{"title":"Innovative Theranostics Strategies in the Fight Against Lung Cancer.","authors":"Aashi Jain, Sakshi Soni, Vandana Soni, Sushil Kumar Kashaw","doi":"10.2174/0113895575338753250228055700","DOIUrl":"https://doi.org/10.2174/0113895575338753250228055700","url":null,"abstract":"<p><p>This review delves into the potential of nanotechnology for improved lung cancer diagnosis and treatment. A critical focus is placed on various overexpressed biomarkers within lung tumors. These biomarkers serve as potential targets for nanoparticle-based drug delivery strategies. The review explores two main targeting approaches: passive and active (receptor-based) targeting. Active targeting mechanisms like EGFR, folic acid, and CD44 receptor targeting are specifically discussed. Additionally, the review examines stimuli-responsive systems for targeted drug delivery, including pH, temperature, ligand-attached, and multi-stimuli-responsive systems. Moreover, the role of nanotechnology in theranostics, which combines therapeutic and diagnostic capabilities, is explored and different types of nanocarriers, including lipid-based, polymer-based, metal-based, and magnetic nanoparticles, are examined for their potential applications. The review also highlights advancements in lung cancer diagnostic techniques beyond nanotechnology. This includes emerging tools like biomarkers, biosensors, and artificial intelligence, alongside improvements to established methods. Finally, the review provides a glimpse into ongoing clinical trials and concludes by emphasizing the transformative potential of nanotechnology in improving lung cancer patient outcomes.</p>","PeriodicalId":18548,"journal":{"name":"Mini reviews in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":3.3,"publicationDate":"2025-03-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143586292","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":"Bioactive Sulfonamides Derived from Amino Acids: Their Synthesis and Pharmacological Activities.","authors":"Melford Chuka Egbujor, Paolo Tucci, Luciano Saso","doi":"10.2174/0113895575353663241129064820","DOIUrl":"https://doi.org/10.2174/0113895575353663241129064820","url":null,"abstract":"<p><p>Currently, the synthesis of bioactive sulfonamides using amino acid as a starting reagent has become an area of research interest in organic chemistry. Over the years, an amine-sulfonyl chloride reaction has been adopted as a common step in traditional sulfonamide synthetic methods. However, recent developments have shown amino acids to be better precursors than amines in the synthesis of sulfonamides. Although amines and amino acids have some structural similarities, using amino acids rather than amines in the synthesis of sulfonamides minimizes several drawbacks. Comparatively, amino acids are preferred to amines as starting reagents in sulfonamide synthesis due to their biological relevance, chirality, stereochemistry, diversity of side chains, orthogonality in functional group manipulation, the potential for peptide and protein synthesis, mild reaction conditions, alignment with green chemistry principles, diverse synthetic applications, easy availability, and economic viability. Amino acids, having the aforementioned properties, offer a versatile platform for the synthesis of sulfonamides with tailored structures. The reaction mechanism of the synthesis of amino acid-derived sulfonamides involves a nucleophilic attack by the amino group on the activated sulfonyl species to produce a sulfonamide functional group. Amino acid-based sulfonamides have numerous pharmacological activities, including antibacterial, antiviral, anticancer, antioxidant, anti-inflammatory, anti-plasmodial, antimalarial, anti-trypanosomal, and insect growth regulatory properties. This review discusses several synthetic processes, emphasizing established ways, cutting- edge techniques, and novel approaches that emphasize the significance of amino acids in the synthesis of sulfonamides. The structure-activity relationship of amino acid-derived sulfonamides and their pharmacological activities are also highlighted.</p>","PeriodicalId":18548,"journal":{"name":"Mini reviews in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":3.3,"publicationDate":"2025-01-13","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142984180","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}
Nawab Ali, Liaqat Rasheed, Wajid Rehman, Muhammad Naseer, Momin Khan, Safia Hassan, Amina Zulfiqar
{"title":"A Review on Recent Trends in Photo-Drug Efficiency of Advanced Biomaterials in Photodynamic Therapy of Cancer.","authors":"Nawab Ali, Liaqat Rasheed, Wajid Rehman, Muhammad Naseer, Momin Khan, Safia Hassan, Amina Zulfiqar","doi":"10.2174/0113895575320468240912093945","DOIUrl":"10.2174/0113895575320468240912093945","url":null,"abstract":"<p><p>Photodynamic Therapy (PDT) has emerged as a highly efficient and non-invasive cancer treatment, which is crucial considering the significant global mortality rates associated with cancer. The effectiveness of PDT primarily relies on the quality of the photosensitizers employed. When exposed to appropriate light irradiation, these photosensitizers absorb energy and transition to an excited state, eventually transferring energy to nearby molecules and generating Reactive Oxygen Species (ROS), including singlet oxygen [<sup>1</sup>O<sub>2</sub>]. The ability to absorb light in visible and nearinfrared wavelengths makes porphyrins and derivatives useful photosensitizers for PDT. Chemically, Porphyrins, composed of tetra-pyrrole structures connected by four methylene groups, represent the typical photosensitizers. The limited water solubility and bio-stability of porphyrin photosensitizers and their non-specific tumor-targeting properties hinder PDT effectiveness and clinical applications. Therefore, a wide range of modification and functionalization techniques have been used to maximize PDT efficiency and develop multidimensional porphyrin-based functional materials. Recent progress in porphyrin-based functional materials has been investigated in this review paper, focusing on two main aspects including the development of porphyrinic amphiphiles that improve water solubility and biocompatibility, and the design of porphyrin-based polymers, including block copolymers with covalent bonds and supramolecular polymers with noncovalent bonds, which provide versatile platforms for PDT applications. The development of porphyrin-based functional materials will allow researchers to significantly expand PDT applications for cancer therapy by opening up new opportunities. With these innovations, porphyrins will overcome their limitations and push PDT to the forefront of cancer treatment options.</p>","PeriodicalId":18548,"journal":{"name":"Mini reviews in medicinal chemistry","volume":" ","pages":"259-276"},"PeriodicalIF":3.3,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142372308","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":"Sulfonated Penta-galloyl Glucose (SPGG): The Pharmacological Effects of Promiscuous Glycosaminoglycan Small Molecule Mimetic.","authors":"Rami A Al-Horani","doi":"10.2174/0113895575332248241030033106","DOIUrl":"10.2174/0113895575332248241030033106","url":null,"abstract":"<p><p>Sulfated glycosaminoglycans (SGAGs), such as heparin, are complex linear polysaccharides attached to core proteins via covalent bonds to form proteoglycans. SGAGs are crucial in assembling extracellular matrix, the regulation of cell signaling and cell behavior, hemostasis, development, and various diseases, including thrombosis, cancer, infectious diseases, and neurodegenerative disorders, through their binding with diverse proteins. Despite the abundant SGAG-protein interactions provided by nature, the development of small SGAG-like molecules remains underexplored. However, sulfonated penta-galloyl glucose (SPGG) represents a promising, easily synthesized, small-molecule mimetic of SGAGs, capable of harnessing these interactions. This minireview discusses the chemical synthesis and characterization of SPGG, along with its pharmacological effects derived from modulating the SGAG-protein interface.</p>","PeriodicalId":18548,"journal":{"name":"Mini reviews in medicinal chemistry","volume":" ","pages":"365-373"},"PeriodicalIF":3.3,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12014344/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142622525","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Vaibhav Singh, Ekta Shirbhate, Rakesh Kore, Subham Vishwakarma, Shadiya Parveen, Ravichandran Veerasamy, Amit K Tiwari, Harish Rajak
{"title":"Microbial Metabolites-induced Epigenetic Modifications for Inhibition of Colorectal Cancer: Current Status and Future Perspectives.","authors":"Vaibhav Singh, Ekta Shirbhate, Rakesh Kore, Subham Vishwakarma, Shadiya Parveen, Ravichandran Veerasamy, Amit K Tiwari, Harish Rajak","doi":"10.2174/0113895575320344240625080555","DOIUrl":"10.2174/0113895575320344240625080555","url":null,"abstract":"<p><p>Globally, one of the most prevalent cancers is colorectal cancer (CRC). Chemotherapy and surgery are two common conventional CRC therapies that are frequently ineffective and have serious adverse effects. Thus, there is a need for complementary and different therapeutic approaches. The use of microbial metabolites to trigger epigenetic alterations as a way of preventing CRC is one newly emerging field of inquiry. Small chemicals called microbial metabolites, which are made by microbes and capable of altering host cell behaviour, are created. Recent research has demonstrated that these metabolites can lead to epigenetic modifications such as histone modifications, DNA methylation, and non-coding RNA regulation, which can control gene expression and affect cellular behaviour. This review highlights the current knowledge on the epigenetic modification for cancer treatment, immunomodulatory and anti-carcinogenic attributes of microbial metabolites, gut epigenetic targeting system, and the role of dietary fibre and gut microbiota in cancer treatment. It also focuses on short-chain fatty acids, especially butyrates (which are generated by microbes), and their cancer treatment perspective, challenges, and limitations, as well as state-of-the-art research on microbial metabolites-induced epigenetic changes for CRC inhibition. In conclusion, the present work highlights the potential of microbial metabolites-induced epigenetic modifications as a novel therapeutic strategy for CRC suppression and guides future research directions in this dynamic field.</p>","PeriodicalId":18548,"journal":{"name":"Mini reviews in medicinal chemistry","volume":" ","pages":"76-93"},"PeriodicalIF":3.3,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141563753","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 Application of the Pyrazole Structure in the Structural Modification of Natural Products.","authors":"Fu-Qun Sun, Ya-Lan Wang, Ke Sun, Fei-Xia Yue, Yun-Xia Sun, Jia-Hong Ju, Zhan-Hui Jin, Qing-Kun Shen, Hong-Yan Guo, Mei-Hui Liu, Zhe-Shan Quan","doi":"10.2174/0113895575359419241211092252","DOIUrl":"10.2174/0113895575359419241211092252","url":null,"abstract":"<p><p>Most natural products in nature have broad but not exceedingly good biological activities. The pyrazole structure has been introduced into natural products due to its suitability for various synthetic methods and its broad pharmacological activities. This article provides a detailed introduction to the anti-inflammatory, antibacterial, antifungal, antiviral, and anti-Alzheimer disease activities of pyrazole-modified natural product derivatives, particularly their anti-tumor activity. It is worth noting that compared to lead compounds, most natural product derivatives modified with pyrazole exhibit excellent pharmacological activity. Some of these derivatives exhibit outstanding anti- tumor activity, with IC<sub>50</sub> values reaching nanomolar levels. This review provides more research directions and choices for future studies on natural products.</p>","PeriodicalId":18548,"journal":{"name":"Mini reviews in medicinal chemistry","volume":" ","pages":"628-652"},"PeriodicalIF":3.3,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143033554","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":"Comprehensive Insight into Green Synthesis Approaches, Structural Activity Relationship, and Therapeutic Potential of Pyrazolic Chalcone Derivative.","authors":"Samyak Bajaj, Akanksha Gupta, Priyanshu Nema, Rashmi Rawal, Varsha Kashaw, Sushil Kumar Kashaw","doi":"10.2174/0113895575327555241024111038","DOIUrl":"10.2174/0113895575327555241024111038","url":null,"abstract":"<p><p>Pyrazolic chalcone exhibits diverse therapeutic activities, including anti-inflammatory, antioxidant, antimicrobial, antitumor, and anti-diabetic properties. Structural activity relationship (SAR) studies play a crucial role in understanding the molecular aspects governing their biological effects, guiding the rational design of derivatives with enhanced efficacy and reduced side effects. This review provides an overview of pyrazolic chalcone derivatives, emphasizing their synthesis through both conventional and green methods. In comparison, conventional synthesis methods have been widely employed in the past for the production of pyrazolic chalcones, often relying on traditional chemical processes that may involve the use of hazardous reagents and generate significant waste. On the other hand, green synthesis methods, in harmony with the growing emphasis on sustainable practices in drug discovery, offer a more environmentally friendly alternative. Green synthesis typically involves the use of eco-friendly reagents, solvents, and energy-efficient processes, resulting in reduced environmental impact and improved resource efficiency. Overall, pyrazolic chalcone derivatives represent a promising class of compounds with significant potential for therapeutic applications.</p>","PeriodicalId":18548,"journal":{"name":"Mini reviews in medicinal chemistry","volume":" ","pages":"539-577"},"PeriodicalIF":3.3,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142603328","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}
Andre Sanglard, Barbara Castello Branco Miranda, Ana Luiza França Vieira, Marcus Vinicius Miranda Macedo, Rodrigo Lara Santos, Alexia Stenner Rodrigues Radicchi Campos, Amanda Campos Piva, Ana Cristina Simoes E Silva
{"title":"The Role of Renin-Angiotensin System in Diabetic Nephropathy: An Update.","authors":"Andre Sanglard, Barbara Castello Branco Miranda, Ana Luiza França Vieira, Marcus Vinicius Miranda Macedo, Rodrigo Lara Santos, Alexia Stenner Rodrigues Radicchi Campos, Amanda Campos Piva, Ana Cristina Simoes E Silva","doi":"10.2174/0113895575344980250130062547","DOIUrl":"10.2174/0113895575344980250130062547","url":null,"abstract":"<p><strong>Background and aims: </strong>Diabetic nephropathy (DN) is an important complication of diabetes, leading to end-stage renal disease (ESRD) worldwide. This review aimed to explore the role of the renin-angiotensin system (RAS) in DN, highlighting current treatments and emerging therapeutic perspectives.</p><p><strong>Methods: </strong>We conducted a narrative review of the literature up to March 2024, focusing on the classical and alternative RAS axes, their implications in DN, and novel therapeutic approaches. Data were sourced from Scopus, PubMed, Scielo, and Cochrane databases.</p><p><strong>Results: </strong>The classical RAS axis, involving angiotensin-converting enzyme (ACE), Angiotensin II (Ang II), and the AT1 receptor, promotes vasoconstriction, sodium retention, and fibrosis in DN. Hyperglycemia-induced Ang II increases oxidative stress, contributing to glomerular hyperfiltration and kidney damage. Current treatments include ACE inhibitors and angiotensin receptor blockers (ARBs), which reduce blood pressure and proteinuria, delaying DN progression. In contrast, the alternative RAS axis, featuring ACE2, Ang-(1-7), and the Mas receptor, offers renoprotective effects by counteracting Ang II actions. Ang-(1-7) reduces inflammation, fibrosis, and podocyte apoptosis. ACE2 activators, Ang-(1-7), and Mas receptor agonists show promise in preclinical studies, reducing glomerular fibrosis and improving renal function. Ang-(1-9) and alamandine may also hold potential in future treatments. Emerging therapies, such as the SGLT2 inhibitors, also demonstrate benefits in reducing DN progression.</p><p><strong>Conclusion: </strong>While ACE inhibitors, ARBs, and SGLT2 inhibitors remain central to DN management, the ACE2-Ang-(1-7)-Mas axis presents a promising therapeutic target. Future research should focus on translating preclinical findings into clinical applications, potentially improving DN treatment.</p>","PeriodicalId":18548,"journal":{"name":"Mini reviews in medicinal chemistry","volume":" ","pages":"591-600"},"PeriodicalIF":3.3,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143399473","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":"Trace Elements in Medicinal Metallomics.","authors":"Marina Orlova, Stepan Kalmykov, Tatiana Trofimova, Dmitry Kuznetsov","doi":"10.2174/0113895575333766240912162252","DOIUrl":"10.2174/0113895575333766240912162252","url":null,"abstract":"<p><p>This analytical mini-review focuses on the effects of trace elements, which includes Cu, Mn, Zn, and Se, as well as some rarer microelements, on the regulation of oxidative stress in the body and of certain diseases associated with it. Synergism and competition between certain microelements have been considered a hot topic in the applied molecular pharmacology of these specific bio-effects. Some ideas for further possible directions of research are expressed. Noteworthy, metal coordinating catalytical sites of certain enzymes function as pharmacophore-forming and connecting nanostructures. These sites can be regarded as targets for various effectors, making them pharmacologically significant contributors to biocatalysis.</p>","PeriodicalId":18548,"journal":{"name":"Mini reviews in medicinal chemistry","volume":" ","pages":"664-674"},"PeriodicalIF":3.3,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142349792","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}
Yuan Liu, Zhixian Zhang, Zeyu Zhu, Yang Yang, Weijia Peng, Qiuhe Chen, Shinghung Mak, Karl Wahkeung Tism, Rongbiao Pi
{"title":"Cinnamic Acid Derivatives: Recent Discoveries and Development Strategies for Alzheimer's Disease.","authors":"Yuan Liu, Zhixian Zhang, Zeyu Zhu, Yang Yang, Weijia Peng, Qiuhe Chen, Shinghung Mak, Karl Wahkeung Tism, Rongbiao Pi","doi":"10.2174/0113895575330648240819112435","DOIUrl":"10.2174/0113895575330648240819112435","url":null,"abstract":"<p><p>Alzheimer's Disease (AD) is a progressive neurodegenerative disorder that leads to cognitive decline and memory impairment. It is characterized by the accumulation of Amyloid-beta (Aβ) plaques, the abnormal phosphorylation of tau protein forming neurofibrillary tangles, and is often accompanied by neuroinflammation and oxidative stress, which contribute to neuronal loss and brain atrophy. At present, clinical anti-AD drugs are mostly single-target, improving the cognitive ability of AD patients, but failing to effectively slow down the progression of AD. Therefore, research on effective multi-target drugs for AD has become an urgent problem to address. The main derivatives of hydroxycinnamic acid, caffeic acid, and ferulic acid, are widely present in nature and have many pharmacological activities, such as antimicrobial, antioxidant, anti-inflammatory, neuroprotective, anti-Aβ deposition, and so on. The occurrence and development of AD are often accompanied by pathologies, such as oxidative stress, neuroinflammation, and Aβ deposition, suggesting that caffeic acid and ferulic acid can be used in the research on anti-AD drugs. Therefore, in this article, we have summarized the multi-target anti-AD derivatives based on caffeic acid and ferulic acid in recent years, and discussed the new design direction of cinnamic acid derivatives as backbone compounds. It is hoped that this review will provide some useful strategies for anti-AD drugs based on cinnamic acid derivatives.</p>","PeriodicalId":18548,"journal":{"name":"Mini reviews in medicinal chemistry","volume":" ","pages":"163-175"},"PeriodicalIF":3.3,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142109289","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}