Medicinal ChemistryPub Date : 2025-10-08DOI: 10.2174/0115734064409397250925105306
Hui Zhao, Yunwen Wang, Huihui Yan, Yanzhen Yu, Lei Xu, Rong Sheng
{"title":"Virtual Screening of HBV Capsid Assembly Modulators with the Combination of Pharmacophore Modeling and Hydrogen Bond Constraints.","authors":"Hui Zhao, Yunwen Wang, Huihui Yan, Yanzhen Yu, Lei Xu, Rong Sheng","doi":"10.2174/0115734064409397250925105306","DOIUrl":"https://doi.org/10.2174/0115734064409397250925105306","url":null,"abstract":"<p><strong>Introduction: </strong>Hepatitis B virus (HBV) infection remains a significant public health challenge. Targeting HBV capsid assembly has the potential to achieve a functional cure for HBV infection, and the capsid assembly modulators (CAMs) have been regarded as promising therapeutic agents for HBV. In this work, we aimed to identify novel scaffold HBV CAMs through a multi-step virtual screening approach.</p><p><strong>Methods: </strong>Pharmacophore-based virtual screening combined with hydrogen bond constraints was performed on the Specs and ChemDiv databases. Potential modulators were screened using qPCR (quantitative PCR) and CCK-8 assays. Molecular dynamics (MD) simulations and ADMET (absorption, distribution, metabolism, excretion, and toxicity) analysis were employed to evaluate ligand-protein binding modes and pharmacokinetic properties.</p><p><strong>Results: </strong>Twenty-one compounds were selected as potential HBV CAMs. Compounds B5, B19, and B21 exhibited excellent anti-HBV activity, with EC50 values of 1.74, 4.29, and 0.38 μM, respectively. MD simulations revealed their possible binding modes with the HBV core protein, confirming the critical role of Trp102-mediated hydrogen bonds.</p><p><strong>Discussion: </strong>Hydrogen bonds are critical for establishing stable and high-affinity interactions between small molecules and targets. Three compounds, B5, B19, and B21, were identified as novel scaffold hits of CAMs through virtual screening with the combination of pharmacophore modeling and hydrogen bond constraints. MD simulations illustrated the critical contributions by Trp102, providing valuable insights for further structural optimization.</p><p><strong>Conclusion: </strong>Compounds B5, B19, and B21 can serve as promising starting points for the development of more potent anti-HBV candidates through future hit-to-lead optimization.</p>","PeriodicalId":18382,"journal":{"name":"Medicinal Chemistry","volume":" ","pages":""},"PeriodicalIF":2.6,"publicationDate":"2025-10-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145292712","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":"Stereoisomerism in Chemistry and Drug Development: Optical, Geometrical, and Conformational Isomers.","authors":"Shivani Chawla, Rishikesh Gupta, Sudhanshu Kumar Jha, Shamim, Sarfraj Kashid, Keshav Taruneshwar Jha","doi":"10.2174/0115734064366389250923044201","DOIUrl":"https://doi.org/10.2174/0115734064366389250923044201","url":null,"abstract":"<p><p>Stereoisomerism in addition to conformational, geometrical, and optical isomerism, has considerable effects on the stability, reactivity, and functioning of molecules. Therefore, the objective of this article is to review the recent developments and research on stereoisomerism, including its consequences in various branches of science. The energetics and stability of conformational isomerism, which depict the concept of cis-trans and E/Z configurations of geometric isomerism, elucidate the molecular behavior and the efficacy of drugs, also discussed. The consequence of stereochemistry on pharmacology and drug design is elucidated by optical isomerism in terms of chirality and enantiomorphic effects. To exemplify the use of stereoisomerism in drug development, this review, offers wide case studies of NSAIDs, anticancer drugs, and antibiotic drugs. In this Article, the phenomenon of stereoisomerism is also primarily discussed concerning biomolecules such as proteins, carbohydrates, lipids, and nucleic acids. Recent advances in comparison operations include computer-aided drug design, advances in personalized medicine, and new therapies such as DNA and peptide drugs, including their possible impacts on the business and natural world. The primary aim of the review is to thoroughly investigate and examine stereoisomerism and its wide-ranging implications.</p>","PeriodicalId":18382,"journal":{"name":"Medicinal Chemistry","volume":" ","pages":""},"PeriodicalIF":2.6,"publicationDate":"2025-10-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145232956","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}
Medicinal ChemistryPub Date : 2025-09-17DOI: 10.2174/0115734064390136250818063436
Eya Caridad Rodríguez-Pupo, Timoteo Delgado-Maldonado, Diana V Navarrete-Carriola, Lenci K Vázquez-Jiménez, Eyra Ortiz-Perez, Alma D Paz-González, Ignacio Martinez, Bertha Espinoza, Gildardo Rivera
{"title":"<i>In Vitro</i> Evaluation of <i>p</i>-Toluenesulfonyl Hydrazones as Anti-<i>Trypanosoma cruzi</i> and Leishmanicidal Agents.","authors":"Eya Caridad Rodríguez-Pupo, Timoteo Delgado-Maldonado, Diana V Navarrete-Carriola, Lenci K Vázquez-Jiménez, Eyra Ortiz-Perez, Alma D Paz-González, Ignacio Martinez, Bertha Espinoza, Gildardo Rivera","doi":"10.2174/0115734064390136250818063436","DOIUrl":"10.2174/0115734064390136250818063436","url":null,"abstract":"<p><strong>Introduction: </strong>Neglected tropical diseases (NTDs), such as Chagas disease (CD) and Cutaneous Leishmaniasis (CL), are significant global health concerns. The limited number of treatments and their severe adverse effects worsen the situation. Therefore, the development of molecules as a new pharmacological alternative is necessary. This work aimed to obtain new p- Toluenesulfonyl hydrazones derivatives to determine their potential antiparasitic activity against <i>Trypanosoma cruzi (T. cruzi)</i> and <i>Leishmania mexicana (L. mexicana)</i>.</p><p><strong>Methods: </strong>Compounds were synthesized by condensing p-Toluenesulfonyl hydrazide with aromatic aldehydes using acetic acid as a catalyst. All compounds were structurally elucidated using infrared (IR) spectroscopy, proton and carbon nuclear magnetic resonance (¹H and ¹³C NMR), and Ultra-Performance Liquid Chromatography-tandem Mass Spectrometry (UPLCMS). The Queretaro (Qro) strain of <i>T. cruzi</i> and the M379 strain of <i>L. mexicana</i> were used for <i>in vitro</i> assays.</p><p><strong>Results: </strong>Compound pT-21 (IC<sub>50</sub>= 49.6 μM) was the most active agent against the <i>T. cruzi</i> Qro strain. Meanwhile, compounds pT-15 and pT-21 inhibited the proliferation of <i>L. mexicana</i> promastigotes with an IC<sub>50</sub> value of 59.2 and 13.8 μM, respectively. In addition, these compounds had low cytotoxic effects against Vero cell lines (CC<sub>50</sub> values >100 μM).</p><p><strong>Discussion: </strong>In this study, compound pT-21 inhibited the proliferation of <i>T. cruzi</i> and <i>L. mexicana in vitro</i>. Its activity is attributed to the reactivity of the 5-nitrofuran ring (present in other drugs such as nifurtimox). Future research could focus on identifying the pharmacological target of compound pT-21 to facilitate rational drug design and enhance its potency against these parasites.</p><p><strong>Conclusion: </strong>In summary, these results show that p-Toluenesulfonyl hydrazones serve as a scaffold to aid in the development of potent and selective agents against <i>T. cruzi</i> and <i>L. mexicana</i>.</p>","PeriodicalId":18382,"journal":{"name":"Medicinal Chemistry","volume":" ","pages":""},"PeriodicalIF":2.5,"publicationDate":"2025-09-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145086467","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}
Medicinal ChemistryPub Date : 2025-09-09DOI: 10.2174/0115734064398347250815061230
Abrar Hussain, Sayeda Sania Seher, Shahzaib Akhter, Khurram Shahzad, Muhammad Arfan, Kyong-Cheol Ko, Sang Hyun Park
{"title":"Recent Advances in the Biological Profiles of Fluorine-Containing Pyridine and its Derivatives: A Brief Overview.","authors":"Abrar Hussain, Sayeda Sania Seher, Shahzaib Akhter, Khurram Shahzad, Muhammad Arfan, Kyong-Cheol Ko, Sang Hyun Park","doi":"10.2174/0115734064398347250815061230","DOIUrl":"https://doi.org/10.2174/0115734064398347250815061230","url":null,"abstract":"<p><p>Fluorine-containing pyridine derivatives have emerged as pivotal structures in modern drug discovery due to their unique physicochemical properties and diverse pharmacological activities. The incorporation of fluorine into pyridine-based scaffolds enhances drug potency, selectivity, metabolic stability, and Pharmacokinetics (PK) of these compounds, making them highly attractive for therapeutic development. These derivatives have been integrated into numerous Food and Drug Administration (FDA)-approved drugs, underscoring their importance in medicinal chemistry. This review systematically compiles recent advances in the pharmacological applications of fluorine-containing pyridine derivatives, focusing on their anticancer, antidiabetic, antioxidant, and anti-Alzheimer's activities. By exploring the Structure-Activity Relationship (SAR) and mechanisms of action, this review provides valuable insights for the design and development of novel biologically active compounds. This comprehensive analysis aims to inspire new directions in drug discovery and highlight the therapeutic potential of fluorine- containing pyridine derivatives.</p>","PeriodicalId":18382,"journal":{"name":"Medicinal Chemistry","volume":" ","pages":""},"PeriodicalIF":2.6,"publicationDate":"2025-09-09","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145065150","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}
Medicinal ChemistryPub Date : 2025-09-01DOI: 10.2174/0115734064381790250722071316
Panagiotis Theodosis-Nobelos, Eleni A Rekka
{"title":"Pluripotent Cinnamic Acid and Valproic Acid Hybrid Molecules Designed as Strong Anti-inflammatory and Anti-hyperlipidemic Compounds.","authors":"Panagiotis Theodosis-Nobelos, Eleni A Rekka","doi":"10.2174/0115734064381790250722071316","DOIUrl":"https://doi.org/10.2174/0115734064381790250722071316","url":null,"abstract":"<p><strong>Introduction: </strong>Inflammation and oxidative stress are considered main pathophysiological factors for neuronal and cardiovascular diseases, also leading to the impairment of main cellular metabolic pathways. Promotion of hyperlipidemia is also the result of inflammatory and oxidative (ROS production) processes. Additionally, compounds of medicinal interest like valproic and caffeic acids and amino acids like proline and tyrosine have shown antiinflammatory and cellular protective potency.</p><p><strong>Methods: </strong>In the present study, amides of L-tyrosine, L-proline, and L-cysteine, and an ester of cinnamyl alcohol were synthesized by conjugation with caffeic acid, valproic acid, or (E)-3- (3,4-dimethoxyphenyl)acrylic acid (cinnamic acid derivative). This design aimed to explore the multiple activities of novel compounds, via the combination of structures related to the desired biological characteristics. The synthesized compounds were tested for their effects on oxidative stress in vitro and on acute inflammation and hyperlipidemia in vivo.</p><p><strong>Results: </strong>The synthesized compounds decreased carrageenan-induced rat paw oedema up to 69% (the most active compound 6), and 49% for compound 2, an amide of valproic acid with L-tyrosine. Several compounds were effective antioxidants, with radical scavenging and lipid peroxidation inhibitory activity. Additionally, the synthesized molecules significantly decreased the plasma lipidemic markers in tyloxapol-induced hyperlipidemic rats. They decreased plasma triglycerides and total cholesterol up to 53% and 78% (compound 1), and LDL-cholesterol up to 69% (compound 5).</p><p><strong>Discussion: </strong>The anti-inflammatory activity of the derivatives was equal to or much higher than that of ibuprofen and tolfenamic acid, two widely applied NSAIDs (nonsteroidal antiinflammatory drugs), whilst compound 2 was 3.3 times more active than valproic acid, with the latter being tested at four times higher dose. Concerning the antioxidant activity, several compounds were comparable to the strong antioxidant Trolox, and the effect on cholesterol levels for all the derivatives was comparable to or equal to simvastatin [a 3-hydroxy-3-methylglutaryl (HMG) coenzyme A reductase inhibitor].</p><p><strong>Conclusion: </strong>The multiple activities of the synthesized compounds may serve for the manipulation of conditions involving inflammation and lipid deregulation, or the further optimization and production of compounds towards these ailments.</p>","PeriodicalId":18382,"journal":{"name":"Medicinal Chemistry","volume":" ","pages":""},"PeriodicalIF":2.6,"publicationDate":"2025-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145000927","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 Medicinal Chemistry of Fused and Substituted Piperazines: Unlocking their Potential as Anticancer Agents.","authors":"Saumya Singh, Rajnish Kumar, Shrishti Tripathi, Salahuddin, Avijit Mazumder","doi":"10.2174/0115734064383459250806115629","DOIUrl":"https://doi.org/10.2174/0115734064383459250806115629","url":null,"abstract":"<p><p>Cancer is an abnormal growth of normal cells and has become a global healthcare concern. The availability of safer anticancer drugs with exceptional selectivity for healthy cells and high efficacy against various forms of cancer remains a significant challenge. Therefore, there is a need to develop target-specific and safer anticancer drugs. In medicinal chemistry, heterocyclic compounds play a crucial role by exhibiting diverse biological activities. Specifically, nitrogen-containing heterocyclic compounds are widely studied due to their diverse activities. The piperazine moiety serves as the building block for several molecules and is reported to have the ability to inhibit the cell cycle (G1/S phase), suppress angiogenesis, and interact with DNA. Piperazine also exhibits a flexible binding feature that enables it to interact with a range of biological targets, making it effective against various types of cancer. As there is a continuous need for an anticancer drug with improved efficacy and fewer side effects, piperazine derivatives are attracting the attention of researchers. This review highlights recent methods for the synthesis of fused and substituted piperazines, their structure-activity relationships, and their interactions with biological targets or receptors as anticancer agents. Thus, the presented review will be helpful to medicinal chemists in designing anticancer molecules that incorporate piperazines.</p>","PeriodicalId":18382,"journal":{"name":"Medicinal Chemistry","volume":" ","pages":""},"PeriodicalIF":2.6,"publicationDate":"2025-08-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144959510","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}
Medicinal ChemistryPub Date : 2025-08-22DOI: 10.2174/0115734064389466250805052834
Mahalakshmi C S Parepalli, Rajitha Galla
{"title":"Design, Synthesis, Biological Evaluation, and <i>In Silico</i> Studies of Tetrazole Derivatives as Potential Cytotoxic Agents.","authors":"Mahalakshmi C S Parepalli, Rajitha Galla","doi":"10.2174/0115734064389466250805052834","DOIUrl":"https://doi.org/10.2174/0115734064389466250805052834","url":null,"abstract":"<p><strong>Introduction: </strong>Despite significant progress in cancer treatment, the need for new anticancer agents remains critical. Current research efforts are directed toward discovering novel compounds that exhibit potent cytotoxic activity while minimizing adverse effects. Thus, tetrazole derivatives have gained attention due to their potential biological activities, including anticancer effects.</p><p><strong>Methods: </strong>A series of tetrazole derivatives (6a-l) were synthesized via α-keto halogenation of 2,4-difluoroacetophenone, followed by cyclization, nucleophilic substitution, and subsequent coupling with various aryl carboxylic acids. The synthesized compounds were characterized using spectroscopic techniques, including <sup>13</sup>C NMR, <sup>1</sup>H NMR, FT-IR, and HRMS. Their cytotoxic potential was assessed through an MTT assay across four human cancer cell lines. Other cytotoxic evaluations included apoptosis induction, cell cycle analysis, and EGFR-TK inhibition assays. Additionally, molecular docking studies were conducted to explore binding interactions, and in silico ADME predictions were performed to assess pharmacokinetic properties.</p><p><strong>Results: </strong>The results obtained by the MTT assay indicated that compound 6d demonstrated significant cytotoxicity against A549 (lung cancer) cell lines, with an IC50 value of 2.74 μM, compared to doxorubicin (IC<sub>50</sub> = 3.87 μM). Furthermore, cell cycle analysis and apoptosis suggested that 6d arrested the cell cycle in the S phase and triggered apoptosis in A549 cells. Docking studies and EGFR-TK inhibition assay proposed that 6l had good binding affinity towards EGFR enzyme and acts as a potential inhibitor (IC<sub>50</sub> 0.099 μM). The ADME analysis demonstrated favourable molecular properties, including acceptable lipophilicity, strong absorption, and high oral bioavailability.</p><p><strong>Discussion: </strong>The synthesized tetrazole derivatives exhibited notable anticancer potential, with compound 6d inducing S-phase arrest and apoptosis in lung cancer cells, and 6l demonstrating strong EGFR inhibition. These biological effects were further supported by docking studies and favorable ADME profiles, providing mechanistic insight into their activity.</p><p><strong>Conclusion: </strong>These findings indicate that the synthesized derivatives offer a promising approach for developing innovative and effective cancer therapies.</p>","PeriodicalId":18382,"journal":{"name":"Medicinal Chemistry","volume":" ","pages":""},"PeriodicalIF":2.6,"publicationDate":"2025-08-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144959559","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}
Medicinal ChemistryPub Date : 2025-07-24DOI: 10.2174/0115734064300135250707043513
Shivangi Sharma
{"title":"Blueberries and Their Polyphenols: A Review of the Evidence and the Potential Impact on Inflammation, Oxidative Stress, Vascular and Cardiometabolic Function.","authors":"Shivangi Sharma","doi":"10.2174/0115734064300135250707043513","DOIUrl":"https://doi.org/10.2174/0115734064300135250707043513","url":null,"abstract":"<p><p>Blueberries contain a wide range of bioactive compounds, including polyphenols- plant-based chemicals known for their antioxidant and anti-inflammatory properties. Numerous <i>in vitro</i> and animal studies have suggested that these compounds may promote health. However, evidence regarding the effects of blueberries and their bioactive components in humans remains limited. This review focuses on 45 human studies investigating how blueberry consumption may influence markers of inflammation, oxidative stress, vascular function, cardiovascular health, and metabolic outcomes in both healthy and at-risk individuals. While some findings suggest potential benefits, especially for vascular function, more high-quality, well-controlled human trials are needed to confirm these effects. Furthermore, research exploring the relationship between the structure of specific polyphenols and their biological activity is essential for a deeper understanding of the mechanisms behind the reported health benefits.</p>","PeriodicalId":18382,"journal":{"name":"Medicinal Chemistry","volume":" ","pages":""},"PeriodicalIF":2.6,"publicationDate":"2025-07-24","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144742673","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}
Medicinal ChemistryPub Date : 2025-07-24DOI: 10.2174/0115734064389091250719051643
Navin Kumar Tailor
{"title":"Unlocking the Multifunctional Therapeutic Potential of Herbacetin: A Flavone derived Scaffold.","authors":"Navin Kumar Tailor","doi":"10.2174/0115734064389091250719051643","DOIUrl":"https://doi.org/10.2174/0115734064389091250719051643","url":null,"abstract":"<p><p>Herbacetin (HBT), a naturally occurring flavone, exhibits broad therapeutic -- potential, including anti-cancer, anti-inflammatory, antioxidant, antimicrobial, neuroprotective, and anti-diabetic effects, by modulating key signaling pathways such as NF-κB, PI3K/AKT, AP-1, SGK1/FoxO1, AMPK, SIRT1, MMP9, and NLRP3. It also inhibits several critical enzymes, including ornithine decarboxylase, ATP-citrate lyase, SGK1, AChE, α-glucosidase, and CYP3A4. In the context of cancer, HBT has shown particularly promising activity against breast cancer, liver carcinoma, human colon cancer, and epidermal carcinoma. Structurally, HBT shares significant similarity with well-known flavonoids such as quercetin and kaempferol, and the availability of established total synthetic methodologies makes it an attractive candidate for synthetic chemists. However, the structural modification and comprehensive evaluation of ' 'HBT's biological activity remain underexplored. This review highlights its isolation, total synthesis, pharmacological properties, molecular targets, and future directions, emphasizing the versatility of the HBT scaffold as a promising foundation for the development of novel therapeutic agents.</p>","PeriodicalId":18382,"journal":{"name":"Medicinal Chemistry","volume":" ","pages":""},"PeriodicalIF":2.6,"publicationDate":"2025-07-24","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144742674","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}
Medicinal ChemistryPub Date : 2025-07-22DOI: 10.2174/0115734064388263250710083810
Faris J Tayeb, Mohammed Fareed Felemban, Amal Adnan Ashour, Alaa Shafie
{"title":"Chitosan-Based Materials: A Comprehensive Review on Anticancer Drug Development.","authors":"Faris J Tayeb, Mohammed Fareed Felemban, Amal Adnan Ashour, Alaa Shafie","doi":"10.2174/0115734064388263250710083810","DOIUrl":"https://doi.org/10.2174/0115734064388263250710083810","url":null,"abstract":"<p><p>Cancer remains one of the most formidable global health threats, responsible for millions of deaths annually due to the uncontrolled proliferation and spread of abnormal cells. The development of effective anticancer therapies is crucial, as anticancer drugs target key cellular mechanisms, including DNA replication, apoptosis, and essential signaling pathways. In this context, chitosan (CT) has emerged as a promising biomaterial for advancing cancer treatment. With its unique combination of biocompatibility, biodegradability, and versatility, CT is gaining significant attention as a platform for developing innovative drug delivery systems. Recent research has highlighted the potential of CT-based materials to enhance drug efficacy by enabling controlled release, improving bioavailability, and facilitating targeted tumor delivery. Further modifications to CT, such as carboxymethylation, sulfation, and graft copolymerization, have significantly expanded its application in cancer therapy, allowing for more efficient encapsulation of chemotherapeutic agents, reducing systemic toxicity, and combating multidrug resistance. This review focuses on the latest developments (2021-2024) in CT-based materials for anticancer drug delivery, exploring their design principles, therapeutic mechanisms, and clinical applications. Additionally, the review discusses the challenges faced in translating these promising systems to clinical practice and highlights future strategies for optimizing CT-based therapies to revolutionize cancer treatment.</p>","PeriodicalId":18382,"journal":{"name":"Medicinal Chemistry","volume":" ","pages":""},"PeriodicalIF":1.9,"publicationDate":"2025-07-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144690707","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}