Rony Abdi Syahputra , Asriadi , Arnika Gloria Br Sitorus , Sintia Karina Putri , Ana Gabriela Silva Olivera , Livia Ramos Santiago , Princella Halim , Amer Ahmed , Aasia Bibi , Aminah Dalimunthe , Poppy Anjelisa Zaitun Hasibuan , Moon Nyeo Park , Rosy Iara Maciel de Azambuja Ribeiro , Bonglee Kim , Pornphimon Meesakul , Shugeng Cao
{"title":"Peptide-mediated modulation of miRNAs: A novel therapeutic strategy for cancer","authors":"Rony Abdi Syahputra , Asriadi , Arnika Gloria Br Sitorus , Sintia Karina Putri , Ana Gabriela Silva Olivera , Livia Ramos Santiago , Princella Halim , Amer Ahmed , Aasia Bibi , Aminah Dalimunthe , Poppy Anjelisa Zaitun Hasibuan , Moon Nyeo Park , Rosy Iara Maciel de Azambuja Ribeiro , Bonglee Kim , Pornphimon Meesakul , Shugeng Cao","doi":"10.1016/j.ejmcr.2025.100313","DOIUrl":"10.1016/j.ejmcr.2025.100313","url":null,"abstract":"<div><div>MicroRNAs are essential post-transcriptional regulators of gene expression, playing dual roles in oncogenesis as either oncogenes or tumour suppressors. Aberrant miRNA expression is a critical factor in cancer progression, influencing tumour development, metastasis, resistance to apoptosis, and therapy evasion. Concurrently, therapeutic peptides have emerged as promising modulators of miRNA activity due to their specificity, low toxicity, and ability to interact with nucleic acids. This review provides of peptide-mediated modulation of miRNA pathways in cancer, emphasising strategies such as degradation of oncogenic miRNAs, stabilization of tumour-suppressive miRNAs, and the targeted delivery of miRNA therapeutics. These methodologies demonstrate the potential to reverse malignant phenotypes by reducing cell proliferation, suppressing metastasis, restoring normal cellular functions, and promoting apoptosis. The integration of peptide-based delivery systems with miRNA-targeted therapies represents a novel paradigm in precision oncology, addressing key challenges related to therapeutic specificity and systemic delivery.</div></div>","PeriodicalId":12015,"journal":{"name":"European Journal of Medicinal Chemistry Reports","volume":"16 ","pages":"Article 100313"},"PeriodicalIF":0.0,"publicationDate":"2026-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145787390","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Nitrofuranyl derivatives as promising antitubercular agents: Structural insights and drug discovery perspectives","authors":"Afreen N , Smriti Sharma","doi":"10.1016/j.ejmcr.2025.100314","DOIUrl":"10.1016/j.ejmcr.2025.100314","url":null,"abstract":"<div><div>The emergence of MDR (multidrug-resistant) and XDR (extensively drug-resistant) variants of <em>Mycobacterium tuberculosis</em> has contributed to the universal resurgence of tuberculosis (TB). Nitrofuran-based compounds, traditionally used as antibacterial agents, have recently gained attention for their potential antitubercular properties. This review presents a comprehensive overview of structural classes of nitrofuran derivatives—including nitrofuranylamides, hydrazides, triazoles, spirocyclic hybrids, and prodrugs—and their corresponding structure–activity relationships, efficacy profiles, and safety evaluations. Several lead compounds exhibit potent <em>in vitro</em> as well as <em>in vivo</em> activity, often surpassing the effectiveness of existing TB drugs while maintaining favorable cytotoxicity and selectivity indices. Repurposing strategies and chemical modifications have significantly improved their pharmacological profiles, offering promising avenues for TB drug discovery. While current findings are encouraging, further mechanistic studies, pharmacokinetic optimization, and translational research are essential to advance nitrofuran derivatives toward clinical application. This review underscores the therapeutic value of nitrofuran scaffolds and supports their continued exploration as viable candidates in the global effort to combat TB.</div></div>","PeriodicalId":12015,"journal":{"name":"European Journal of Medicinal Chemistry Reports","volume":"16 ","pages":"Article 100314"},"PeriodicalIF":0.0,"publicationDate":"2026-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145683368","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Evaluation of the hepatoprotective properties of Vitex Altissima bark extracts and isolated bioactive: In-vitro and In-vivo approach","authors":"I.A. Chethan , Jaishree Vaijanathappa","doi":"10.1016/j.ejmcr.2025.100312","DOIUrl":"10.1016/j.ejmcr.2025.100312","url":null,"abstract":"<div><div><em>Vitex altissima</em> (<em>V. altissima</em>), an ethnopharmacologically valuable plant, is explicitly used as traditional medicine by local folks to cure liver-related disorders in Coorg. Hence, the present study aimed to evaluate the bark extract's hepatoprotective and antioxidant mechanisms and its isolated potent compound against CCl<sub>4</sub>-induced toxicity. Ethanolic bark extracts underwent phytochemical screening, LC-MS profiling and bioactivity-guided antioxidant assays, including DPPH and hydroxyl radical scavenging methods. Preparative HPLC enabled the isolation of three compounds, among which Isolate-1 demonstrated the most potent bioactivity and was structurally characterized as Albafuran C via FTIR, NMR, and LC-MS/MS analyses. <em>In vitro</em> hepatoprotection studies using HepG2 cells revealed that pretreatment with Isolate-1 significantly enhanced cell viability, suppressed CCl<sub>4</sub>-induced oxidative stress, and restored antioxidant enzyme levels (SOD, CAT). Flow cytometry confirmed reduced intracellular ROS and iNOS expression, supporting its antioxidative and anti-inflammatory potential. <em>In vivo</em> experiments in CCl<sub>4</sub>-induced Wistar rats demonstrated significant amelioration of hepatic markers (ALT, AST, ALP, bilirubin, and albumin) and restoration of liver histoarchitecture upon treatment with Isolate-1. Molecular analysis by RT-PCR and Western blotting revealed downregulation of NF-κB signaling and inflammatory mediators. These findings confirm the hepatoprotective mechanism of <em>V. altissima</em>, substantiating its traditional use and identifying Albafuran C as a promising phytotherapeutic agent. This study establishes a scientific rationale for further development of Albafuran C as a natural hepatoprotective compound targeting oxidative and inflammatory liver injury.</div></div>","PeriodicalId":12015,"journal":{"name":"European Journal of Medicinal Chemistry Reports","volume":"16 ","pages":"Article 100312"},"PeriodicalIF":0.0,"publicationDate":"2026-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145617527","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Xiaoya Li , Wen-Li Fu , Fenfen He , Xiaoli Xu , Bianxiang Hu , Yuqing Wang , Shuo-Bin Chen , Jianmin Chen
{"title":"Sanguinarine alleviates cisplatin-induced apoptosis in AKI by upregulating BCL-2 through targeting the gene promoter i-motif","authors":"Xiaoya Li , Wen-Li Fu , Fenfen He , Xiaoli Xu , Bianxiang Hu , Yuqing Wang , Shuo-Bin Chen , Jianmin Chen","doi":"10.1016/j.ejmcr.2025.100316","DOIUrl":"10.1016/j.ejmcr.2025.100316","url":null,"abstract":"<div><div>Acute kidney injury (AKI) is a severe clinical condition with high morbidity and mortality. Apoptosis of renal tubular epithelial cells is a key pathological driver, and upregulation of the anti-apoptotic protein <em>BCL-2</em> is a validated protective mechanism. The <em>BCL-2</em> promoter harbors a C-rich sequence capable of forming an i-motif, a non-canonical DNA secondary structure with regulatory functions. Previous studies have reported steroid-like molecules as potential ligands for the <em>BCL-2</em> i-motif, but their interactions were generally weak and lacked systematic pharmacophore insight. Here, we identify Sanguinarine (<strong>SG</strong>), a benzophenanthridine alkaloid, as a more potent ligand from a natural product library. Surface plasmon resonance (SPR) revealed broad-spectrum binding of <strong>SG</strong> to multiple promoter i-motifs, yet circular dichroism (CD) and melting assays suggested a relatively stronger stabilizing effect on the BCL-2 C-rich structure under our assay conditions. This apparent conformational preference, rather than strict binding selectivity, led to transcriptional activation of <em>BCL-2</em> and protection of HK-2 cells from cisplatin-induced apoptosis. While i-motifs have only rarely been explored in AKI, our study provides new mechanistic insight by defining an aromatic–cationic pharmacophore and suggesting that structure-dependent stabilization may serve as a plausible mechanism for promoter-specific modulation. These findings support the biological relevance of the <em>BCL-2</em> i-motif and highlight natural products as valuable scaffolds for nucleic-acid–interacting agents in renal injury models.</div></div>","PeriodicalId":12015,"journal":{"name":"European Journal of Medicinal Chemistry Reports","volume":"16 ","pages":"Article 100316"},"PeriodicalIF":0.0,"publicationDate":"2026-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145734032","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Imidazole‒sulfonamide hybrid conjugate: A privilege scaffold with significant therapeutic potential","authors":"Riham M. Bokhtia","doi":"10.1016/j.ejmcr.2025.100321","DOIUrl":"10.1016/j.ejmcr.2025.100321","url":null,"abstract":"<div><div>Combining two or more biologically active moieties in a single structure recently became one of the most proposed concepts that have been adopted in drug development process. Enhanced efficacy, limited side effects and declined drug resistance are the main features of molecular hybridization approach. Both imidazole and sulfonamide cores are valuable pharmacophores and precious structural motifs of highly anticipated medicinal interest that grabbed researchers’ attention in the last few years and could serve as lead candidates with prodigious antibacterial, antifungal, antiviral, anticancer, anti-inflammatory, anticholinesterase, antioxidant and antidiabetic significance. Imidazole tethered sulfonamides utilized a shotgun strategy through binding to different sites on receptor, hitting multiple targets and exhibiting synergized therapeutic potential, dual inhibitory activity against various diseases including drug-resistant forms with diminished adverse reactions. This comprehensive review focuses on the fruitful influence of connecting these two scaffolds in a single hybrid molecule and outlines the promising biological importance of some imidazole‒sulfonamide conjugates as multitarget‒directed ligands (MTDLs) in terms of structure‒activity relationships.</div></div>","PeriodicalId":12015,"journal":{"name":"European Journal of Medicinal Chemistry Reports","volume":"16 ","pages":"Article 100321"},"PeriodicalIF":0.0,"publicationDate":"2026-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145920795","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Yue Zhang , Tingting Lu , Xuping Luo , Chang Jin , Meizhu Zheng , Dongfang Shi , Kai Song , Qicheng Ying , Yongxing Ai
{"title":"Elucidating the mechanism of anti-ischemic stroke action of Irisflorentin:A combined approach using network pharmacology, molecular docking, and in vitro validation","authors":"Yue Zhang , Tingting Lu , Xuping Luo , Chang Jin , Meizhu Zheng , Dongfang Shi , Kai Song , Qicheng Ying , Yongxing Ai","doi":"10.1016/j.ejmcr.2025.100318","DOIUrl":"10.1016/j.ejmcr.2025.100318","url":null,"abstract":"<div><div>Irisflorentin, an isoflavonoid isolated from <em>Belamcanda chinensis</em> (L.) Redouté, serves as a key bioactive molecule in Sagittaria, exhibiting antioxidative, hypoglycemic, and anti-inflammatory properties. Despite these attributes, the precise roles and mechanisms of Irisflorentin in mitigating cerebral ischemia/reperfusion injury are not well elucidated. This study aims to clarify the therapeutic targets and pathways of irisflorentin in ischemic stroke utilizing network pharmacology, molecular docking, molecular dynamics simulation and experimental validation. The predictions generated by network pharmacology and molecular docking concerning potential targets and pathways. Irisflorentin influences numerous biological processes, such as signaling, protein phosphorylation, the suppression of neuronal apoptosis and the amplification of the MAPK cascade. Key targets identified via molecular docking include ESR1, EGFR, HIF1A, HSP90AB1, CCND1, ERBB2, MTOR, ESR2, MAPK8, and MAPK1. Molecular dynamics simulations indicate that the Irisflorentin small molecule exhibits favourable binding interactions with the HIF1A and MTOR target proteins.Cellular studies showed that irisflorentin improves cellular morphology, boosts cell viability and mitochondrial membrane potential, and decreases LDH release, ROS production, Ca<sup>2+</sup> levels, and apoptosis rates. IFR enhances the expression of PI3K, AKT, mTOR, Bcl-2, BDNF, TRқB, ERK1, ERK2, p90RSK, and CREB, while suppressing FOXO1A, HIF1A, Bax, and Caspase-3.Ultimately, Irisflorentin promotes neuroprotection and lessens cerebral ischemia/reperfusion damage by activating the PI3K/AKT/FOXO1A, mTOR/HIF1A, and BDNF/TRқB/ERK1/2/p90RSK/CREB pathways, underscoring its potential as an adjunct therapy for ischemic stroke and providing a foundation for its further development and clinical utility.</div></div>","PeriodicalId":12015,"journal":{"name":"European Journal of Medicinal Chemistry Reports","volume":"16 ","pages":"Article 100318"},"PeriodicalIF":0.0,"publicationDate":"2026-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145787345","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Giorgio Antoniolli , Gabriel Rodrigues de Moraes , Caterina Deruvo , Cosimo Damiano Altomare , Fernando Coelho , Modesto de Candia
{"title":"N-Acylhydrazones: applications and advances in drug discovery","authors":"Giorgio Antoniolli , Gabriel Rodrigues de Moraes , Caterina Deruvo , Cosimo Damiano Altomare , Fernando Coelho , Modesto de Candia","doi":"10.1016/j.ejmcr.2025.100317","DOIUrl":"10.1016/j.ejmcr.2025.100317","url":null,"abstract":"<div><div><em>N</em>-Acylhydrazones (NAHs) represent a structurally versatile and pharmacologically active class of compounds widely explored over last two decades in medicinal chemistry. Characterized by the presence of both hydrazide and imine functionalities, NAHs exhibit a rich spectrum of biological activities, including anti-inflammatory, antimicrobial, antitubercular, antiprotozoal, anticancer, and antiviral effects, as showed by a number of approved drugs (nitrofurazone, nitrofurantoin, carbazochrome, nifuroxazide, dantrolene, and azumolene) containing the NAH framework. Although discussion about toxicity, and efficacy of NAH-based drugs, several derivatives have been developed as a strategy to overcome failure and resistance in drug discovery. Indeed, in the NAH derivatives key physicochemical properties (lipophilicity/solubility, hydrogen-bonding property, and geometric or conformational isomerism) can easy modulated, to enhance their ability to generate bioactive small-molecules. In this review, by considering the PubMed, Scopus, Web of Science, and Google Scholar databases, we would provide a comprehensive current landscape of the therapeutic potential in drug-design and the state of the art of NAH progresses in pharmaceutical research.</div></div>","PeriodicalId":12015,"journal":{"name":"European Journal of Medicinal Chemistry Reports","volume":"16 ","pages":"Article 100317"},"PeriodicalIF":0.0,"publicationDate":"2026-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145787344","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Ana Álvarez-Mena , Mélanie Berbon , Carmelo Di Primo , Rebeca Garcia-Fandino , Ángel Piñeiro , Carlos Fernandez-Lozano , Hugo A.L. Filipe , Birgit Habenstein
{"title":"Exploiting the synergy between computational and experimental biophysics for efficient cancer drug development","authors":"Ana Álvarez-Mena , Mélanie Berbon , Carmelo Di Primo , Rebeca Garcia-Fandino , Ángel Piñeiro , Carlos Fernandez-Lozano , Hugo A.L. Filipe , Birgit Habenstein","doi":"10.1016/j.ejmcr.2025.100320","DOIUrl":"10.1016/j.ejmcr.2025.100320","url":null,"abstract":"<div><div>Targeted cancer therapies have revolutionized oncology by developing treatments that specifically target cancer cells, reducing side effects. However, traditional drug discovery approaches are often hindered by high costs, long timelines, and low success rates. To address these challenges, the combination of computational and experimental biophysical techniques has become a highly effective approach. Molecular modeling methods, such as docking, molecular dynamics simulations, and virtual screening, enable <em>in silico</em> identification and optimization of drug candidates, while experimental biophysical techniques like NMR, SPR, and BLI validate molecular structures, binding interactions and affinities. This combined approach enhances the precision and efficiency of drug discovery, enabling progress in targeting oncogenic mutations, disrupting protein-protein interactions, and advancing drug repurposing efforts. Despite its potential, several challenges remain, including predictive limitations in computational models, experimental reproducibility, and the complexity of integrating diverse datasets. Future advances, particularly in artificial intelligence-driven methodologies, high-throughput screening, and drug repurposing, hold great potential to accelerate the development of innovative and effective cancer therapies.</div></div>","PeriodicalId":12015,"journal":{"name":"European Journal of Medicinal Chemistry Reports","volume":"16 ","pages":"Article 100320"},"PeriodicalIF":0.0,"publicationDate":"2026-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145734033","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Zhaoqin Wen , Huiyun Yang , Hong Ling , Huicai Lin , Xiaoyan Chen , Wan-Lan Shi , Yongxiang Song , Jiang Deng
{"title":"Inhibition of ginsenoside Re on pulmonary fibrosis induced by bleomycin in mice: Involved in modulating the CX3CL1/CX3CR1 axis","authors":"Zhaoqin Wen , Huiyun Yang , Hong Ling , Huicai Lin , Xiaoyan Chen , Wan-Lan Shi , Yongxiang Song , Jiang Deng","doi":"10.1016/j.ejmcr.2025.100319","DOIUrl":"10.1016/j.ejmcr.2025.100319","url":null,"abstract":"<div><div>Pulmonary fibrosis (PF) is a common pathological feature of a variety of diffuse, progressive and irreversible pulmonary interstitial diseases, and effective therapeutic agents are currently lacking. Our previous study found that the total ginsenosides can improve pulmonary fibrosis induced by bleomycin in mice. Ginsenosides Re (G-Re) is one of the most abundant active ingredients in total ginsenosides and has a variety of pharmacological activities. This study investigated the inhibitory effect and mechanism of Re on pulmonary fibrosis in mice induced by bleomycin. The effects of G-Re on pulmonary fibrosis were evaluated using lung function measurement, pathological analysis, and detection of deposition of extracellular matrix (ECM). To investigate the mechanisms underlying the anti-pulmonary fibrosis effects of G-Re, chemokine CX3C ligand 1 (CX3CL1) and receptor 1 (CX3CR1), transforming growth factor beta 1 (TGF-β1), mitogen-activated protein kinase 1/2 (MEK1/2), extracellular signal-regulated kinase1/2 (ERK1/2), matrix metalloproteinase 2 (MMP2), and tissue inhibitor of metalloproteinases-1 (TIMP-1) in lung tissues were detected by molecular biology techniques, immunofluorescence and immunohistochemistry. Treatment with G-Re ameliorated pulmonary fibrosis in mice induced by bleomycin. In addition, it downregulated the levels of CX3CL1, CX3CR1, TGF-β1, MEK1/2, and MMP2. It upregulated the level of TIMP-1. These findings indicate that G-Re exerts protective effects against pulmonary fibrosis, likely through suppression of the CX3CL1/CX3CR1 axis and coordinated regulation of the ERK 1/2 signaling pathway and matrix metalloproteinases (MMPs), leading to reduced alveolar basement membrane injury and diminished extracellular matrix (ECM) accumulation in murine lung tissue.</div></div>","PeriodicalId":12015,"journal":{"name":"European Journal of Medicinal Chemistry Reports","volume":"16 ","pages":"Article 100319"},"PeriodicalIF":0.0,"publicationDate":"2026-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145734031","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Glanish Jude Martis, Sowmya Maiya, Santosh L. Gaonkar
{"title":"Synthetic developments and biological insights of 1,2,3-triazoles: Unravelling scope for drug discovery","authors":"Glanish Jude Martis, Sowmya Maiya, Santosh L. Gaonkar","doi":"10.1016/j.ejmcr.2025.100315","DOIUrl":"10.1016/j.ejmcr.2025.100315","url":null,"abstract":"<div><div>1,2,3-Triazoles have emerged as instrumental heterocyclic scaffolds playing key role in the field of synthetic and medicinal chemistry. The recent advancements utilizing the evolving technologies and the subsequent development of various synthetic strategies have dragged the attention based on their merits when compared to those with classical methods. In this review, different synthetic methods such as metal-catalyzed cycloaddition and metal-free reactions have been discussed with their noteworthy results. Also, focussing on the eco-friendliness domain, reactions following the green principles have been included. The scope of click reactions is wide and their optimisations play a crucial role. Erstwhile, the biological activity of the potential medicinal targets has opened a wide-gateway for the future medicinal chemistry and chemical biology. The impact of potent triazoles in appropriate areas is inclined throughout the review having the coverage of past twelve years which would help researchers working on discovery chemistry and biology across the world.</div></div>","PeriodicalId":12015,"journal":{"name":"European Journal of Medicinal Chemistry Reports","volume":"16 ","pages":"Article 100315"},"PeriodicalIF":0.0,"publicationDate":"2026-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145683307","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}