Anti-cancer agents in medicinal chemistry最新文献

{"title":"Caffeic Acid Phenethyl Ester (CAPE) Inhibits Hepatocellular Carcinoma Growth and Angiogenesis via Vascular Endothelial Growth Factor Suppression: A Preclinical Evidence.","authors":"Lei Gong, Wenzhen Wang, Zenghua Deng, Nan Luo, Jirun Peng","doi":"10.2174/0118715206436841260123054356","DOIUrl":"https://doi.org/10.2174/0118715206436841260123054356","url":null,"abstract":"<p><strong>Introduction: </strong>Caffeic acid phenethyl ester (CAPE), a natural compound, has shown antitumor potential, but its efficacy and mechanism in hepatocellular carcinoma (HCC) require further validation, particularly in vivo. This study systematically investigated the antitumor efficacy and safety profile of CAPE against HCC through comprehensive in vitro and in vivo experiments.</p><p><strong>Methods: </strong>In vitro, the anti-proliferative effect of CAPE (0-160 μM) on the human HCC cell line Bel-7402 was evaluated using the CCK-8 assay. The anti-angiogenic potential was assessed by measuring the migration of human umbilical vein endothelial cells (HUVECs) using a Transwell assay and by quantifying Vascular Endothelial Growth Factor (VEGF) secretion via enzyme-linked immunosorbent assay (ELISA). In vivo, a subcutaneous xenograft model using Bel-7402 cells in BALB/c nude mice was established. Mice were randomized to receive vehicle or CAPE (10 mg/kg/day) for 4 weeks. Tumor growth was monitored, and microvessel density (MVD) in tumor tissues was quantified by Factor VIII immunohistochemistry. An acute toxicity study was conducted in healthy Kunming mice with a single high dose (5 g/kg) of CAPE.</p><p><strong>Results: </strong>CAPE exhibited significant anti-proliferative effects on Bel-7402 cells (IC50 = 17.6 μM) and inhibited HUVECs in a dose-dependent manner. In the xenograft model, CAPE suppressed tumor growth. CAPE demonstrated no acute toxicity in mice, suggesting preliminary safety for further investigation. Furthermore, it inhibited angiogenesis in vivo, impeded MVD in HCC specimens, and decreased VEGF secretion.</p><p><strong>Discussion: </strong>This preclinical study provides evidence that CAPE exerts antitumor effects against HCC by inhibiting cell proliferation and suppressing angiogenesis.</p><p><strong>Conclusion: </strong>These findings, coupled with a good preliminary safety profile, support CAPE as a promising candidate for further mechanistic investigation and development in HCC therapy.</p>","PeriodicalId":7934,"journal":{"name":"Anti-cancer agents in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":3.0,"publicationDate":"2026-04-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147832782","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":"The Emerging Role of Histone Methyltransferase ASH1L in Tumor Development.","authors":"Xiang-Yu Zhang, Yue Li","doi":"10.2174/0118715206410039251203071353","DOIUrl":"https://doi.org/10.2174/0118715206410039251203071353","url":null,"abstract":"<p><p>Histone modifications play a fundamental role in epigenetic regulation. Histone methylation mediated by enzymes like absent, small, or homeotic discs 1-like (ASH1L) has emerged as a critical process in normal cellular function and disease, particularly cancer. ASH1L, a member of the Trithorax-group (TrxG) protein family, acts as a histone methyltransferase with the ability to establish H3K36 dimethylation (H3K36me2). In recent years, an increasing number of studies have focused on the dysregulation of ASH1L in various tumors and its potential as a therapeutic target. A detailed literature survey was conducted to compile data from PubMed, SciFinder, and ScienceDirect. After screening, data extraction, and descriptive analysis, a series of related articles was retained. This comprehensive review systematically dissects the molecular mechanisms by which ASH1L modulates oncogenic processes in these cancers, emphasizing its roles in transcriptional activation of driver genes, epigenetic reprogramming, cell cycle progression, and maintenance of cancer stem cell properties. Additionally, we summarize current progress in targeting ASH1L for cancer therapy, highlighting challenges and future directions. ASH1L, as a histone methyltransferase, is associated with the tumor microenvironment, and its anti-tumor targeted therapies require further exploration in the future.</p>","PeriodicalId":7934,"journal":{"name":"Anti-cancer agents in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":3.0,"publicationDate":"2026-04-24","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147832800","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":"Chitosan-Graphene Composite for Drug Delivery in Cancer Therapy: Recent Progress and Advances.","authors":"Negar Lari Lavasani, Mohammad Hossein Roozbahani, Seyed Morteza Naghib","doi":"10.2174/0118715206393479251124110518","DOIUrl":"https://doi.org/10.2174/0118715206393479251124110518","url":null,"abstract":"<p><p>This review focuses on anticancer drug delivery systems using graphene/chitosan (CS) nanocomposites, and the present discussion explores the potential of chitosan/graphene oxide composites and their applications in wound dressings and drug delivery systems, particularly in cancer therapy. Graphene/chitosan-based drug delivery is gaining popularity due to its unique physical, chemical, and electrical properties, improving drug efficacy. The inherent biodegradability, non-toxicity, and antibacterial properties of chitosan make it a highly promising biopolymer for therapeutic interventions. Researchers have also identified graphene oxide as a non-toxic, cost-effective, and biocompatible material suitable for a diverse range of applications. Therefore, here we will examine the reasons for their use in drug delivery, especially in cancer. In addition, we will also study the combination of these two excellent materials. The combination of chitosan (CS) and graphene is currently under investigation for its enhanced therapeutic benefits.</p>","PeriodicalId":7934,"journal":{"name":"Anti-cancer agents in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":3.0,"publicationDate":"2026-04-24","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147832749","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":"Fungal β-D-Glucans: Versatile Agents in Immune Modulation, Tumor Suppression, and Nanomedicine Advances.","authors":"Ao Jin, Yicheng Peng, Dianqi Zhang, XinYi Zhou, Yaoxiang Sun, Xiang Chen","doi":"10.2174/0118715206435063260413064006","DOIUrl":"https://doi.org/10.2174/0118715206435063260413064006","url":null,"abstract":"<p><strong>Introduction/objective: </strong>β-D-Glucans, natural polysaccharides abundant in fungal cell walls, have emerged as promising immunomodulatory and antitumor biomaterials due to their unique triple-helix structure and excellent biocompatibility. Their structural versatility-defined by β-1,3/1,6-glycosidic linkages, branching patterns, and conformational transitions-enables precise optimization for targeted cancer therapy, overcoming the limitations of conventional chemotherapeutics. This article provides a comprehensive review of the structural characteristics, preparation methodologies, pharmacological functions, and underlying mechanisms of fungal β-D-glucans.</p><p><strong>Methods: </strong>A systematic review of peer-reviewed literature was conducted to delineate the structure-activity relationships of fungal β-D-glucans, with a focus on extraction methodologies, antitumor mechanisms, and nanodrug delivery applications.</p><p><strong>Results: </strong>β-D-glucans exhibit dual antitumor efficacy: (1) Direct tumoricidal effects via induction of G1/S-phase cell cycle arrest, suppression of metastasis, and oxidative stress-mediated apoptosis; (2) Immunomodulatory effects by reprogramming Tumor-Associated Macrophages (TAMs) and exerting synergistic effects with Immune Checkpoint Inhibitors (ICIs). Nano-formulations based on β-D-glucans improve targeted delivery efficiency and overcome bioavailability barriers, achieving a 3-fold higher tumor accumulation than free drugs in murine models.</p><p><strong>Discussion: </strong>Fungal β-D-glucans represent a promising therapeutic platform that integrates direct tumor cytotoxicity and immune activation for next-generation cancer treatment. Although the safety and regulatory framework for glucan-based nanomedicines is still evolving, it is imperative to prioritize the clinical development of nanoparticle- based glucan delivery systems and explore optimized synergistic combination strategies to address the key challenges of tumor heterogeneity and drug resistance.</p><p><strong>Conclusion: </strong>The unique triple-helix structure renders them excellent nanocarriers to enhance targeted drug delivery and combination therapeutic efficacy. The current clinical translation of fungal β-D-glucans is limited by the lack of standardized extraction protocols, structural variation across different fungal sources, and insufficient safety evaluation. Future research should focus on optimizing the oral delivery system of β-D-glucans and developing novel combination strategies to overcome drug resistance and accelerate their clinical translation.</p>","PeriodicalId":7934,"journal":{"name":"Anti-cancer agents in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":3.0,"publicationDate":"2026-04-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147721637","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":"Hyperthermia of MCF-7 under Near Infrared Radiation in the Presence of PEGylated Graphene Oxide Nanoparticles.","authors":"Maria Denisovna Dolgikh, Maria Stanislavovna Bochkova, Valeria Pavlovna Timganova, Darya Igorevna Usanina, Sergey Stanislavovich Lazarev, Mikhail Borisovich Rayev, Svetlana Anatolyevna Zamorina","doi":"10.2174/0118715206450707260105071412","DOIUrl":"https://doi.org/10.2174/0118715206450707260105071412","url":null,"abstract":"<p><strong>Introduction: </strong>Breast cancer remains a major healthcare challenge due to its high incidence worldwide. Current treatment methods involve invasive surgical procedures, underscoring the urgent need for more effective and less invasive therapies. One promising approach explored in this study is hyperthermia-based treatment of cancer cells using NIR radiation in the presence of PEGylated graphene oxide. This method aims to leverage the photothermal properties of nanoparticles to selectively ablate cancer cells, offering a potential alternative to other therapeutic strategies.</p><p><strong>Methods: </strong>We investigated graphene oxide coated with linear (LP-GO) or branched (BP-GO) polyethylene glycol at concentrations of 5, 25, and 50 μg/mL in combination with NIR radiation. The irradiation was performed twice for 20 minutes. Cell viability, apoptosis, and the number of MCF-7 cells were assessed at 24 and 48 hours post-irradiation using flow cytometry.</p><p><strong>Results: </strong>The research shows that only LP-GO increases the temperature in a dose-dependent manner. The maximum temperature (45.9°C) was recorded at a concentration of 50 μg/mL after the second irradiation. Additionally, LP-GO is sorbed by MCF-7 cells in a dose-dependent manner. Furthermore, when LP-GO was used at concentrations of 25 and 50 μg/mL in combination with NIR irradiation, the maximum antitumor effect was observed after 48 hours, with a general apoptosis rate of 30%.</p><p><strong>Discussion: </strong>We observed that after NIR irradiation of MCF-7 cells, early apoptosis was induced. According to the literature, this effect may be associated with increased levels of pro-apoptotic proteins and pro-inflammatory cytokines. In addition, apoptosis is known to be triggered after photothermal/photodynamic therapy by increasing the amount of ROS, caspase 8/9 activation, as well as caspase 3/7 and cytochrome c protein. At the same time, we did not observe a great increase in apoptosis, which may be due to the fact that hyperthermia is able to increase the expression of heat shock genes, in particular HSP70, HSP90, and HSP27, HSPВ1, which protect the cell from the negative influence of IR rays.</p><p><strong>Conclusion: </strong>This study demonstrates that LP-GO effectively induces hyperthermia in MCF-7 cells in a concentration- dependent manner, resulting in an increased percentage of apoptotic cells. Therefore, the combination of LP-GO with NIR irradiation shows promise as a hyperthermia-based therapeutic approach for breast cancer treatment.</p>","PeriodicalId":7934,"journal":{"name":"Anti-cancer agents in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":3.0,"publicationDate":"2026-04-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147721614","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":"Qualitative Analysis and Cytotoxic Activity of Ethanolic Extract of Piper betle Linn. Leaves: Induction of Apoptosis, Cell Cycle Arrest, and Caspase-3/7 Activation in HER2+ AU565 Breast Cancer Cell Line.","authors":"Sharmeen Fayyaz, Atia Tul-Wahab, Rimsha Irshad, Maria Mir, Naveera Zafar, Humaira Zafar, M Iqbal Choudhary","doi":"10.2174/0118715206382374250831130527","DOIUrl":"https://doi.org/10.2174/0118715206382374250831130527","url":null,"abstract":"<p><strong>Introduction: </strong>Piper betle, or betel vine, is a common chewing plant used for recreational purposes. Recently, there has been an increased interest in the cancer chemotherapeutic potential of dietary plants due to their antioxidant, antiinflammatory, and anti-mutagenic actions. While previous studies have demonstrated that P. betle leave extract inhibits the proliferation of breast cancer cells in vitro, the underlying mechanisms of its anti-cancer activity remain poorly understood. In this study, we investigated the effect of P. betle leaf extract on breast cancer cell lines and identified the possible mechanisms involved.</p><p><strong>Methods: </strong>Cell viability was assessed using the MTT assay. Annexin V and caspase-3/7 assays were used to determine apoptosis (programmed cell death). Major bioactive constituents in the extract were identified by using LC-MS and GC-MS techniques.</p><p><strong>Results: </strong>We found that P. betle leaves' extract inhibited the proliferation of all the breast cancer cell lines. Mechanistic analyses revealed that P. betle mediated inhibition of cell growth is a result of cell cycle arrest and DNA fragmentation. Moreover, the expression of apoptotic genes increased, ultimately leading to the activation of caspase-3/7 and cell death. The major compounds identified were hydroxychavicol, methyl palmitate, (E)- methyl octadec-9-enoate, and coniferaldehyde. We therefore speculate that the anti-cancer effect of P. betle is largely dependent on these phytochemicals.</p><p><strong>Discussions: </strong>In line with previously reported studies, our results demonstrate, for the first time, the anti-cancer effect of P. betle extract on the AU565 a HER2+ breast cancer cell line. Together with in silico and mechanistic approaches, we established that major compounds identified in the P. betle extract could be further evaluated as potential lead molecules against breast cancer.</p><p><strong>Conclusion: </strong>In summary, we report here for the first time that P. betle extract inhibits the proliferation of the AU565 (HER2+) breast cancer cell line, which may aid in advancing treatment options, particularly for HER2+ breast cancer.</p>.</p>","PeriodicalId":7934,"journal":{"name":"Anti-cancer agents in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":3.0,"publicationDate":"2026-04-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147721578","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-Silico Identification of Natural Compounds as Dual Inhibitors of Aromatase and CDK4/6: A Multi-Target Approach for ER-Positive Breast Cancer Treatment.","authors":"Priyanka Yadav, V Samuel Raj, Manoj Kumar Yadav","doi":"10.2174/0118715206412723251128073929","DOIUrl":"https://doi.org/10.2174/0118715206412723251128073929","url":null,"abstract":"<p><strong>Introduction: </strong>The diagnosis of Estrogen-positive (ER+) breast cancer remains a major challenge for postmenopausal women. The progression of this disease depends heavily on estrogen signaling, which serves as an essential target for treatment strategies. The progression of the disease and the development of resistance to treatment occur because of abnormalities in the cyclin D1-CDK4/6-Rb pathway, even though aromatase inhibitors are effective.</p><p><strong>Methods: </strong>To identify potential dual inhibitors of aromatase and CDK4/6, 170,269 natural compounds from the Asinex database were screened using multi-target virtual screening. The top hits underwent molecular docking, ADMET profiling, density functional theory (DFT) analysis, 100 ns Molecular Dynamics (MD) simulations, and MM-GBSA binding energy calculations as part of a comprehensive in silico analysis.</p><p><strong>Results: </strong>In the initial phase, 76 aromatase-targeting compounds were screened against CDK4 and CDK6. Two dual-target candidates demonstrated promising potential: LAS52119664 and BBF30702300, which showed aromatase (-8.21 kcal/mol) and CDK4 (-197.87 ± 14.09 kcal/mol) binding, and BBF30702300, which showed aromatase (-6.21 kcal/mol) and CDK6 (-110.58 ± 8.43 kcal/mol) binding.</p><p><strong>Discussion: </strong>The DFT analysis demonstrated that the HOMO-LUMO gaps were 0.184 and 0.181 eV, which indicated high reactivity. Both complexes maintained stability during a 100-nanosecond molecular dynamics simulation, as shown by their steady RMSD and RMSF values. ADMET profiling and in silico toxicity predictions confirmed the drug-like features of these compounds. ER+ breast cancer therapy may benefit from these compounds, which act as dual inhibitors.</p><p><strong>Conclusion: </strong>Both LAS52119664 and BBF30702300 emerged as novel and promising natural dual inhibitors of aromatase and CDK4/6, providing a basis for future experimental validation and the development of multitargeted therapies for ER-positive breast cancer.</p>","PeriodicalId":7934,"journal":{"name":"Anti-cancer agents in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":3.0,"publicationDate":"2026-04-09","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147669778","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":"Targeting the Arachidonic Acid Cascade in Cancer: Recent Advances in Enzyme Inhibitor Design.","authors":"Zorica Vujić, Jelena Savić, Olivera Čudina, Jasmina Brborić, Vladimir Dobričić","doi":"10.2174/0118715206424807251207200409","DOIUrl":"https://doi.org/10.2174/0118715206424807251207200409","url":null,"abstract":"<p><strong>Introduction: </strong>Cancer is a multifactorial disease involving multiple interrelated molecular targets and signaling pathways. Some epidemiological studies have suggested that nonsteroidal anti-inflammatory drugs could reduce the incidence of certain types of cancer, indicating the interplay between inflammation and cancer. Designing compounds that inhibit an enzyme of the arachidonic acid inflammatory cascade while exhibiting anticancer effects has emerged as a promising strategy.</p><p><strong>Methods: </strong>A descriptive review and analysis of recently published studies on the synthesis of compounds that target two enzymes of the arachidonic acid cascade and simultaneously exhibit anticancer activity was performed.</p><p><strong>Results: </strong>Numerous cyclooxygenase-2 (COX-2) inhibitors with anticancer activity are known. Fewer examples exist for 5-lipoxygenase (5-LOX) inhibitors, while many dual COX-2/5-LOX inhibitors also display anticancer effects. Some examples of dual inhibitors with anticancer potential include 5-LOX/microsomal prostaglandin E2 synthase (mPGES), and COX-2/soluble epoxide hydrolase inhibitors. There are also compounds designed to inhibit three targets: COX-2, 15-LOX, and carbonic anhydrase.</p><p><strong>Discussion: </strong>Given the complex interplay between inflammation and cancer, the term \"anticancer effects\" encompasses various therapeutic opportunities, ranging from adjuvant therapy and chemoprevention to angiogenic and cytotoxic activity.</p><p><strong>Conclusion: </strong>This multitarget approach highlights the broad therapeutic possibilities of targeting inflammatory pathways, establishing a direction for the development of innovative anticancer therapies with improved safety profiles.</p>","PeriodicalId":7934,"journal":{"name":"Anti-cancer agents in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":3.0,"publicationDate":"2026-04-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147669828","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":"Recent Advances in Natural Phytocompounds for the Chemotherapeutic Management of Head and Neck Squamous Cell Carcinoma from 2018-2024.","authors":"Zulfa Nooreen, Vinayak Rai, Harshita Sachan, Awani Kumar Rai, Sudeep Tandon","doi":"10.2174/0118715206432579251210114013","DOIUrl":"https://doi.org/10.2174/0118715206432579251210114013","url":null,"abstract":"<p><p>The most prevalent cancers of the head and neck are oral squamous cell carcinomas, which arise from the mucosal epithelium of the oral cavity, throat, and larynx. According to GLOBOCAN, oral squamous cell carcinoma is the sixth most frequent malignancy worldwide and is expected to increase in prevalence by 30% by 2030. A thorough understanding of the underlying molecular processes can lead to novel therapeutic approaches that utilize phytochemicals, either alone or in combination with currently approved medicines, for a range of malignancies. Phytochemicals present in food can influence the antioxidant status of the oral cavity and contribute to its protection. Plant-derived antioxidants, including polyphenols, have been shown to scavenge reactive nitrogen species, chelate ions, and mitigate adverse effects. The mucosal and submucosal compartments are involved in enhanced immune responses, decreased cell proliferation, increased cell death, and diminished regenerative capacity. To effectively prevent and treat oral squamous cell carcinoma, this review summarizes some of the most potent phytochemicals. These compounds can arrest the cell cycle, induce differentiation and apoptosis, inhibit angiogenesis, and suppress the invasive and metastatic properties of cancer cells. Their mechanisms of action include cytochrome-c release, loss of mitochondrial membrane potential, downregulation of antiapoptotic proteins, upregulation of pro-apoptotic proteins, activation of caspases and p53, inhibition of the Akt/mTOR signaling pathway, and modulation of NF-κB, STAT3, and PI3K phosphorylation. Additionally, phytochemicals can reduce the damage caused by radiation and chemotherapy to healthy cells during treatment. This review highlights plant extracts and their bioactive compounds reported for the management of head and neck cancers from 2018 to 2024.</p>","PeriodicalId":7934,"journal":{"name":"Anti-cancer agents in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":3.0,"publicationDate":"2026-04-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147669853","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":"Poly(2-oxazolines) as Precision Nanocarriers in Triple-Negative Breast Cancer: Advancing Targeted Chemotherapy Through Polymeric Innovation.","authors":"Shikha Baghel Chauhan, Chirag Jain, Aniket Yadav, Indu Singh","doi":"10.2174/0118715206432665251204114832","DOIUrl":"https://doi.org/10.2174/0118715206432665251204114832","url":null,"abstract":"<p><strong>Introduction: </strong>Poly(2-ethyl-2-oxazoline) (POx) has emerged as a highly promising drug delivery polymer due to its biocompatibility, stealth-like behavior, and versatile functionalization options. POx-based nanocarriers offer significant advantages for targeted drug delivery in oncology, particularly for challenging tumors such as triple-negative breast cancer (TNBC).</p><p><strong>Methods: </strong>Recent literature from 2015 to 2025 on the synthesis, characterization, and biological applications of POx-based nanocarriers was systematically reviewed. Emphasis was placed on drug conjugation techniques, in vitro and in vivo performance, and computational studies that inform design optimization.</p><p><strong>Results: </strong>POx micelles and hybrid systems demonstrate improved encapsulation efficiency, reduced off-target toxicity, and sustained drug release, achieving effective tumor targeting via the enhanced permeability and retention (EPR) effect. Notably, POx micelles loaded with β-elemene exhibit dual pH/GSH-responsive behavior with >92% encapsulation efficiency. Computational modeling has guided micelle design and predicted critical drug-polymer interactions.</p><p><strong>Discussion: </strong>The structural flexibility of POx enables the engineering of dual-drug carriers and theranostic platforms. Clinical translation is progressing, although challenges remain regarding large-scale synthesis and regulatory standardization. Integration of POx-based systems into combination therapies and personalized oncology strategies represents a promising path forward, supported by encouraging preclinical results.</p><p><strong>Conclusion: </strong>POx nanocarriers exhibit strong translational potential for TNBC due to high drug loading, biocompatibility, and tunable release profiles. They provide enhanced tumor accumulation, active targeting, and the ability to overcome multidrug resistance, supported by favorable pharmacokinetics and computational design insights. Remaining challenges include large-scale production, long-term safety assessment, and regulatory approval. Future directions focus on dual- and stimuli-responsive systems and their integration into precision oncology to accelerate clinical translation.</p>","PeriodicalId":7934,"journal":{"name":"Anti-cancer agents in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":3.0,"publicationDate":"2026-04-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147669846","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}