Mini reviews in medicinal chemistry最新文献

筛选
英文 中文
Retrospection of Argemone mexicana and its Derived Analogs as a Futuristic Approach Exhibiting Anticancer Potential. 墨西哥银皂酮及其衍生类似物作为一种具有抗癌潜力的未来方法的回顾。
IF 3.3 3区 医学
Mini reviews in medicinal chemistry Pub Date : 2026-03-16 DOI: 10.2174/0113895575417548251208235008
Sunanda Kulshrestha, Istuti Saraswat, Anjana Goel
{"title":"Retrospection of Argemone mexicana and its Derived Analogs as a Futuristic Approach Exhibiting Anticancer Potential.","authors":"Sunanda Kulshrestha, Istuti Saraswat, Anjana Goel","doi":"10.2174/0113895575417548251208235008","DOIUrl":"https://doi.org/10.2174/0113895575417548251208235008","url":null,"abstract":"<p><p>Argemone mexicana (Linn.), commonly known as prickly poppy, is a well-documented medicinal plant in Indian Ayurvedic literature, recognized for its diverse pharmacological properties. It has been investigated for its potential applications in the treatment of cancer, inflammation, and wound healing, thereby highlighting its pharmacological significance. Traditionally, it has been used successfully to treat skin diseases, ulcers, tumors, boils, and snake venom poisoning. The therapeutic potential of this plant has been further validated by recent studies, which also demonstrated its safety in clinical trials for antimalarial activity. Berberine, argemonine, argenaxine, and chelerythrine are among the bioactive alkaloids abundant in Argemone mexicana, shown to possess significant anticancer, antibacterial, anti-inflammatory, and antimalarial properties. These compounds exert cytotoxic effects against various cancer cell lines by modulating key oncogenic pathways and preventing the acquisition of cancer hallmark characteristics, such as uncontrolled proliferation, apoptosis evasion, inflammation, invasion, angiogenesis, and drug resistance. Preclinical studies have further explored the role of Argemone mexicana in cancer treatment and wound healing, expanding its pharmacological relevance. This review systematically compiles evidence from in vitro and in vivo studies, elucidating the mechanisms through which Argemone mexicana and its derived compounds exhibit anticancer activity. By highlighting its potential as a natural source of anticancer agents, this review aims to provide a foundation for future research and the development of novel plant-based cancer therapeutics.</p>","PeriodicalId":18548,"journal":{"name":"Mini reviews in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":3.3,"publicationDate":"2026-03-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147494181","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}
引用次数: 0
Association of Metabolic Syndrome and Cholelithiasis: Understanding the Underlying Mechanism for Better Treatment. 代谢综合征与胆石症的关联:了解更好治疗的潜在机制。
IF 3.3 3区 医学
Mini reviews in medicinal chemistry Pub Date : 2026-03-13 DOI: 10.2174/0113895575423784251206060716
Anas Emmad Al Wahaibi, Abdullah Al Lawati, Maiyan Al Hinai, Abdulrahman Al Hadhrami, Ibrahim Al-Ruheili, Maram Salim AlMusallami, Hanan Al Lawati, Srijit Das
{"title":"Association of Metabolic Syndrome and Cholelithiasis: Understanding the Underlying Mechanism for Better Treatment.","authors":"Anas Emmad Al Wahaibi, Abdullah Al Lawati, Maiyan Al Hinai, Abdulrahman Al Hadhrami, Ibrahim Al-Ruheili, Maram Salim AlMusallami, Hanan Al Lawati, Srijit Das","doi":"10.2174/0113895575423784251206060716","DOIUrl":"https://doi.org/10.2174/0113895575423784251206060716","url":null,"abstract":"<p><p>Metabolic syndrome is characterized by a combination of conditions, including abdominal obesity, elevated blood pressure, increased blood sugar levels, and high triglycerides. The incidence of metabolic syndrome is concerningly increasing worldwide. Metabolic syndrome increases the risk of cardiovascular diseases, type 2 diabetes mellitus, non-alcoholic fatty liver disease, chronic kidney disease, and even cancer. Cholelithiasis refers to the formation of gallstones. Metabolic associations, including dyslipidemia, obesity, diabetes, and insulin resistance, are all risk factors for cholelithiasis. Modifiable factors include changes in lifestyle and metabolic conditions. In this narrative review, we searched the PubMed, Scopus, and Google Scholar databases to identify evidence-based literature on the association between metabolic syndrome and cholelithiasis. We discuss the biochemical reaction underlying cholelithiasis, the receptors and signaling pathways involved, and therapeutic options targeting hepatic cholesterol synthesis and secretion. We discuss the molecular mechanisms underlying the association between metabolic syndrome and cholelithiasis, including insulin resistance, genetic factors, and gallbladder functions relevant to cholelithiasis. The clinical implications, along with surgical interventions and treatment, are also discussed in detail. The review may benefit physicians involved in the treatment of cholelithiasis and metabolic syndrome, and help researchers develop appropriate drugs in the future.</p>","PeriodicalId":18548,"journal":{"name":"Mini reviews in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":3.3,"publicationDate":"2026-03-13","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147463682","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}
引用次数: 0
Antisense Molecules: Design, Chemistry, and Therapeutic Innovations. 反义分子:设计、化学和治疗创新。
IF 3.3 3区 医学
Mini reviews in medicinal chemistry Pub Date : 2026-03-13 DOI: 10.2174/0113895575428832251206055438
Prema Vediappan, Swetha Aravamudhan, Jocelyn Olivia Prabhakar David, Abitha Sri Ganapathy, Suryalakshmi Guhanathan
{"title":"Antisense Molecules: Design, Chemistry, and Therapeutic Innovations.","authors":"Prema Vediappan, Swetha Aravamudhan, Jocelyn Olivia Prabhakar David, Abitha Sri Ganapathy, Suryalakshmi Guhanathan","doi":"10.2174/0113895575428832251206055438","DOIUrl":"https://doi.org/10.2174/0113895575428832251206055438","url":null,"abstract":"<p><strong>Introduction: </strong>Antisense molecules are short synthetic nucleic acid strands designed to bind to complementary sequences of messenger RNA (mRNA) to regulate gene expression. This study focuses on understanding the chemistry, modifications, and therapeutic applications of antisense molecules.</p><p><strong>Method: </strong>A comprehensive literature review was conducted using scientific databases, including PubMed, Scopus, and Google Scholar. Relevant published articles were selected using keywords such as \"antisense oligonucleotides,\" \"gene silencing,\" \"therapeutic applications,\" \"neurological disorders,\" and \"cancer.\" Studies included in this review consisted of research focusing on the mechanisms, delivery methods, and therapeutic outcomes of antisense oligonucleotides.</p><p><strong>Result: </strong>The data obtained in this study indicate that third-generation ASOs exhibit greater therapeutic efficacy than first- and second-generation ASOs.</p><p><strong>Discussion: </strong>This review compiles and discusses the mechanisms of action, structural features, chemical modifications, recent advances, applications, challenges, and future directions of ASOs in genetic disorders and other diseases.</p><p><strong>Conclusion: </strong>Antisense oligonucleotides (ASOs) have been successfully approved by the FDA for the development of drugs such as Nusinersen (used for the treatment of spinal muscular atrophy) and Fomivirsen (used for treating Cytomegalovirus retinitis). ASOs offer a unique ability to target specific RNA sequences and help overcome limitations associated with traditional therapies.</p>","PeriodicalId":18548,"journal":{"name":"Mini reviews in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":3.3,"publicationDate":"2026-03-13","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147463646","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}
引用次数: 0
Computational Innovations in Cancer Research and How Computing is Transforming Drug Discovery and Development: A Review. 癌症研究中的计算创新以及计算如何改变药物发现和开发:综述。
IF 3.3 3区 医学
Mini reviews in medicinal chemistry Pub Date : 2026-03-13 DOI: 10.2174/0113895575418750251204104229
Ilavanalangki Lytan, Basanta Singha, Nichan Boruah, Partha Pratim Gogoi, Penlisola Longkumer, Mhasilhoutuo Pucho, Beware Dkhar, Upasana Bora Sinha
{"title":"Computational Innovations in Cancer Research and How Computing is Transforming Drug Discovery and Development: A Review.","authors":"Ilavanalangki Lytan, Basanta Singha, Nichan Boruah, Partha Pratim Gogoi, Penlisola Longkumer, Mhasilhoutuo Pucho, Beware Dkhar, Upasana Bora Sinha","doi":"10.2174/0113895575418750251204104229","DOIUrl":"https://doi.org/10.2174/0113895575418750251204104229","url":null,"abstract":"<p><strong>Introduction: </strong>Cancer is a major global health concern, causing millions of deaths each year due to the uncontrolled growth and spread of abnormal cells. Despite advances in diagnosis and treatment, its complexity and therapy resistance keep it a leading cause of mortality. This review highlights the impact of CADD and related computational approaches in advancing cancer research and therapy.</p><p><strong>Methods: </strong>This literature review examined studies on CADD in cancer research, focusing on its use in drug discovery, target identification, and compound optimization. It describes how CADD accelerates drug development, reduces costs, and supports the design of more selective anticancer agents.</p><p><strong>Discussion: </strong>Traditional experimental methods are time-consuming, costly, and limited in predictive power. Computational innovations such as CADD, AI, ML, and quantum computing enable rational drug design, predictive modeling, and efficient target prioritization. Early-stage challenges illustrated by PROTACs, EGFR inhibitors, miRNA therapeutics, and T-cell-engaging bispecific antibodies include issues related to selectivity, toxicity, drug resistance, and limitations of preclinical models. Although tumor biomarkers aid detection and monitoring, sensitivity and reproducibility remain concerns. AI, ML, and quantum computing enhance screening, toxicity prediction, and the simulation of protein-ligand interactions. Despite regulatory and clinical hurdles, integrating genomics, proteomics, imaging, and computational approaches offers a path toward more effective, personalized cancer therapies.</p><p><strong>Results: </strong>In this review study, it was found that computer-aided drug design and related computational approaches have significantly enhanced cancer drug discovery. Several methods including molecular docking, molecular dynamics, QSAR, virtual screening and AI/ML driven models have accelerated target identification, lead optimization and prediction of efficacy, toxicity and resistance. In multiple instances, integration of multi-omics data has improved biomarker discovery and patient stratification. Several case studies on EGFR, PARP, KRAS G12C and immunotherapy targets have demonstrated reduced development time and improved selectivity. Overall, computational innovations have streamlined anticancer drug development while providing substantial leads for experimental validation.</p><p><strong>Conclusion: </strong>CADD is transforming cancer research by accelerating drug discovery, optimizing target interactions, and aiding the design of selective agents. Its limitations include reliance on structural data, high computational demands, and the need for experimental validation. Future efforts should integrate AI, machine learning, and multi-omics data to improve predictive accuracy and accelerate therapy development.</p>","PeriodicalId":18548,"journal":{"name":"Mini reviews in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":3.3,"publicationDate":"2026-03-13","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147463705","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}
引用次数: 0
The Nasal Route Redefined: The Impact of Chitosan Nanoparticles on Drug Delivery. 重新定义鼻途径:壳聚糖纳米颗粒对药物给药的影响。
IF 3.3 3区 医学
Mini reviews in medicinal chemistry Pub Date : 2026-03-06 DOI: 10.2174/0113895575417283251127105439
Lalit Kumar, Vikas Aggarwal, Ritesh Rana, Sumit Durgapal, Harishchandra Verma, Shiv Kumar Kushawaha, Mohit Vij, Mridhula Manimaran
{"title":"The Nasal Route Redefined: The Impact of Chitosan Nanoparticles on Drug Delivery.","authors":"Lalit Kumar, Vikas Aggarwal, Ritesh Rana, Sumit Durgapal, Harishchandra Verma, Shiv Kumar Kushawaha, Mohit Vij, Mridhula Manimaran","doi":"10.2174/0113895575417283251127105439","DOIUrl":"https://doi.org/10.2174/0113895575417283251127105439","url":null,"abstract":"<p><strong>Introduction: </strong>The nasal route presents a viable alternative for medication administration, circumventing first-pass metabolism and improving bioavailability, especially for neurological conditions. Nonetheless, obstacles such as mucociliary clearance and enzymatic degradation constrain its effectiveness. Chitosan nanoparticles (CS-NPs) have emerged as a viable option due to their mucoadhesive properties, biocompatibility, and capacity to modulate tight junctions, thereby enabling direct nose-to-brain administration.</p><p><strong>Methods: </strong>This review explores various methods for the production of chitosan nanoparticles (CSNPs), their characterization techniques, drug delivery applications via the nasal route, and an examination of related patents. Search engines such as PubMed, Google Scholar, and ScienceDirect were utilized for the literature search. Studies published between 2015 and 2025 were included.</p><p><strong>Results: </strong>The use of CS-NPs in the delivery of various treatments, including anticancer, antiparkinsonian, antianxiety, and antischizophrenic medications, shows great promise. Research has demonstrated that certain formulations, such as chitosan-PEG nanovesicles and transferrin-conjugated nanoparticles, exhibit improved bioavailability, sustained release, and enhanced brain targeting. Patents have further supported the development of mucoadhesive and combinatorial therapies.</p><p><strong>Discussion: </strong>While there are notable benefits, obstacles such as rapid mucociliary clearance, limited drug-loading capacity, and variability in nasal responses persist. Proposed solutions to address these challenges include innovations like mucoadhesive coatings, hybrid polymers, and stimuli-responsive systems. Utilizing computational modeling and conducting clinical trials are crucial for improving formulations.</p><p><strong>Conclusion: </strong>CS-NPs represent a transformative approach to nasal medication delivery. To fully realize their potential, future research should focus on advanced formulations and personalized delivery systems, thereby facilitating clinical translation and improving therapeutic outcomes.</p>","PeriodicalId":18548,"journal":{"name":"Mini reviews in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":3.3,"publicationDate":"2026-03-06","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147458398","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}
引用次数: 0
The Rise of Palladium Nanoparticles: From Fabrication to Biomedical Breakthroughs. 钯纳米颗粒的兴起:从制造到生物医学的突破。
IF 3.3 3区 医学
Mini reviews in medicinal chemistry Pub Date : 2026-02-26 DOI: 10.2174/0113895575422986251128022844
Lalit Kumar, Ritesh Rana, Rakesh Kumar Sharma, Rakesh Kumar, Anjana Devi, Neelam Sharma, Mridhula Manimaran
{"title":"The Rise of Palladium Nanoparticles: From Fabrication to Biomedical Breakthroughs.","authors":"Lalit Kumar, Ritesh Rana, Rakesh Kumar Sharma, Rakesh Kumar, Anjana Devi, Neelam Sharma, Mridhula Manimaran","doi":"10.2174/0113895575422986251128022844","DOIUrl":"https://doi.org/10.2174/0113895575422986251128022844","url":null,"abstract":"<p><strong>Introduction: </strong>Palladium nanoparticles (PdNPs) are at the vanguard of nanotechnologydriven biomedical and industrial applications due to their exceptional electronic, catalytic, and optical properties.</p><p><strong>Methods: </strong>The synthesis methodologies for PdNPs, which include physical, chemical, and biological approaches, are systematically examined in this review. A comprehensive literature survey is conducted to critically analyze key advancements, challenges, and application domains. Search engines explored were PubMed, Google Scholar, and Science Direct. Studies ranging from 2015 to 2025 were incorporated.</p><p><strong>Results: </strong>Nanoparticle size and morphology can be precisely controlled through physical and chemical synthesis methods; however, these methods frequently pose environmental and scalability concerns. An eco-friendly alternative with enhanced biocompatibility is provided by biogenic synthesis, which employs microbial and plant extracts. PdNPs exhibit substantial potential in the fields of fuel cells, sensors, catalysis, and emerging biomedical applications, including cancer therapy, drug delivery, and imaging.</p><p><strong>Discussion: </strong>While there are notable benefits, obstacles like swift mucociliary clearance, restricted drug-loading capacity, and variability in nasal responses continue to exist. Proposed solutions to address these challenges include innovations such as mucoadhesive coatings, hybrid polymers, and stimuli-responsive systems. Utilizing computational modeling and conducting clinical trials are crucial for enhancing formulations.</p><p><strong>Conclusion: </strong>In a variety of domains, PdNPs have the potential to create revolutionary changes. To successfully integrate them into real-world applications, further study into toxicity, functionalization, and scalable production is crucial.</p>","PeriodicalId":18548,"journal":{"name":"Mini reviews in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":3.3,"publicationDate":"2026-02-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147321939","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}
引用次数: 0
New Therapeutic Options Against Clinically Relevant Proteases in Cancer Progression. 针对癌症进展中临床相关蛋白酶的新治疗选择。
IF 3.3 3区 医学
Mini reviews in medicinal chemistry Pub Date : 2026-02-24 DOI: 10.2174/0113895575426438251104072459
Anastasiya O Syrocheva, Darya S Volkova, Evgenya R Denisova, Valeria V Streltsova, Polina S Marukhina, Alessandro Parodi, Andrey A Zamyatnin
{"title":"New Therapeutic Options Against Clinically Relevant Proteases in Cancer Progression.","authors":"Anastasiya O Syrocheva, Darya S Volkova, Evgenya R Denisova, Valeria V Streltsova, Polina S Marukhina, Alessandro Parodi, Andrey A Zamyatnin","doi":"10.2174/0113895575426438251104072459","DOIUrl":"https://doi.org/10.2174/0113895575426438251104072459","url":null,"abstract":"<p><p>Proteases are key regulators in cancer progression and metastasis, representing promising therapeutic targets. This review underscores the critical role of diverse proteases-encompassing cell surface ectoproteases, extracellular proteases, and intracellular proteases-in tumor biology, with a focus on the most significant and clinically relevant ones. Their overexpression in tumors reflects their importance in cancer development, invasion, and drug resistance. Emerging research has unveiled novel strategies to target proteases for cancer therapy, offering hope for improved treatment outcomes. However, challenges, such as selectivity, drug delivery, and toxicity remain significant hurdles to overcome. This article discusses current advancements, challenges, and future opportunities in targeting proteases for cancer therapy.</p>","PeriodicalId":18548,"journal":{"name":"Mini reviews in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":3.3,"publicationDate":"2026-02-24","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147365560","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}
引用次数: 0
Preface. 前言。
IF 3.3 3区 医学
Mini reviews in medicinal chemistry Pub Date : 2026-02-24 DOI: 10.2174/0113895575478472260220061323
Davide Barreca
{"title":"Preface.","authors":"Davide Barreca","doi":"10.2174/0113895575478472260220061323","DOIUrl":"https://doi.org/10.2174/0113895575478472260220061323","url":null,"abstract":"","PeriodicalId":18548,"journal":{"name":"Mini reviews in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":3.3,"publicationDate":"2026-02-24","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147321937","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}
引用次数: 0
Inavolisib-based Combination Therapy for the Treatment of PIK3CAMutated HR+/HER2- Breast Cancer: An Overview. 以不可避免为基础的联合疗法治疗pik3突变的HR+/HER2-乳腺癌:综述
IF 3.3 3区 医学
Mini reviews in medicinal chemistry Pub Date : 2026-02-24 DOI: 10.2174/0113895575418114251210151424
Sushmita Bhatia, Neha Bhatia, Suresh Thareja
{"title":"Inavolisib-based Combination Therapy for the Treatment of PIK3CAMutated HR+/HER2- Breast Cancer: An Overview.","authors":"Sushmita Bhatia, Neha Bhatia, Suresh Thareja","doi":"10.2174/0113895575418114251210151424","DOIUrl":"https://doi.org/10.2174/0113895575418114251210151424","url":null,"abstract":"<p><p>Inavolisib is a selective phosphoinositide 3-kinase alpha (PI3Kα) inhibitor representing the next generation of anticancer drugs for the treatment of PIK3CA-mutated HR+/HER2- breast cancer. The dysregulated PI3K/AKT/mTOR signalling axis is an established mechanism of breast cancer progression and resistance to therapy, emphasizing the need for selective inhibitors that have both improved tolerance and efficacy. Inavolisib exhibits enhanced potency and selectivity for PI3Kα, resulting in superior antitumor activity and lower off-target effects than older generations of PI3K inhibitors. The present review provides a comprehensive discussion on inavolisib, covering its structure, pharmacokinetic properties, mechanism of action, and in vivo preclinical efficacy. The antitumor effects of combination strategies are also being highlighted for their potential to overcome endocrine resistance and optimize patient outcomes. Furthermore, it discusses the emerging resistance mechanisms to PI3K inhibition, mitigation of adverse effects, and future directions for inavolisib in personalized oncology. As studies continue to demonstrate its clinical utility, inavolisib exhibits preferential activity against the mutated PI3Kα isoform, thereby enhancing therapeutic specificity for combination therapy.</p>","PeriodicalId":18548,"journal":{"name":"Mini reviews in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":3.3,"publicationDate":"2026-02-24","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147321909","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}
引用次数: 0
Chalcones as Multi-target Ligands for Alzheimer's Disease: A Review of Synthetic Strategies and Therapeutic Promise. 查尔酮作为阿尔茨海默病的多靶点配体:合成策略和治疗前景综述。
IF 3.3 3区 医学
Mini reviews in medicinal chemistry Pub Date : 2026-02-20 DOI: 10.2174/0113895575436583251223100249
Giorgio Antoniolli
{"title":"Chalcones as Multi-target Ligands for Alzheimer's Disease: A Review of Synthetic Strategies and Therapeutic Promise.","authors":"Giorgio Antoniolli","doi":"10.2174/0113895575436583251223100249","DOIUrl":"https://doi.org/10.2174/0113895575436583251223100249","url":null,"abstract":"<p><strong>Introduction: </strong>Alzheimer's disease remains a multifactorial neurodegenerative disorder with limited therapeutic options. Chalcones, flavonoid-derived molecules with high structural flexibility and diverse biological activities, have emerged as promising candidates due to their ability to inhibit Aβ aggregation and cholinesterase activity. Recent research highlights their relevance as multi-target agents suitable for early-stage drug discovery.</p><p><strong>Methods: </strong>This review compiled and analyzed studies published between 2022 and 2025 on chalcones and their derivatives with anti-Alzheimer's potential. Data were extracted regarding biosynthetic origins, synthetic strategies, physicochemical properties, and biological activities, including inhibitory potencies against AChE, MAO-B, and Aβ aggregation.</p><p><strong>Results: </strong>Numerous chalcone-based compounds exhibited significant activity against key Alzheimer's disease targets, such as Aβ1-42 aggregation (up to 78.2% inhibition) and enzymatic inhibition (e.g., AChE IC50 = 11.6 nM; MAO-B IC50 = 92 nM). Their structural versatility enabled the identification of potent derivatives with multi-target effects, addressing oxidative stress, amyloid pathology, and cholinergic dysfunction.</p><p><strong>Discussion: </strong>Chalcones represent a privileged scaffold suitable for medicinal chemistry optimization, offering ease of synthesis and adaptable chemical space for structure-activity relationship exploration. Their multi-target nature aligns with the complexity of Alzheimer's disease. However, challenges remain, including selectivity, pharmacokinetics, and translation from preclinical models to therapeutic relevance.</p><p><strong>Conclusion: </strong>Chalcones and their derivatives show strong preclinical promise as multi-target agents for Alzheimer's disease. Continued structural optimization and biological evaluation may advance these compounds toward disease-modifying therapies, supporting their potential role in future drug discovery efforts.</p>","PeriodicalId":18548,"journal":{"name":"Mini reviews in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":3.3,"publicationDate":"2026-02-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147307612","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}
引用次数: 0
0
×
引用
GB/T 7714-2015
复制
MLA
复制
APA
复制
导出至
BibTeX EndNote RefMan NoteFirst NoteExpress
×
提示
您的信息不完整,为了账户安全,请先补充。
现在去补充
×
提示
您因"违规操作"
具体请查看互助需知
我知道了
×
提示
确定
请完成安全验证×
相关产品
×
本文献相关产品
联系我们:info@booksci.cn Book学术提供免费学术资源搜索服务,方便国内外学者检索中英文文献。致力于提供最便捷和优质的服务体验。 Copyright © 2023 布克学术 All rights reserved.
京ICP备2023020795号-1
ghs 京公网安备 11010802042870号
Book学术文献互助
Book学术文献互助群
群 号:604180095
Book学术官方微信
小红书