Mini reviews in medicinal chemistry最新文献

{"title":"Hybrid Pharmacophores in Cancer Treatment: Emphasis on Coumarinbased Scaffolds and Their Multi-target Mechanisms.","authors":"Sanheeta Chakrabarty, Rimmi Lata, Sanju Kumari, Sanjay Kumar, Shreyans K Jain","doi":"10.2174/0113895575435130260401102109","DOIUrl":"https://doi.org/10.2174/0113895575435130260401102109","url":null,"abstract":"<p><p>Hybrid molecules have emerged as a promising strategy in anti-cancer drug discovery, offering the ability to simultaneously modulate multiple molecular targets and overcome limitations associated with conventional chemotherapeutics. This review presents an updated and systematically organized overview of recent advancements (2013-2025) in the design, synthesis, and biological evaluation of coumarin-based hybrid molecules with anti-cancer potential. Coumarin, owing to its structural versatility, natural abundance, and broad spectrum of pharmacological profiles, has become a valuable scaffold for generating hybrid pharmacophores with enhanced potency, selectivity, and reduced off-target toxicity. We summarize major classes of coumarin-integrated hybrids, including sulfonamide, thiazole, triazole, indole, quinoline, pyridine, chalcone, pyrazole, and selenophene conjugates, highlighting representative molecules, their cytotoxic profiles, and mechanistic insights into their modes of action. Additionally, the mechanistic section elucidates how hybrid entities exert anti-cancer effects either by coordinated modulation of multiple nodes within key signaling pathways (such as PI3K/Akt/mTOR, MAPK/ERK, NF-κB, and apoptotic networks) or by synergistic interaction at different sites of the same molecular target. Collectively, the evidence underscores molecular hybridization as a robust medicinal chemistry approach and positions coumarinbased hybrids as promising candidates for future anti-cancer drug development.</p>","PeriodicalId":18548,"journal":{"name":"Mini reviews in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":3.3,"publicationDate":"2026-04-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147840020","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Antimicrobial Efficacy and Mechanistic Insights of 0D, 1D, 2D, and 3D Nanoparticles: A Review.","authors":"Shruthi Venkataraman, Raji Atchudan, Sandeep Arya, Surendra H Mahadevegowda, Ashok K Sundramoorthy","doi":"10.2174/0113895575428691260122055445","DOIUrl":"https://doi.org/10.2174/0113895575428691260122055445","url":null,"abstract":"<p><p>The escalating global challenge of Antimicrobial Resistance (AMR) underscores the urgent need for alternative therapeutic approaches beyond conventional antibiotics. Nanoparticles (NP), with their distinct physicochemical properties, tunable morphologies, high surface reactivity, and structural diversity, have emerged as promising candidates in combating microbial infections. This review adopts a dimensional framework encompassing zero-dimensional (0D), one-dimensional (1D), two-dimensional (2D), and three-dimensional (3D) nanostructures to systematically classify and analyze their antimicrobial mechanisms. Key bactericidal pathways explored include the generation of Reactive Oxygen Species (ROS), physical disruption of microbial membranes, controlled metal ion release, and light-mediated effects such as photothermal and photodynamic actions. Each dimensional class of NPs exhibits unique interactions with bacterial cells, influenced by parameters such as geometry, crystallinity, surface chemistry, and specific surface area, all of which collectively dictate their antimicrobial potency and selectivity. Furthermore, nanotoxicity, scalability, and clinical applications have also been addressed. This review focuses on the rational design and optimization of next-generation nanomaterials by linking nanostructural characteristics to specific antibacterial pathways. Such an approach provides an outline for customizing NP-based systems to more effectively fight resistant infections. Furthermore, we discussed the development of novel, multi-mechanistic techniques for reducing the global burden of AMR and promoting the transition of nanotechnology-enabled antimicrobials from laboratory research to real-world clinical and environmental applications.</p>","PeriodicalId":18548,"journal":{"name":"Mini reviews in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":3.3,"publicationDate":"2026-04-27","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147839988","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Metal-based Chemotherapeutics Targeting Oral Cancer: A Review.","authors":"Fahad Saeed Algahtani, Mohammed Abdullah Alzubaidi, Abdullah M Al Shumrani, Amal Adnan Ashour","doi":"10.2174/0113895575445956260409195724","DOIUrl":"https://doi.org/10.2174/0113895575445956260409195724","url":null,"abstract":"<p><p>Oral cancer, primarily oral squamous cell carcinoma (OSCC), remains a significant global health challenge due to its high morbidity, frequent late-stage diagnosis, and limited therapeutic options. Metal-based chemotherapeutics have emerged as promising anticancer agents due to their unique physicochemical properties. These drugs can induce cell apoptosis via different mechanisms, such as the generation of free radicals, oxidative stress, inhibition of certain enzymes, and DNA binding ability. The above-mentioned properties lead to the development of metal-based drugs as a strategy for OSCC. Moreover, the metal complexes enhance cell apoptosis through disturbing different cancer pathways, as well as the suppression of certain gene expression responsible for cancer. Also, the emergence of a hybrid approach that constitutes both the metal center and organic linkers, such as metal-organic frameworks (MOFs), has been used as a carrier of anticancer drugs, detection, imaging, and release of drugs at the acidic pH of the cancer cells has opened new biocompatible and tunable platforms for cancer treatment. This review focuses on the applications of metal-based drugs, such as coordination complexes, MOFs, and metal/metal oxide nanoparticles, and their recent development in the treatment of oral cancer, with special emphasis on their mode of action, clinical applications, and biocompatibility. We expect that the current review will provide comprehensive details and guidance on the development of metal-based chemotherapeutic agents and their current applications in oral cancer.</p>","PeriodicalId":18548,"journal":{"name":"Mini reviews in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":3.3,"publicationDate":"2026-04-24","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147839956","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"The Tripartite Regulatory Framework of the Skin Extracellular Microenvironment and Related Anti-aging Strategies.","authors":"Liangsen Zhao, Yong Liao","doi":"10.2174/0113895575436479260306062725","DOIUrl":"https://doi.org/10.2174/0113895575436479260306062725","url":null,"abstract":"<p><p>This review proposes a tripartite regulatory framework for the Skin Extracellular Microenvironment (SEM), which the authors conceptualize as three cross-talked functional domains: hydration, nutritional, and signaling microenvironments. It systematically elaborates on the core functional architectures of each component-for instance, Hyaluronic Acid (HA) as the foundational element of the hydration microenvironment, collagen-based transport pathways in the nutritional microenvironment, and multi-axis signal networks (inflammatory, biochemical, mechanical) in the signaling microenvironment. Based on this, age-related dynamic alterations within each domain were further delineated: the hydration microenvironment undergoes progressive HA degradation and reduced biosynthesis, leading to decreased skin water retention, increased transepidermal water loss, and clinical manifestations like dryness and fine lines; the nutritional microenvironment exhibits microvascular degeneration, disrupted nutrient transport, and advanced glycation end-product accumulation, impairing extracellular matrix metabolic homeostasis; the signaling microenvironment suffers from chronic inflammation, TGF-β/Smad pathway imbalance, and mechanical signaling dysfunction, triggering a cascade of \"inflammatory activation-uncontrolled degradation- mechanical disruption.\" Cross-regulatory interactions among the three microenvironments (e.g., hydration-signaling coupling via TGF-β/HAS2) are summarized to highlight their integrated regulatory nature. Additionally, targeted anti-aging strategies are discussed: exogenous HA supplementation and endogenous activation for the hydration microenvironment, metabolic substrate supply (e.g., proline, trace elements) for the nutritional microenvironment, and multi-pathway modulation (e.g., anti-inflammatory agents, platelet-rich plasma, collagen stimulants) for the signaling microenvironment, with particular attention to the synergistic effects observed in combination approaches such as mesotherapy-based cocktails and exosome therapy. Overall, this framework integrates previously fragmented SEM research and provides a coherent theoretical basis for evidence-based clinical anti-aging strategies and future precision interventions targeting skin aging.</p>","PeriodicalId":18548,"journal":{"name":"Mini reviews in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":3.3,"publicationDate":"2026-04-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147776066","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Extraction and Mass Spectrometry Detection of Cannabinoids in Clinical Samples.","authors":"Matthew Coughlin, Mahdi Garelnabi","doi":"10.2174/0113895575403595251119091701","DOIUrl":"https://doi.org/10.2174/0113895575403595251119091701","url":null,"abstract":"<p><p>The legalization of cannabis products across many states in the USA has sparked a surge of interest within the scientific and medical communities, prompting researchers to investigate the pharmacological and mechanistic properties of the numerous bioactive compounds found in cannabis. Among these, cannabinoids, such as tetrahydrocannabinol (THC) and cannabidiol (CBD), have garnered particular attention due to their potential therapeutic effects and psychoactive properties. A foundational step in understanding the behavior and impact of these compounds involves their accurate identification and quantification, which hinges on the effectiveness of various detection techniques. However, before these methods can be employed, cannabinoids must be isolated from complex biological matrices, such as blood, urine, or tissue, using precise extraction protocols that preserve compound integrity and minimize degradation. This analytical review not only provides a detailed overview of the extraction procedures used to isolate cannabinoids from biological samples but also explores the principles, advantages, and limitations of common detection techniques. Special focus is placed on chromatographic methods, such as gas chromatography (GC) and liquid chromatography (LC), which are frequently coupled with mass spectrometry (MS), as well as on immunoassay-based approaches that offer rapid, cost-effective screening options. The review aims to highlight the evolving landscape of analytical methodologies in cannabinoid research, especially considering growing clinical, forensic, and regulatory interests.</p>","PeriodicalId":18548,"journal":{"name":"Mini reviews in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":3.3,"publicationDate":"2026-04-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147776097","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Polymer-doxorubicin Conjugates: Redefining Chemotherapy for Breast Cancer.","authors":"Sneha Kumari, Aman Kumar, Md Mustahidul Islam, Nitin Singh, Preeti Patel, Balak Das Kurmi","doi":"10.2174/0113895575471485260408204857","DOIUrl":"https://doi.org/10.2174/0113895575471485260408204857","url":null,"abstract":"<p><p>Polymer drug conjugates (PDCs) represent a targeted modification of conventional chemotherapeutics, transforming small-molecule drugs like doxorubicin (dox) into macromolecular structures with significantly altered biological properties. By incorporating a biocompatible polymer backbone, a cleavable linker, and an active cytotoxic payload, PDCs achieve prolonged systemic persistence, advantageous biodistribution, and tumor-specific release. This architecture facilitates more reliable exploitation of the enhanced permeability and retention (EPR) effect, thereby encouraging preferential intratumoral accumulation while reducing off-target exposure. The regulated and microenvironment-sensitive release of dox provides a logical approach to mitigate cardiotoxicity, a significant limitation of anthracycline treatment. PDCs can partially bypass efflux-mediated multidrug resistance by using endocytic uptake pathways rather than transporter-dependent mechanisms. Prototypical systems such as HPMA-dox and PEG-dox offer persuasive translational evidence that macromolecular conjugation can enhance the therapeutic index of dox. PDCs collectively demonstrate how advanced molecular engineering might rejuvenate traditional chemotherapeutics for contemporary oncology.</p>","PeriodicalId":18548,"journal":{"name":"Mini reviews in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":3.3,"publicationDate":"2026-04-14","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147776076","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Therapeutic Potentials of Pyridine Derivatives, Highlighting the Synthetic Pathway, Biological Activity, and Structure-activity Relationship: A Mini- Review.","authors":"Muhammad Majed Abdin, Mustapha Suleiman, Syazwani Itri Amran, Helmi Mohammed Al-Maqtari, Sarkar M A Kawsar, Joazaizulfazli Jamalis","doi":"10.2174/0113895575449756260317054228","DOIUrl":"https://doi.org/10.2174/0113895575449756260317054228","url":null,"abstract":"<p><p>Heterocyclic compounds constitute the largest family in organic chemistry. Their potential to treat and deter various types of diseases renders them essential compounds. Moreover, their extensive implementations in drug discovery and development are significantly contributing to the current state of medicinal chemistry. Pyridine is one of the most fundamental heterocyclic compounds. Pyridine-based compounds are structurally diverse and have been utilized to tackle various challenges in pharmaceuticals and medicinal chemistry, providing novel approaches for enhanced health accomplishments. The main objective of this review is to comprehensively clarify the crucial role of pyridine derivatives in drug discovery between 2015 and 2025 by summarizing the various synthetic pathways and evaluating their therapeutic relevance. In addition, it highlights the outstanding pharmacological applications of pyridine-containing compounds across a broad range of therapeutic areas, such as oncology, infectious diseases, inflammatory disorders, oxidative stress-related conditions, metabolic disorders, and neurodegenerative diseases, emphasizing their prominence among clinically approved drugs. Furthermore, structure-activity relationship analyses are investigated to illustrate how particular substitutions, electronic effects, and positional modifications on the pyridine ring affect biological potency, selectivity, and pharmacokinetic behavior. Finally, by integrating synthetic approaches, biological evaluations, and structure-activity relationship insights, this review aims to support the rational design and optimization of more potent, selective, and safer pyridine- based therapeutic agents for future drug development.</p>","PeriodicalId":18548,"journal":{"name":"Mini reviews in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":3.3,"publicationDate":"2026-04-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147618765","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Immunomodulatory Mechanisms in Regenerative Therapies: Enhancing Healing and Modulating Inflammation in Breast Cancer.","authors":"Jyoshna Rani Dash, Pragyanjeeta Panda, Ashirbad Nanda, Gurudutta Pattnaik","doi":"10.2174/0113895575428046260311055441","DOIUrl":"https://doi.org/10.2174/0113895575428046260311055441","url":null,"abstract":"<p><p>The immune system is essential for tissue regeneration and repair. Indeed, the rate and outcome of the healing process, including the degree of scarring and the restoration of organ function, are greatly influenced by the immune response to tissue damage. Therefore, since therapies based on stem cells and growth factors have not yet shown widespread clinical success, using biomaterials and drug delivery systems to modulate immune components is becoming an appealing approach in regenerative medicine. A deeper comprehension of the immune system's role in tissue repair and regeneration is required to develop effective reparatory and regenerative therapies. This understanding should be accompanied by numerical data or quantitative information that links the narrative flow with specific analyses and findings. We start by summarizing the functions of the different immune cell types in tissue repair. The basic concept, applications, and constraints of regulatory T (Treg) cell-based therapy, a subset of cellbased immunotherapy, are then covered. Finally, we address immunotherapy strategies based on biomaterials, which use different biomaterials to modulate immune cells to promote tissue repair and regeneration. Conventional breast cancer treatment includes surgery, chemotherapy, radiation therapy, and targeted medications, including PARP inhibitors and HER2 monoclonal antibodies. Cancer stem cells (CSCs) and triple-negative breast cancer (TNBC) are linked to treatment resistance and recurrence. To overcome the complexity of breast cancer and improve clinical outcomes, this study highlights the critical intersection of regenerative medicine, nanotechnology, and personalized therapies.</p>","PeriodicalId":18548,"journal":{"name":"Mini reviews in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":3.3,"publicationDate":"2026-04-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147618707","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"The Multifaceted Potential of Adhatoda vasica Nees: Traditional Uses, Pharmacological Activities and Biotechnological Applications.","authors":"Sekhar Tiwari, Priyanka Panchal, Harsh Mehta, Sabir Khan Pathan, Sujeet Kumar Mritunjay, Aryaman Singh, Cecileya Jasmin Meshak Dhanashekaran, Vinod Prabhu Venugopal","doi":"10.2174/0113895575430554260206060149","DOIUrl":"https://doi.org/10.2174/0113895575430554260206060149","url":null,"abstract":"<p><p>Adhatoda vasica Nees (A. vasica), known as the Malabar nut, belongs to the Acanthaceae family and is widely distributed across South and Southeast Asia. It is used in Ayurveda and Unani medicine as a therapy for human diseases, such as respiratory ailments like asthma, bronchitis, and tuberculosis. These plants are reported to be rich in alkaloids, flavonoids, tannins, and saponins, with vasicine and vasicinone as the primary bioactive compounds for their therapeutic activity. A. vasica has also been identified to contain several secondary metabolites, such as quercetin, kaempferol, and apigenin, that exhibit antioxidant, antimicrobial, anti-inflammatory, and immunomodulatory activities. The transcriptome analysis of A. vasica identified 171,064 transcripts corresponding to 55,528 genes, which are associated with key biosynthetic pathways. Therefore, these A. vasica were overharvested, precisely because of their widespread medicinal use and habitat destruction, and have been placed in the threatened species category in India. This review will emphasize the need for sustainable cultivation practices and biotechnological applications in order to preserve its availability for its therapeutic benefits. Moreover, clinical trials are necessary to validate its effectiveness and safety for its therapeutic applications. Integrating traditional knowledge with modern biotechnological advancements, the A. vasica plant could be a potential contributor to the pharmaceutical industry, developing new drugs with little or no adverse effects that can improve the quality of life of patients during treatment.</p>","PeriodicalId":18548,"journal":{"name":"Mini reviews in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":3.3,"publicationDate":"2026-04-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147776090","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Medicinal Chemistry of Fourth-generation Tyrosine Kinase Inhibitors.","authors":"Mohamed F Zayed","doi":"10.2174/0113895575451047260306044852","DOIUrl":"https://doi.org/10.2174/0113895575451047260306044852","url":null,"abstract":"<p><p>Introduction / Objectives: Resistance to chemotherapies represents a critical challenge in the treatment of Non-Small Cell Lung Cancer (NSCLC). This clinical imperative drove the discovery of Fourth-Generation Tyrosine Kinase Inhibitors (FGTKIs) to defeat such resistance mechanisms. The study comprehensively reviews and critically analyzes the medicinal chemistry of FGTKIs, focusing on their rational design, mechanisms of action, Structure-Activity Relationships (SARs), and therapeutic potential for overcoming resistance mutations in oncology.</p><p><strong>Methods: </strong>A systematic search of major medical databases was conducted to recognize and integrate related literature.</p><p><strong>Results: </strong>FGTKIs represent a class of structurally efficient anticancer agents that function through the allosteric inhibition of TKs via reversible interactions. This mechanism confers potent inhibitory activity along with improved pharmacokinetic and pharmacodynamic properties.</p><p><strong>Discussion: </strong>They target the mutant-EGFR to overcome the tertiary resistant mutations (Del19/T790M/C797S), which represent a major clinical challenge against other Tyrosine Kinase Inhibitors (TKIs). They have definite molecular designs and pharmacokinetic properties supporting their action.</p><p><strong>Conclusion: </strong>FGTKIs have altered the therapeutic concept for mutant NSCLC patients and offered unprecedented efficacy and durability compared to earlier-generation inhibitors.</p>","PeriodicalId":18548,"journal":{"name":"Mini reviews in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":3.3,"publicationDate":"2026-03-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147593157","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}