Current topics in medicinal chemistry最新文献

{"title":"Purpurogallin: A Multi-targeting Benzotropolone with Promising Anti-cancer and Chronic Disease Applications.","authors":"Navin Kumar Tailor","doi":"10.2174/0115680266430982260324184212","DOIUrl":"https://doi.org/10.2174/0115680266430982260324184212","url":null,"abstract":"<p><p>Purpurogallin is a naturally occurring benzotropolone derivative, first isolated from oak nutgalls, and has emerged as a molecule of significant biomedical interest due to its broad spectrum of bioactivities. It exhibits anticancer, antioxidant, anti-inflammatory, anti-platelet, anti-thrombotic, antibacterial, antimalarial, diabetic nephropathy, and neuroprotective properties. Mechanistically, purpurogallin modulates several key signaling pathways, including NF-κB, MAPK, c-Fos, NFATc1, and TNNT2, which are central to inflammation, apoptosis, and cellular proliferation. Its anticancer potential is underscored by its ability to inhibit crucial oncogenic targets such as Pololike kinases (PLKs), xanthine oxidase, and catechol-O-methyltransferase (COMT). These interactions disrupt cancer cell growth, induce apoptosis, and maintain cellular redox homeostasis. Additionally, its structural resemblance to tropolone-based pharmacophores enhances its utility as a scaffold in anticancer drug development, allowing for strategic chemical modifications to improve efficacy and selectivity. Recent research highlights its promise in the treatment of oxidative stressrelated disorders, including diabetic nephropathy and neurodegenerative diseases, through its potent redox-modulating capabilities. This multifaceted bioactivity profile positions purpurogallin as a compelling candidate for therapeutic advancement. This review delves into the current body of evidence on purpurogallin's biological effects, molecular mechanisms, and synthesis, emphasizing its dual functionality in targeting cancer-related signaling and oxidative stress. Such findings support further investigation into its pharmacological optimization and development as a lead compound in future drug discovery efforts.</p>","PeriodicalId":11076,"journal":{"name":"Current topics in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":3.3,"publicationDate":"2026-04-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147671255","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"A Review on the Development of Semisynthetic Phytochemicals in the Discovery of Anticancer Drugs.","authors":"Fatma Zehra Alkac, Cem Yamali","doi":"10.2174/0115680266467530260405204054","DOIUrl":"https://doi.org/10.2174/0115680266467530260405204054","url":null,"abstract":"<p><p>Cancer is a serious public health problem worldwide, and research into the development of new targeted cancer drugs is continuing intensively. A wide variety of approaches have been developed, ranging from traditional cytotoxic agents to modern targeted therapies, antibody-drug conjugates, immunotherapies, and advanced drug delivery systems, etc. The integration of omics strategies, bioinformatics, network pharmacology, molecular docking, molecular dynamics simulation, and artificial intelligence techniques into the process has accelerated the development of modern cancer treatments. While the search for different cancer treatment methods and anticancer drugs continues intensively, semi-synthetic drug designs still attract attention. As most targeted anticancer drugs are insufficient in clinical treatment, natural products and their derivatives are important in new multi-targeted anticancer drug research. Alongside traditional plant-derived anticancer agents, cardamonin, harmin, podophyllotoxin, β-carboline, magnolol, α-onocerin, boehmeriasin A, parthenolide, celastrol, pinosembrin, furochromone, curcumin, diosgenin, betulinic acid, ursolic acid, honokiol, goniodiol, scopoletin, caffeic acid, and pinocembrin derivatives have attracted interest due to their enhanced efficacy and selectivity relative to their natural analogs. These phytochemicals or their derivatives offer new strategies and have the potential to reduce the side effects of traditional treatments and overcome drug resistance. This review aims to discuss recent semisynthetic advancements in natural product research for anticancer drug development. It demonstrates that several semisynthetic anticancer candidates with enhanced selective anticancer effects compared to natural precursors have been developed, and that problems such as low bioactivity, poor solubility, or selectivity issues can be effectively resolved through the rational design of the chemical structures of their natural analogs.</p>","PeriodicalId":11076,"journal":{"name":"Current topics in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":3.3,"publicationDate":"2026-04-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147671032","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"In Vitro and In Silico Approaches for the Evaluation of Antimycobacterial and Biofilm Inhibition Activity of Asiatic Acid Against Dual Targets of Mycobacterium smegmatis.","authors":"Kratika Singh, Tarun Kumar Upadhyay, Ambreen Bano, Niharika Pandey, Sorabh Lakhanpal, Rolee Sharma","doi":"10.2174/0115680266395445251204125654","DOIUrl":"https://doi.org/10.2174/0115680266395445251204125654","url":null,"abstract":"<p><p>The increasing resistance to anti-TB drugs has become a global issue, highlighting an urgent need to investigate new drug candidates for combating Mycobacterium tuberculosis (M.tb.). Asiatic Acid (AA), a major phytoconstituent of Centella asiatica, exhibits anti-microbial and anti-biofilm activities against several microbes. In the present investigation, AA was explored for prospective anti-biofilm activity against mycobacteria.</p><p><strong>Methods: </strong>We first used a computational approach to probe the in silico inhibitory potential of AA against selected target proteins of the FAS-II pathway, involved in mycolic acid biosynthesis, which contributes to mycobacterial cell wall and biofilm formation. Further, in vitro anti-mycobacterial assays were performed to determine the inhibitory concentration and biofilm inhibition against M. smegmatis, which was quantified by crystal violet staining and validated by SEM and CLSM.</p><p><strong>Results: </strong>The structure-based inhibitory potential of AA was evaluated against β-Ketoacyl ACP Synthase (KasA) and Enoyl acyl carrier protein (InhA) by molecular docking analysis, showing good binding affinities, with binding energies of -9.53 kcal/mol and -10.53 kcal/mol, and inhibition constants of 3.04 μM and 80.20 nM, respectively. Further, the in vitro anti-mycobacterial assays confirmed the MIC as 20 μg/ml against M. smegmatis. A conspicuous reduction in mycobacterial biofilm formation was observed upon exposure to AA at the MIC, as quantified by crystal violet staining and validated by SEM and CLSM. The EC50 value, the concentration showing 50% inhibition of biofilm formation, was observed as 40 μg/ml against M. smegmatis.</p><p><strong>Discusssion: </strong>This study shows advancement in understanding the natural compound AA as a potent anti-tubercular compound by elucidating its dual mechanism of action, including antimycobacterial and anti- biofilm activity, and by targeting enzymes of the FASII pathway, i.e., InhA and KasA. The present in vitro investigation suggests that asiatic acid may serve as a good anti- TB compound, with the possibility of potentiation of anti- mycobacterial effects via additional biofilm-inhibition activity.</p><p><strong>Conclusion: </strong>These findings are expected to pave the way for the design and development of novel anti-TB medications and strategies that enhance treatment efficacy and minimize resistance development in this persistent pathogen. Further investigations are required to determine the mode of action and validate its candidacy as a promising anti-biofilm agent in the current clinical setting.</p>","PeriodicalId":11076,"journal":{"name":"Current topics in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":3.3,"publicationDate":"2026-04-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147671068","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Antiviral Activity of Synthetic Bis-Naphthoquinone (H-5) against Chikungunya Virus Replication.","authors":"Max Willian Lisboa Gomes, Priscilla Esteves de Assis, Victória Maranhão, Rafaela Dos Santos Pereira, Claudio Cesar Cirne-Santos, Kíssila Rabelo, Jorge Jose de Carvalho, Daniel Tadeu Gomes Gonzaga, Fernando de Carvalho da Silva, Vitor Francisco Ferreira, Caroline de Souza Barros, Izabel Christina Palmer Paixão","doi":"10.2174/0115680266358458251009100413","DOIUrl":"https://doi.org/10.2174/0115680266358458251009100413","url":null,"abstract":"<p><strong>Introduction: </strong>The chikungunya virus (CHIKV) is a significant public health concern, as it is one of the most critical re-emerging infections and still lacks specific treatment or vaccination measures.</p><p><strong>Methods: </strong>In this study, bis-naphthoquinone (H-5) was tested in CHIKV-infected cells and mice. Several techniques were employed to understand the drug's mechanism of action.</p><p><strong>Results: </strong>Cytotoxicity (CC50) and antiviral activity (EC50) tests revealed that H-5 presented low toxicity 1103 μM and good antiviral potential 0.96 μM. Virucidal test and time of addition of the compound to verify the mechanism of action presented good results. In vivo assays showed promise. In addition, synergism tests with Ribavirin indicated a strong synergistic effect.</p><p><strong>Discussion: </strong>The antiviral effect associated with low toxicity demonstrates that the compound shows promise. In addition, the mechanism of action studies is crucial for the characterization of a good compound. Tests in mice demonstrated potential reduction of edema and favorable histological changes.</p><p><strong>Conclusion: </strong>It is concluded that H-5 is a promising antiviral candidate against CHIKV.</p>","PeriodicalId":11076,"journal":{"name":"Current topics in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":3.3,"publicationDate":"2026-04-06","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147627484","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Contemporary Developments in PROTACs for Cancer Management: An In-Depth Review.","authors":"Shaik Abdul Rahaman, Garla Venkateswarlu, Sakshi Patel, Prem Shankar Mishra, Rahul Kumar, Nayyar Parvez","doi":"10.2174/0115680266384226251013054011","DOIUrl":"https://doi.org/10.2174/0115680266384226251013054011","url":null,"abstract":"<p><p>Proteolysis-Targeting Chimeras (PROTACs) represent a novel and promising cancer treatment strategy considered a direct alternative to conventional small-molecule inhibitors. PROTACs selectively degrade disease-causing proteins (including previously 'undruggable' targets such as transcription factors and scaffolding proteins) by harnessing the cellular ubiquitin proteasome system. In this review, we look at the most recent developments in PROTAC technology and their oncology applications. Versatility, while maintaining substrate selectivity and degradation efficiency, has also been enhanced by the expanded range of E3 ligases used in PROTAC design. Improvements in the stability, bioavailability, and systemic delivery of PROTACs are being achieved through innovations in pharmacokinetics and cell permeability, enabling their clinical translations. Initial clinical trials have confirmed the potential of these agents in human patients, and early preclinical studies have shown them to be highly efficacious in models of solid tumors and hematologic malignancies. Despite these encouraging developments, crucial challenges remain, including reducing off-target effects, addressing resistance mechanisms, and clarifying the significance of PROTAC-mediated degradation pathways. Future efforts must focus on refining the selectivity and tunability of degrader compounds, enhancing treatment efficacy via combination therapies, and optimizing PROTAC design through computational and structural biology. As the field continues to evolve, PROTACs remain a highly promising strategy for addressing unmet clinical needs in oncology. In this review, recent advancements in PROTAC technology are discussed, along with its contribution to cancer therapy and ways to circumvent existing challenges to its full therapeutic potential.</p>","PeriodicalId":11076,"journal":{"name":"Current topics 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":"147618606","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Small Molecule Inhibitors Targeting Pathogenic Protein Aggregation in Neurodegenerative Diseases: Medicinal Chemistry and Mechanistic Insights.","authors":"Kishna Ram Senwar, Anjali Dhillon, Monu Yadav","doi":"10.2174/0115680266439510260223082224","DOIUrl":"https://doi.org/10.2174/0115680266439510260223082224","url":null,"abstract":"<p><p>A hallmark of Neurodegenerative Diseases (NDs) is protein misfolding, aggregation, and accumulation in specific brain regions. The accumulation of insoluble, misfolded protein aggregates is usually referred to as amyloid formation. This process leads to cellular dysfunction, destruction of neurons, loss of neuronal connections in specific brain areas, and brain damage. Despite the involvement of distinct pathogenic proteins, the underlying mechanisms of misfolding and aggregate formation are remarkably similar across various NDs. In this review, we present a comprehensive overview of the medicinal chemistry and mechanistic insights into phytochemicals and synthetic small molecules with potential for the treatment of neurodegenerative disorders. Various small molecules have been reported to have therapeutic effects by inhibiting the misfolding, aggregation, and accumulation of pathogenic proteins, such as amyloid-β, tau, and α- synuclein. This review mainly covers natural product-derived small molecules, notably polyphenols (including flavonoids and non-flavonoid polyphenols), as well as other phytochemical classes, such as quinones and alkaloids, along with their possible mechanisms of action. In addition, synthetic small molecules, osmolytes, metal chelators, and repurposed drugs for neurodegenerative disorders are thoroughly discussed.</p>","PeriodicalId":11076,"journal":{"name":"Current topics in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":3.3,"publicationDate":"2026-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147608161","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Research Progress on Membranous Nephropathy-Related Antigens and Immune-Targeted Therapy.","authors":"Lu Sui, Zihang Jin, Yilin Meng, Haoze Wu, Ligeer Che, Li Sun","doi":"10.2174/0115680266410507260224062006","DOIUrl":"https://doi.org/10.2174/0115680266410507260224062006","url":null,"abstract":"<p><p>Chronic Kidney Disease (CKD) has emerged as a significant global public health concern, with membranous Nephropathy (MN) being the most prevalent pathological type of nephrotic syndrome in adults. MN is classified as an antibody-mediated autoimmune disease. There is a growing interest in the research of MN-related antigens. Furthermore, the treatment of MN predominantly relies on the administration of immunosuppressants, with traditional regimens such as corticosteroids and cyclophosphamide, which have significant side effects, and rituximab, having a 35-40% failure rate, highlighting the critical need for the development of specific and effective immunotherapy strategies. In this review, we summarized the research progress on newly discovered MN-related antigens, including exostosin 1/exostosin 2(EXT1/EXT2), Neural Cell Adhesion Molecule 1 (NCAM-1), Neural Epidermal Growth Factor-like 1 (NELL-1), Contactin 1 (CNTN1), Semaphorin 3B, High-Temperature Recombinant Protein A1 (HTRA1), protocadherin FAT atypical cadherin 1(FAT1) and Protocadherin 7(PCDH7). Among them, NELL-1 and HTRA1 primarily serve as target antigens for primary MN, and their serum antibody titers show a strong correlation with disease activity. While EXT1/EXT2, NCAM1, CNTN-1, and FAT1 mainly act as target antigens for secondary MN. In addition, we evaluated the clinical applications and efficacy of novel immunosuppressants and therapeutic approaches, including new anti-CD20 antibodies, proteasome inhibitors, anti-plasma cell therapies, belimumab, complement inhibitors, and immunoadsorption. The new anti-CD20 agents represented by obalimumab and obinutuzumab, along with anti-plasma cell therapies such as daratumumab, have emerged as ideal alternatives for patients with rituximab resistance. Other therapeutic approaches, including complement inhibitors, immunoadsorption, and belimumab, have also exhibited their unique advantages.</p>","PeriodicalId":11076,"journal":{"name":"Current topics 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":"147608205","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Preparation of Curcumin-Loaded Nanocarriers and its Application on Promoting Wound Healing.","authors":"Jingyi Yuan, Jie Yu, Lijie Sun, Xiaobo Luo, Yang Liu, Xinrui Wang","doi":"10.2174/0115680266397479250823161555","DOIUrl":"https://doi.org/10.2174/0115680266397479250823161555","url":null,"abstract":"<p><strong>Introduction: </strong>To address curcumin's limitations (e.g., poor solubility and low bioavailability), we developed a curcumin-loaded ZnMgAl-layered double hydroxide nanocomposite (Cur@LDHs), aiming to enhance its therapeutic efficacy in wound healing.</p><p><strong>Methods: </strong>The study involves the preparation of ZnMgAl-LDHs as the carrier and the synthesis of Cur@LDHs composites through co-precipitation. Characterization of the composites is performed using XRD and FT-IR. In vitro release experiments are conducted using the dialysis bag method, and stability tests are performed under different temperature conditions. Biocompatibility and cell migration assays are carried out on human skin fibroblast (HSF) cells. In vivo wound healing studies are performed on a rat model, with histological evaluation and ELISA assays for inflammatory factors.</p><p><strong>Results: </strong>The XRD and FT-IR analyses confirm the successful loading of curcumin onto LDHs. In vitro release experiments show that Cur@LDHs exhibit slow and sustained release characteristics, reducing the cytotoxicity of pure curcumin. Cell migration experiments indicate that Cur@LDHs significantly enhance the migration rate of HSF cells compared to pure curcumin. In vivo studies demonstrate that Cur@LDHs significantly promote wound healing, with reduced inflammatory responses and improved re-epithelialization and collagen deposition. The ELISA results show that Cur@LDHs effectively reduce the levels of IL-1β and TNF-α proteins in traumatic tissues.</p><p><strong>Discussion: </strong>The Cur@LDHs composite demonstrated significant potential in accelerating wound healing by synergizing the sustained release of curcumin with bioactive Zn2+/Mg2+ ions from the hydrotalcite carrier, which promoted fibroblast migration and collagen deposition. This dual-action mechanism-curcumin suppressing early inflammation (evidenced by reduced IL-1β/TNF-α) and LDH-released ions enhancing tissue regeneration-outperformed free curcumin or LDHs alone in both in vitro and in vivo models. While the system improved curcumin's stability and reduced cytotoxicity compared to conventional delivery methods, the study acknowledges limitations such as the lack of environmental simulations (humidity, infection) and a small animal cohort. Nevertheless, the results position Cur@LDHs as a promising bioactive wound dressing capable of stagespecific therapeutic intervention.</p><p><strong>Conclusion: </strong>Cur@LDHs demonstrated enhanced stability, sustained release, and reduced cytotoxicity compared to free curcumin. The composite synergistically accelerated wound healing in vitro (via HSF migration) and in vivo (90% wound closure by day 7 in rats) by modulating inflammation and promoting tissue regeneration. This study supports Cur@LDHs as a promising bioactive wound dressing.</p>","PeriodicalId":11076,"journal":{"name":"Current topics 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":"147608151","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Total Alkaloids of Yanhusuo Attenuate Chronic Cerebral Hypoperfusion-Induced Brain Injury: Mechanisms and Neuroprotection.","authors":"Bing Tian, Shuming Huang, Yutong Song, Biwei Bai, Jing Fang, Xiangming Sun, Chenxue Li, Yue Yang, Wenlan Li","doi":"10.2174/0115680266432740260106075226","DOIUrl":"https://doi.org/10.2174/0115680266432740260106075226","url":null,"abstract":"<p><strong>Introduction: </strong>Rhizoma Corydalis, which contains alkaloids as its main active moieties, is widely used in the treatment of cerebrovascular disorders. The present study aimed to investigate the neuroprotective effects and mechanisms of the total alkaloid from Yanhusuo (YHTA) against chronic cerebral hypoperfusion (CCH).</p><p><strong>Methods: </strong>Sixty Sprague-Dawley (SD) rats were randomly divided into sham, model, YHTA lowdose, medium-dose, high-dose, and nimodipine positive group (n=10). A CCH model was established by performing bilateral common carotid artery occlusion. Cognitive function was assessed using behavioral tests, and neuronal morphological alterations were analyzed by histopathology. Immunohistochemistry was used to assess microvessel density and the protein expression of HIF- 1α, VEGF, and VEGFR-2. Neuronal apoptosis was detected by TUNEL assay. The protein levels of HIF-1α, VEGF, VEGFR-2, Bax, and Bcl-2 were measured by Western blotting.</p><p><strong>Results: </strong>YHTA treatment ameliorated CCH-induced cognitive impairment, alleviated neuronal damage, and increased the number of surviving neurons. All doses of YHTA inhibited neuronal apoptosis, which was associated with the upregulation of Bcl-2 and downregulation of Bax expression. Furthermore, YHTA promoted cerebral angiogenesis and upregulated the expression of HIF- 1α, VEGF, and VEGFR-2 proteins.</p><p><strong>Discussion: </strong>These results provide a pharmacological basis for the clinical application of Corydalis in cerebrovascular diseases and identify YHTA as a multi-target agent against vascular cognitive impairment and hypoperfusion-related neurodegeneration.</p><p><strong>Conclusion: </strong>YHTA protects against nerve damage caused by CCH in the hippocampus. The mechanism may involve activation of the HIF-1α/VEGF/VEGFR-2 pathway, modulating the expression of apoptosis-related proteins Bcl-2 and Bax, and inhibiting nerve cell apoptosis, thereby promoting the generation of microvessels in brain tissue, improving blood flow supply, accelerating the repair of neurons, and playing a role in neuroprotection.</p>","PeriodicalId":11076,"journal":{"name":"Current topics in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":3.3,"publicationDate":"2026-03-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147590754","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Quercetin and Cancer: Molecular Mechanisms and Signaling Pathway Modulation for Therapeutic Benefits.","authors":"Md Al Amin, Mehrukh Zehravi, Hasna Bouhenni, Kurratul Aiun Siddika, Jeetendra Kumar Gupta, Rajeshwar Vodeti, Uppuluri Varuna Naga Venkata Arjun, Patibandla Jahnavi, Gayathri K, Ramenani Hari Babu, Abdul Ajeed Mohathasim Billah, P Dharani Prasad, Safia Obaidur Rab, Koula Doukani, Talha Bin Emran","doi":"10.2174/0115680266429919260224034527","DOIUrl":"https://doi.org/10.2174/0115680266429919260224034527","url":null,"abstract":"<p><p>Quercetin, a natural flavonoid found in vegetables and fruits, has been demonstrated to have potential anticancer properties. This review investigates the molecular mechanisms of quercetin's effectiveness in cancer prevention and treatment. The diverse effects of quercetin on key molecular signaling pathways, including PI3K/Akt, MAPK, NF-κB, and Wnt/β-catenin, are investigated for their roles in cell cycle progression, apoptosis, and metastasis. Quercetin effectively targets specific cancer signaling pathways, demonstrating promising therapeutic benefits such as the inhibition of proliferation, apoptosis, and suppression of metastasis. The review highlights the synergistic effects of quercetin in combination with conventional chemotherapy and radiotherapy, underscoring its potential to overcome drug resistance and enhance treatment efficacy. It investigates the underlying molecular complexities of quercetin's anticancer effects, providing valuable insights for developing targeted therapeutic strategies and optimizing quercetin-based cancer management interventions. The review explores quercetin's potential to combat drug resistance and enhance treatment efficacy, suggesting further research on optimal dosages, treatment regimens, and targeted patient populations. Furthermore, this review highlights quercetin's potent anticancer properties, suggesting further exploration for targeted therapies and improved cancer management strategies.</p>","PeriodicalId":11076,"journal":{"name":"Current topics in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":3.3,"publicationDate":"2026-03-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147590713","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}