecular structure of the compound. Molecular docking and dynamics simulations demonstrated that compound L1 had a higher affinity and stability when forming complexes with the crystal structure of CYP51, particularly in interaction with the tetrazole-based antifungal drug candidate VT1161 (PDB ID: 5TZ1). ADME/Tox evaluations indicated favorable drug-like properties for compound L1.
ConclusionThe results suggest that compound L1 is a promising antifungal candidate, showing greater potential than fluconazole in the conducted evaluations. Further studies are warranted to explore its full therapeutic potential.
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Synthetic Strategies for the Development of Ibuprofen Derivatives: A Classified Study
Authors: Kuchana Madhavi and Barla Karuna DeviAvailable online: 10 January 2025More LessIbuprofen, a widely used NSAID from the aryl propionic acid class, effectively relieves pain, fever, and inflammation. On prolonged use, it leads to gastrointestinal, hepatic, and renal toxicities, particularly gastrointestinal ulcers. These side effects are largely attributed to the carboxylic acid functional group common to NSAIDs. The present review highlights the different modifications done to the carboxylic group in Ibuprofen, by various researchers such as estersgramma, amides, hydroxamic acids, and N-substituted hydrazides, along with the integration of heterocyclic moieties like triazoles, tetrazoles, and oxadiazoles. Additionally, Ibuprofen has been hybridized with other drugs and complexed with metals to enhance therapeutic effects. The different synthetic strategies that were employed were esterification, amidation, condensation, Schiff’s base formation, etc. These modifications have resulted in derivatives with antimicrobial, antifungal, anticancer, and other biological activities, aiming to reduce side effects while retaining or enhancing anti-inflammatory, analgesic, and antipyretic properties.
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Targeting Malaria's Achilles' Heels: A Review of Plasmodium Life Cycle Vulnerabilities for Drug Discovery
Authors: Shruti Shukla, Shikha Kushwah and Ashutosh ManiAvailable online: 10 January 2025More LessThe global rise of drug-resistant malaria parasites is becoming an increasing threat to public health, emphasizing the urgent need for the development of new therapeutic strategies. Artimisinin-based therapies, once the backbone of malaria treatment, are now at risk due to the resistance developed in parasites. The lack of a universally accessible malaria vaccine exacerbates this crisis, underscoring the need to explore new antimalarial drugs. A more comprehensive understanding of the parasites’s life cycle has revealed several promising targets, including enzymes, transport proteins, and essential metabolic pathways that the parasite relies on for its survival and proliferation. This review provides an in-depth analysis of the vulnerabilities displayed by Plasmodium and recent advances that highlight potential drug targets and candidate molecules.
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Conformation Study and Design of Novel 6-Hydroxybenzothiazole-2-Carboxamides as Potentially Potent and Selective Monoamine Oxidase B Inhibitors for Neuroprotection
Authors: Dong Xie, Penghang Guo, Quantang Zhao, Yu Gao, Jianan Zhang and Jie ZhouAvailable online: 10 January 2025More LessBackground6-hydroxybenzothiazole-2-carboxamide is a novel, potent, and specific monoamine oxidase B inhibitor that can be used to study the structure of molecules and come up with new ways to protect neurons.
ObjectiveThe objective of this work was to create an effective model using derivatives of 6-hydroxybenzothiazole-2-carboxamide and establish a dependable predictive foundation for the development of neuroprotective monoamine oxidase B inhibitors for the treatment of neurodegenerative diseases.
MethodsThe construction and optimization of all compounds were carried out sequentially using ChemDraw software and Sybyl-X software. The optimized compounds were further analyzed using the COMSIA approach and the Sybyl-X software tool for QSAR modeling. A set of novel compounds of 6-hydroxybenzothiazole-2-carboxamide were created and their IC50 values were forecasted using QSAR modeling. Ultimately, the recently developed compounds underwent a screening process using their IC50 values, and molecular docking tests were conducted on the ten most promising compounds with the highest IC50 values.
ResultsThe 3D-QSAR model exhibited favorable outcomes. The value of q2 in the COMSIA model was 0.569. The model demonstrated a superior r2 value of 0.915, a lower SEE of 0.109, and a higher F-value of 52.714. The statistical findings and validation of the model were deemed adequate. Furthermore, analyzing the contour plots might assist in identifying the necessary structural specifications.
ConclusionThis work has the potential to provide an insight into the development of active medicines that protect the nervous system against neurodegenerative disorders.
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Traditional Chinese Medicine for Liver Cancer Treatment: Network Pharmacology Research
Authors: Shihao Zheng, Yixiao Gu, Wenying Qi, Wei Wang, Xiaoke Li, Xiaobin Zao, Size Li, Shaoyu Liu, Tianyu Xue, Yongan Ye and Aimin LiuAvailable online: 09 January 2025More LessBackgroundAs one of the common malignant tumors nowadays, liver cancer has more risk factors for its development and is characterized by a high recurrence rate, high mortality rate, and poor prognosis, which poses a great threat to people's health. The specific efficacy of traditional Chinese medicine is based on clinical practice, which is a high degree of generalization of the characteristics and scope of the clinical effects of prescription medicines and a special form of expression of the medical effects of the human body within the scope of traditional Chinese medicine. Because of its multi-ingredient, multi-target, and multi-pathway characteristics, it has a great advantage in the treatment of liver cancer. Still, at present, its specific molecular mechanism of action has not yet been clarified.
AimThis study reviews the current status and characteristics of network pharmacology research in the treatment of liver cancer, aiming to provide new ideas and methods for traditional Chinese medicine treatment of the disease.
MethodsThis study was searched on the Web of Science and PubMed using keywords, such as “traditional Chinese medicine”, “liver cancer,” and “network pharmacology.” The citation dates of the literature cited in this review are from 2000 to 2024.
ResultsThe discovery of the key molecular mechanisms of traditional Chinese medicine in the treatment of liver cancer through the network pharmacology approach and the in-depth study of the related signaling pathways are conducive to a more in-depth exploration of traditional Chinese medicine.
ConclusionNetwork pharmacology research plays a key role in the treatment and prevention of liver cancer and deserves deeper exploration in the future.
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Benzimidazole Derivatives in Breast Cancer: Target-Specific Therapeutic Breakthroughs
Available online: 07 January 2025More LessDespite ongoing advancements in drug design and developments, breast cancer remains a serious and devastating disease and is ranked as the second most common illness in women. Breast cancer rates have increased significantly during the last 40 years. This necessitates the development of novel treatment techniques. Currently, chemotherapy is the primary mode of treatment for breast cancer; however, its toxicity to normal cells and drug resistance are considered the main obstacles. Researchers are looking for novel anti-breast cancer medication classes to improve cancer therapy efficacy and survival rates. Using non-targeting medicines in a 'one-size-fits-all' strategy can harm healthy cells and may not be effective for all patients. Thus, now, the treatment of breast cancer is exploring targeted-based therapy. The tactics involved in this therapy may improve patient survival rates, but their extended usage can lead to significant side effects and medication resistance. Targeted therapy enables precision medicine by targeting particular oncogenic markers in malignancies. Because of their strong cytotoxicity against several cancer cell types, heterocyclic compounds play an important role in the development of therapeutically effective anticancer drugs. Benzimidazole derivatives have grown in favour of anti-breast cancer medicines in recent years due to their broad biological characteristics and therapeutic applications. This review provides healthcare professionals and researchers with an overview of current breakthroughs (2019-2024) in benzimidazole derivatives as breast cancer-targeted therapy, based on the perspectives of leading experts. We have illuminated the diverse and evolving landscape of hybridized benzimidazole, along with its biological targets and anti-breast cancer activity. Further, we also have compiled the various ongoing clinical trials of benzimidazole scaffolds as anti-breast cancer agents. A detailed illustration of the structure-activity connection with special emphasis is provided. The effort may help to develop potent, selective, and effective drugs to combat breast cancer.
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