Current topics in medicinal chemistry最新文献

{"title":"Phytochemicals of Biologically Active Fractions from Silene conoidea Leaves and Stems.","authors":"Akram Taleghani, Roya Moghimi, Samira Eghbali","doi":"10.2174/0115680266324758241223063534","DOIUrl":"https://doi.org/10.2174/0115680266324758241223063534","url":null,"abstract":"<p><strong>Background: </strong>Silene conoidea, a member of the Caryophyllaceae family, is a rare edible weed in Iran. It possesses various medicinal properties, including insecticidal, antimicrobial, antibacterial, and allelopathic effects.</p><p><strong>Methods: </strong>This study represents the investigation into the phytochemical contents, compounds, and biological activities of six different fractions [petroleum ether, chloroform, dichloromethane, ethyl acetate, methanol, and water] obtained from the leaves and stems of this species, with the aim of developing new natural drugs.</p><p><strong>Result: </strong>The methanol fractions of both the leaves and stems exhibited the highest levels of total phenolic and flavonoid contents and demonstrated strong antioxidant activity in the DPPH free radical scavenging method, with IC50 values of 5.1± 1.34 and 9.67 ± 0.02 μg/mL, respectively, surpassing the activity of BHT. Additionally, the chloroform and methanol fractions showed moderate antimicrobial activity against bacterial strains, with MIC values ranging from 0.0625 to 0.5 mg/ml when compared to gentamicin. The more active fractions [chloroform and methanol] were further analyzed to identify bioactive compounds. GC-MS analysis detected forty and forty-five compounds, representing 97.97% and 99.22% of the total composition, in the chloroform fractions of the leaves and stems, respectively. The main constituents of the leaves were fatty acid derivatives [54.66%] and terpene derivatives [21.94%], whereas the stems contained terpene derivatives [40.46%] and hydrocarbon derivatives [31.41%]. LC-ESI-MS analysis of the methanol fractions revealed the presence of common groups, including flavonoids, steroids, and triterpenoid saponins. Several bioactive compounds have been identified, including rutin, kaempferol-neohesperidoside derivative, diosmin, sileneoside, hesperidin, luteolin-di-O-glucoside, orientin-O-glucoside, vitexin- O-rhamnoside, and swertisin-O-glucoside. Heatmap analysis was conducted to visualize the differences in metabolite profiles among the samples.</p><p><strong>Conclusion: </strong>The analyzed fractions contained compounds with potential pharmacological activities.</p>","PeriodicalId":11076,"journal":{"name":"Current topics in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":2.9,"publicationDate":"2025-01-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143122382","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":"Advances in Synthetic Lethality in Potential Oncology Therapeutic Approaches.","authors":"Feifei Yang, Huiyu Wang, Shule Fan, Huiran Qiu, Xiangzhi Li, Guangyao Shi, Zihao Li, Xiaotian Luan, Haigang Wu","doi":"10.2174/0115680266349547241231051447","DOIUrl":"https://doi.org/10.2174/0115680266349547241231051447","url":null,"abstract":"<p><p>Synthetic lethality represents a novel paradigm in molecular targeted cancer therapy. In synthetic lethality, perturbation of one gene alone does not hinder cell viability, yet simultaneous perturbation of both genes results in a loss of cellular viability. The presence of gene mutations in cancer cells, as opposed to normal cells, provides an opportunity for targeted therapies that mimic the effects of the second genetic mutation, enabling selective eradication of cancer cells. Recent advances in high-throughput screening technologies, such as CRISPR-Cas9 and RNA interference, have significantly enhanced the identification of synthetic lethal interactions, expanding the potential targets for therapeutic intervention. Challenges in exploiting synthetic lethality for cancer treatment include the complexities of tumor biology, limited comprehension of synthetic lethal interactions, drug resistance, and impediments in screening and clinical translation. Emerging strategies, such as combination therapies and novel drug designs, are being developed to overcome these obstacles. By virtue of its selective lethality towards cancer cells bearing specific genetic alterations, targeting synthetic lethal genes holds the promise to provide wider therapeutic windows compared to traditional cytotoxic chemotherapy. This review describes the current state of synthetic lethality applications in cancer treatment, encompassing both biological and methodological perspectives. It highlights the latest advancements in synthetic lethality with emerging interventional strategies. Furthermore, it explores future directions for research and clinical implementation, aiming to refine and expand the therapeutic potential of synthetic lethality in oncology.</p>","PeriodicalId":11076,"journal":{"name":"Current topics in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":2.9,"publicationDate":"2025-01-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143122377","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":"Galegine, a Bioprivileged Alkaloid from Tithonia tubaeformis: Antipyretic Activity Insights.","authors":"Noor Ul Ain Nawaz, Muhammad Saeed, Shaheen Faizi, Irfan Ali, Muhammad Shafiq, Muhammad Shahid, Fazle Rabbi, Fahim Ullah Khan, Rabeea Sharif, Zaheer Ul-Haq, Khalid Mohammed Khan, Hassan A Hemeg, Waleed Al Abdulmonem, Abdullah S M Aljohani, Abdur Rauf","doi":"10.2174/0115680266333237241212071912","DOIUrl":"https://doi.org/10.2174/0115680266333237241212071912","url":null,"abstract":"<p><strong>Background: </strong>In continuation of our chemical and biological work on Tithonia tubaeformis, we evaluated the antipyretic activity of its extract which on fractionation gives a pure alkaloid galegine. Galegine a bioprivileged compound, is a hemiterpene bearing a guanidine group, which holds significant importance in medicinal chemistry. Biological activities such as antimicrobial, antidiabetic, anti-inflammatory, cardiovascular, anticancer, and antihypertensive, are often associated with guanidine-containing molecules.</p><p><strong>Objective: </strong>Given the biological importance of guanidine and in search of safe antipyretic agents from natural resources, an in vivo antipyretic activity of methanolic extract of T. tubaeformis and galegine was conducted to discover a potential hypothermic drug candidate from the plant.</p><p><strong>Methods: </strong>In vivo, the antipyretic activity of galegine (5, 25, and 50 mg/kg doses) and methanolic extract of T. tubaeformis (50, 100, and 200 mg/kg doses) was investigated by employing yeastinduced pyrexia in mice model. In silico molecular docking analysis involving target enzymes cyclooxygenase- 1 (COX-1), cyclooxygenase-2 (COX-2), and microsomal prostaglandin E synthase-1 (mPGES-1) was conducted. Additionally, galegine underwent ADME/T profiling using SwissADME and Protox-II tools to evaluate its bioavailability and safety profiles.</p><p><strong>Results: </strong>Both the extract and galegine showed a progressive dose-dependent reduction in body temperatures of the hyperthermic test animals. Moreover, in silico molecular docking analysis revealed significant binding affinities ranging from -3.58 to -5.41 kcal/mol. ADME/T analyses of galegine predicted its high drug-likeness and good safety profile.</p><p><strong>Conclusion: </strong>These biological and computational approaches supported T. tubaeformis in addressing pyrexia, with the isolated compound galegine emerging as a promising antipyretic agent.</p>","PeriodicalId":11076,"journal":{"name":"Current topics in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":2.9,"publicationDate":"2025-01-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143063997","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":"Melatonin Overexpression in the Management of Alzheimer's Disease: Therapeutic Exploration.","authors":"Babita Gupta, Rishabha Malviya, Sonali Sundram, Sathvik Belagodu Sridhar, Deependra Pratap Singh","doi":"10.2174/0115680266327614241121050448","DOIUrl":"https://doi.org/10.2174/0115680266327614241121050448","url":null,"abstract":"<p><p>Alzheimer's Disease (AD), a progressive neurodegenerative disorder, is characterized by the accumulation of neurofibrillary tangles and β-amyloid plaques, leading to a decline in cognitive function. AD is characterized by tau protein hyperphosphorylation and extracellular β-amyloid accumulation. Even after much research, there are still no proven cures for AD. The neuroprotective, anti-inflammatory, and antioxidant qualities of melatonin, a hormone mostly produced by the pineal gland, have drawn interest as a possible treatment option for AD. This study looks at new evidence that suggests melatonin overexpression to be a promising therapy option for AD. Melatonin levels naturally decline with age and decrease more significantly in individuals with AD, worsening neurodegenerative processes. Melatonin has therapeutic potential as it inhibits Aβ formation, prevents amyloid fibril extension through structure-dependent interactions, and protects neurons from Aβ-induced toxicity. Melatonin promotes neurogenesis, which is decreased in AD, suggesting it may treat the disease's many pathologies. The review emphasizes the importance of melatonin's mechanisms of action, including its capacity to reduce neuroinflammation, regulate mitochondrial function, scavenge free radicals, and influence apoptotic pathways. As research into AD continues, this article provides a forward-looking perspective on how future studies could leverage melatonin's multifaceted neuroprotective properties to develop more effective treatments for AD.</p>","PeriodicalId":11076,"journal":{"name":"Current topics in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":2.9,"publicationDate":"2025-01-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143064013","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":"Chemical Profiling, Antioxidant, and Antiproliferative Activities of Algerian Cistus creticus L. Leaf Extracts: Evidence from In vitro and In Silico Studies.","authors":"Yacine Aouiffat, Farouk Benaceur, Boulanouar Bakchiche, Imededdine Kadi, Fathi Berrabah, Hicham Gouzi, Sanaa K Bardaweel, Ashok K Shakya, Asmaa S Mohamed, Mosad A Ghareeb","doi":"10.2174/0115680266345222250109102407","DOIUrl":"https://doi.org/10.2174/0115680266345222250109102407","url":null,"abstract":"<p><strong>Background: </strong>Research into oxidative stress, cancer, and natural products revealed promising avenues for therapeutic intervention. Natural products are considered potent pharmaceuticals in combating oxidative stress and its relationship with cancer.</p><p><strong>Methods: </strong>This study was carried out to evaluate the chemical profile and antioxidant activities using DPPH, ABTS, Phenanthroline, Cupric, Phosphomolybdenum, FRAP, Hydroxyl, Iron chelation in vitro assays, and anticancer properties by MTT method of Cistus creticus extracts. The chemical composition was determined using the LC/MS-MS technique. Therefore, in silico methods, particularly molecular docking and dynamic simulation were applied for molecular interaction analysis.</p><p><strong>Results: </strong>The obtained results revealed a wide variety of phenolic compounds in all studied fractions, in their qualitative and quantitative distribution. In most antioxidant assays, the butanol and ethyl acetate extracts exhibited the most effective effects, followed by the aqueous extract, while the petroleum ether and chloroform fractions exhibited much lower activity in comparison with standards. In parallel, ethyl acetate, n-butanol, and chloroform extracts exhibited potent antiproliferative activity against T47D and A549 cell lines, while the aqueous extract showed an IC50 in the range of mg/ml. Moreover, the analysis of interactions identified compounds against particular targets in studied cell lines using molecular docking showed a great affinity, especially for the ligands Hesperidin, Luteolin-7-O-glucoside and Rutin. Also, the molecular dynamic simulation of the interacting complexes Hesperidin-mTOR, Lutin-EGFR and Apigenin-HER2 revealed precise interaction, providing insights into their stability and dynamic behavior. Furthermore, the studied ligand exhibited interesting pharmacokinetic properties with no reported toxicity.</p><p><strong>Conclusion: </strong>These findings confirmed the potential of Algerian Cistus creticus L. leaf extracts as promising therapeutic molecules for combating oxidative stress and cancer.</p>","PeriodicalId":11076,"journal":{"name":"Current topics in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":2.9,"publicationDate":"2025-01-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143058069","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":"Roles of C/EBPβ/AEP in Neurodegenerative Diseases.","authors":"Jing Guo, Xin-Yi Liu, Sha-Sha Yang, Qiang Li, Yang Duan, Shan-Shan Zhu, Ke Zhou, Yi-Zhi Yan, Peng Zeng","doi":"10.2174/0115680266357822250119172351","DOIUrl":"https://doi.org/10.2174/0115680266357822250119172351","url":null,"abstract":"<p><p>In recent years, an increasing number of studies have shown that increased activation of aspartic endopeptidases (AEPs) is a common symptom in neurodegenerative diseases (NDDs). AEP cleaves amyloid precursor protein (APP), tau (microtubule-associated protein tau), α- synuclein (α-syn), SET (a 39-KDa phosphoprotein widely expressed in various tissues and localizes predominantly in the nucleus), and TAR DNA-binding protein 43 (TDP-43), and promotes their aggregation, contributing to Alzheimer's disease (AD), Parkinson's disease (PD), Huntington's disease, multiple sclerosis (MS), amyotrophic lateral sclerosis (ALS), and frontotemporal dementia (FTD) pathogenesis. Abundant evidence supports the notion that CCAAT/enhancer-binding protein β (C/EBPβ)/AEP may play an important role in NDDs. Developing its small molecule inhibitors is a promising treatment of NDDs. However, current research suggests that the pathophysiological mechanism of the C/EBPβ/AEP pathway is very complex in NDDs. This review summarizes the structure of C/EBPβ and AEP, their major physiological functions, potential pathogenesis, their small molecule inhibitors, and how C/EBPβ/AEP offers a novel pathway for the treatment of NDDs.</p>","PeriodicalId":11076,"journal":{"name":"Current topics in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":2.9,"publicationDate":"2025-01-27","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143051973","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":"Synthesis and Evaluation of Coumarin Clubbed Sulfanilamide and 2-Aminobenzothiazole Hybrids for Antibacterial Applications.","authors":"Suman Lata, Gagandeep Mehmi, Hardeep Kaur, Anuradha Sharma, Amit Pandit, Vikrant Abbot","doi":"10.2174/0115680266362029250111172921","DOIUrl":"https://doi.org/10.2174/0115680266362029250111172921","url":null,"abstract":"<p><strong>Background: </strong>The increasing prevalence of drug-resistant bacterial infections poses a significant challenge to global healthcare, necessitating the development of novel antibacterial agents. Coumarin-based derivatives are well-recognized for their diverse biological activities, and hybridization with other pharmacophores offers a promising strategy for enhancing therapeutic efficacy and overcoming resistance.</p><p><strong>Objective: </strong>This study aimed to synthesize and evaluate a novel series of coumarin hybrids by integrating the coumarin scaffold with sulfanilamide (9a-e) and 2-aminobenzothiazole (10a-e), targeting bacterial pathogens through a dual pharmacophoric approach.</p><p><strong>Methods: </strong>The synthesized hybrids were characterized using mass spectrometry, FTIR, and NMR (1H and 13C) to confirm their structural integrity. Antibacterial activity was assessed in vitro against Escherichia coli and Staphylococcus aureus at concentrations of 100, 250, and 500 μg/ml, with ciprofloxacin as the standard. The molecular binding mechanism was explored using molecular docking and pharmacophore-based analysis.</p><p><strong>Results: </strong>Among the synthesized derivatives, compounds 9e and 10e exhibited the highest antibacterial activity, with inhibition zones of 22 mm and 21 mm against E. coli and 25 mm and 22 mm against S. aureus at 500 μg/ml, demonstrating comparable efficacy to ciprofloxacin. Molecular docking studies revealed strong interactions of these compounds with bacterial enzymes, supporting the in vitro results and highlighting their potential as protein-inhibitor candidates.</p><p><strong>Conclusion: </strong>The novel hybrid derivatives demonstrated significant antibacterial activities, suggesting their potential as promising therapeutic agents. Their effectiveness against various bacterial strains indicated that these compounds could serve as a foundation for the development of new antibacterial drugs. Further research and optimization are needed to enhance their potency and ensure their safety, paving the way for future clinical applications.</p>","PeriodicalId":11076,"journal":{"name":"Current topics in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":2.9,"publicationDate":"2025-01-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143001816","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":"Osseointegration Process Improving via Functionalization of Titanium Dioxide Nanotubes: A Bibliometric Analysis and Systematic Review.","authors":"Sergio Murilo da Silva Braga Martins Junior, Jose Manuel Noguera Bazan, Lucas Dos Santos Silva, Luis Claudio Nascimento da Silva","doi":"10.2174/0115680266334190241213101547","DOIUrl":"https://doi.org/10.2174/0115680266334190241213101547","url":null,"abstract":"<p><strong>Introduction/objectives: </strong>Failures of osseointegrated implants pose a significant challenge in the medical field, often attributed to prolonged osseointegration periods and bacterial infections. Functionalization of Titanium Dioxide Nanotubes (TNTs) has emerged as a promising strategy to improve osseointegration and mitigate infections. This study aims to conduct a bibliometric analysis and systematic review to identify trends, gaps, and advancements in research on the functionalization of TNTs for osseointegration improvement.</p><p><strong>Methods: </strong>Articles were retrieved from the Web of Science database using the keywords \"osseointegration,\" \"titanium dioxide nanotubes,\" and \"functionalization.\" The inclusion criteria were studies published between 2014 and 2023, written in English, and focusing on the use of TNTs in implant surface modifications. A total of 126 articles were included after screening. Data extraction and analysis were performed using VOS Viewer, Microsoft Excel, and GraphPad Prism.</p><p><strong>Results: </strong>The review revealed a growing number of publications on TNT functionalization, with China, the United States, and Brazil leading in contributions. Key findings include the effectiveness of TNTs loaded with bioactive agents (e.g., silver, strontium, hydroxyapatite) in promoting osseointegration and antibacterial activity. Collaborative networks among institutions and authors were mapped, highlighting the Sao Paulo State University and Yong Huang as the most prolific contributors.</p><p><strong>Conclusion: </strong>The findings underscore the potential of TNT functionalization to enhance implant performance. However, a gap remains in translating preclinical findings into clinical trials. Future research should focus on clinical validation to bridge this gap and translate laboratory advancements into therapeutic solutions.</p>","PeriodicalId":11076,"journal":{"name":"Current topics in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":2.9,"publicationDate":"2025-01-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143022627","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":"SRT1720 Treatments Hepatic Ischemia Reperfusion Injury by Regulation of NF-κB Signaling Pathways and Reduce Cell Apoptosis: From Network Pharmacology to Experimental Validation.","authors":"Zhongzhe Li, Wenting Geng, Beilei Yu, Bin Wang, Shuxuan Sun, Lu Zhou","doi":"10.2174/0115680266322450241212070042","DOIUrl":"https://doi.org/10.2174/0115680266322450241212070042","url":null,"abstract":"<p><strong>Background and objective: </strong>Hepatic ischemia reperfusion injury (HIRI) is a common complication closely related to the prognosis of liver surgery, and effective treatment methods are still unavailable. SRT1720 has the characteristics of multifunction and multitarget which may cope with the multidirectional complex pathological process caused by HIRI. The present study aimed to explore the potential mechanism of SRT1720 in HIRI through a combination of network pharmacology, in vitro experiments and in vivo models.</p><p><strong>Methods: </strong>Differentially expressed genes (DEGs) were identified based on the GSE15480 and Genecards database. Enrichment analyses were then conducted. SRT1720-targeted genes were obtained through databases such as Chembl, TTD, GtoPdb, and so on. All target genes were standardized by the Uniprot database and the Kyoto Encyclopedia of Genes and Genomes (KEGG) pathways were identified by STRING. Shared KEGG pathways were identified using a Venn diagram among SRT1720-targeted pathways and HIRI. Furthermore, experimental techniques such as cell apoptosis assay and western blotting were used to confirm the most significant biological processes and the key pathway between SRT1720-targeted and HIRI.</p><p><strong>Results: </strong>This study identified 118 HIRI-related DEGs, 69 shared KEGG pathways of SRT1720 and HIRI. In addition, the findings revealed that SRT1720 significantly reduced liver ischemiareperfusion (I/R) injury. NF-κB signaling pathway and the expression of promoting apoptosis factors such as Bax and Caspase3 were inhibited, while antiapoptotic protein Bcl-2 was promoted in the SRT1720 group compared with the I/R group.</p><p><strong>Conclusion: </strong>The findings indicate that SRT1720 may inhibit the development of HIRI by inhibiting the NF-κB signaling pathway and reducing cell apoptosis, acting as a treatment for HIRI.</p>","PeriodicalId":11076,"journal":{"name":"Current topics in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":2.9,"publicationDate":"2025-01-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143022635","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":"Advances in the Study of Halogenated Natural Products.","authors":"Lijing Zhang, Bing Liu, Ting Zhu, Xue Tian, Ning Chen, Yuxin Wang","doi":"10.2174/0115680266344796241211214414","DOIUrl":"https://doi.org/10.2174/0115680266344796241211214414","url":null,"abstract":"<p><p>Halogenated natural products are an important class of secondary metabolites that are widely distributed in nature. The presence of halogen atoms usually enhances the pharmacological activity of the compounds. As a result, halogenated natural products have shown promising pharmacological activities in antibacterial, antitumour, anti-inflammatory and antiplasmodial properties, providing a rich resource for the development of new drugs. To date, more than 62% of halogenated compounds are produced by marine organisms, mainly including marine sponges, algae, corals, fungi and other organisms. In addition, terrestrial microorganisms, including bacteria and fungi, also produce halogenated metabolites, which are equally important sources of halogenated natural products. The biosynthesis of halogenated natural products involves the synergistic action of multiple enzymes that efficiently and selectively bind halogen atoms to organic molecules, a process that enhances the biological activity of the compounds. Halogenated natural products have a wide range of uses as important raw materials in the agricultural, pharmaceutical and chemical industries. This paper reviews the progress of research on halogenated compounds and their biosynthesis in recent years, laying the foundation for further utilisation and development of halogenated compounds.</p>","PeriodicalId":11076,"journal":{"name":"Current topics in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":2.9,"publicationDate":"2025-01-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143022625","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}