Anti-cancer agents in medicinal chemistry最新文献

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Emerging Claudin18.2-targeting Therapy for Systemic Treatment of Gastric Cancer: Seeking Nobility Amidst Danger. 用于胃癌全身治疗的新兴 Claudin18.2 靶向疗法:险中求胜。
IF 2.6 4区 医学
Anti-cancer agents in medicinal chemistry Pub Date : 2025-01-01 DOI: 10.2174/0118715206329892240927081033
Xueshuai Ye, Yongqiang Wu, Haiqiang Zhang
{"title":"Emerging Claudin18.2-targeting Therapy for Systemic Treatment of Gastric Cancer: Seeking Nobility Amidst Danger.","authors":"Xueshuai Ye, Yongqiang Wu, Haiqiang Zhang","doi":"10.2174/0118715206329892240927081033","DOIUrl":"10.2174/0118715206329892240927081033","url":null,"abstract":"<p><p>Gastric cancer in advanced stages lacked effective treatment options. claudin18.2 (CLDN18.2) is a membrane protein that is crucial for close junctions in the differentiated epithelial cells of the gastric mucosa, playing a vital role in barrier function, and can be hardly recognized by immune cells due to its polarity pattern. As the polarity of gastric tumor cells changes, claudin18.2 is exposed on the cell surface, resulting in immune system recognition, and making it an ideal target. In this review, we summarized the expression regulation mechanism of claudin18.2 both in normal cells and malignant tumor cells. Besides, we analyzed the available clinical results and potential areas for future research on claudin18.2-positive gastric cancer and claudin18.2-targeting therapy. In conclusion, claudin18.2 is an ideal target for gastric cancer treatment, and the claudin18.2-targeting therapy has changed the treatment pattern of gastric cancer.</p>","PeriodicalId":7934,"journal":{"name":"Anti-cancer agents in medicinal chemistry","volume":" ","pages":"223-231"},"PeriodicalIF":2.6,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142370794","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}
引用次数: 0
MG132-mediated Suppression of the Ubiquitin-proteasome Pathway Enhances the Sensitivity of Endometrial Cancer Cells to Cisplatin. MG132- 介导的泛素-蛋白酶体通路抑制增强了子宫内膜癌细胞对顺铂的敏感性
IF 2.6 4区 医学
Anti-cancer agents in medicinal chemistry Pub Date : 2025-01-01 DOI: 10.2174/0118715206343550240919055701
Zhanhu Zhang, Yiqian Ding
{"title":"MG132-mediated Suppression of the Ubiquitin-proteasome Pathway Enhances the Sensitivity of Endometrial Cancer Cells to Cisplatin.","authors":"Zhanhu Zhang, Yiqian Ding","doi":"10.2174/0118715206343550240919055701","DOIUrl":"10.2174/0118715206343550240919055701","url":null,"abstract":"<p><strong>Background: </strong>Tumor cell resistance to cisplatin is a common challenge in endometrial cancer chemotherapy, stemming from various mechanisms. Targeted therapies using proteasome inhibitors, such as MG132, have been investigated to enhance cisplatin sensitivity, potentially offering a novel treatment approach.</p><p><strong>Objective: </strong>The aim of this study was to investigate the effects of MG132 on cisplatin sensitivity in the human endometrial cancer (EC) cell line RL95-2, focusing on cell proliferation, apoptosis, and cell signaling.</p><p><strong>Methods: </strong>Human endometrial cancer RL95-2 cells were exposed to MG132, and cell viability was assessed in a dose-dependent manner. The study evaluated the effect of MG132 on cisplatin-induced proliferation inhibition and apoptosis, correlating with caspase-3 activation and reactive oxygen species (ROS) upregulation. Additionally, we examined the inhibition of the ubiquitin-proteasome system and the expression of pro-inflammatory cytokines IL-1β, IL-6, IL-8, and IL-13 during MG132 and cisplatin co-administration.</p><p><strong>Results: </strong>MG132 exposure significantly reduced cell viability in a dose-dependent manner. It augmented cisplatin- induced proliferation inhibition and enhanced apoptosis, correlating with caspase-3 activation and ROS upregulation. Molecular analysis revealed a profound inhibition of the ubiquitin-proteasome system. MG132 also significantly increased the expression of cisplatin-induced pro-inflammatory cytokines, suggesting a transition from chronic to acute inflammation.</p><p><strong>Conclusion: </strong>MG132 enhances the therapeutic efficacy of cisplatin in human EC cells by suppressing the ubiquitin- proteasome pathway, reducing cell viability, enhancing apoptosis, and shifting the inflammatory response. These findings highlighted the potential of MG132 as an adjuvant in endometrial cancer chemotherapy. Further research is needed to explore detailed mechanisms and clinical applications of this combination therapy.</p>","PeriodicalId":7934,"journal":{"name":"Anti-cancer agents in medicinal chemistry","volume":" ","pages":"281-291"},"PeriodicalIF":2.6,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142360951","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}
引用次数: 0
Screening and in vitro Biological Evaluation of Novel Multiple Tyrosine Kinases Inhibitors as Promising Anticancer Agents. 摘要:新型多种酪氨酸激酶抑制剂的筛选及体外生物学评价
IF 2.6 4区 医学
Anti-cancer agents in medicinal chemistry Pub Date : 2025-01-01 DOI: 10.2174/1871520623666230403104816
Xiuying Li, Pinglang Ruan, Gang Jiang, Weidong Zhang
{"title":"Screening and <i>in vitro</i> Biological Evaluation of Novel Multiple Tyrosine Kinases Inhibitors as Promising Anticancer Agents.","authors":"Xiuying Li, Pinglang Ruan, Gang Jiang, Weidong Zhang","doi":"10.2174/1871520623666230403104816","DOIUrl":"10.2174/1871520623666230403104816","url":null,"abstract":"<p><strong>Background: </strong>Tyrosine kinases have emerged as key stimulatory drivers in several cancer-related pathways. This is particularly evident in non-small cell lung cancer with regulating cell growth and apoptosis and so on. Tyrosine kinase inhibitors (TKI) are one breakthrough option that could improve the life quality of cancer patients.</p><p><strong>Objective: </strong>This study aims to find more effective tyrosine kinase inhibitors.</p><p><strong>Methods: </strong>In this study, natural products from TargetMol that may be the potential TKI for lung cancer were screened through structure-based virtual screening and experimental validation. Moreover, the binding between the hit compounds and tyrosine kinase was explored.</p><p><strong>Results: </strong>From the study findings, Gramicidin and Tannic acid have strong interactions with the four tyrosine kinases (ALK, TRK, MET, and ABL), and this could significantly inhibit the viability of A549 cells in a concentrationdependent manner.</p><p><strong>Conclusion: </strong>These findings indicated that Gramicidin and Tannic acid might be potential multiple TKI and are promising anticancer agents that call for further study.</p>","PeriodicalId":7934,"journal":{"name":"Anti-cancer agents in medicinal chemistry","volume":" ","pages":"555-562"},"PeriodicalIF":2.6,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"9254173","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}
引用次数: 0
An Updated Review on Dysregulated lncRNAs and their Contribution to the Various Molecular Types of Lung Carcinoma. 失调lncrna及其在肺癌各种分子类型中的作用的最新综述。
IF 2.6 4区 医学
Anti-cancer agents in medicinal chemistry Pub Date : 2025-01-01 DOI: 10.2174/0118715206336608241104065557
Narges Dastmalchi, Mohammad Reza Alipour, Reza Safaralizadeh, Khalil Hajiasgharzadeh
{"title":"An Updated Review on Dysregulated lncRNAs and their Contribution to the Various Molecular Types of Lung Carcinoma.","authors":"Narges Dastmalchi, Mohammad Reza Alipour, Reza Safaralizadeh, Khalil Hajiasgharzadeh","doi":"10.2174/0118715206336608241104065557","DOIUrl":"10.2174/0118715206336608241104065557","url":null,"abstract":"<p><p>Lung cancer is correlated with a high death rate, with approximately 1.8 million mortality cases reported worldwide in 2022. Despite development in the control of lung cancer, most cases are detected at higher stages with short survival rates. This reveals a need to recognize novel techniques to treat malignancy and decrease the burden of lung cancer. Long noncoding RNAs (lncRNAs) manage vital cellular and biochemical functions. lncRNAs play crucial roles in transcriptional and translational processes and signaling cascades. Recently, lncRNAs have been reported to be associated with malignancy where their expression is deregulated, leading to abnormal cellular activities and signaling pathways. In various malignancies, including lung cancer, lncRNA deregulation disrupts normal cellular function, promoting tumorigenesis and influencing patient outcomes and treatment responses. Studies have shown that lncRNAs can act as both oncogenes and tumor suppressors, depending on the lung cancer subtype, specifically in Non-small Cell Lung Cancer (NSCLC) and Small Cell Lung Cancer (SCLC). This dual role of lncRNAs as critical biomarkers might provide insights into lung cancer development and progression. lncRNAs have been discussed as key biomarkers in lung cancer. A comprehensive understanding of the biological activities of lncRNAs in NSCLC and SCLC may improve prognosis, diagnosis, and therapeutic methods. Researchers are increasingly interested in lncRNAs as potential diagnostic biomarkers and therapeutic targets in cancer treatment. As researchers continue to explore lncRNAs, their pivotal roles in lung cancer become increasingly evident. This review highlights the function of lncRNAs in lung carcinogenesis and discusses their molecular mechanisms of function.</p>","PeriodicalId":7934,"journal":{"name":"Anti-cancer agents in medicinal chemistry","volume":" ","pages":"490-498"},"PeriodicalIF":2.6,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142926263","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}
引用次数: 0
Pioneering a New Era in Oral Cancer Treatment with Electrospun Nanofibers: A Comprehensive Insight. 开创电纺纳米纤维治疗口腔癌新时代:全面洞察。
IF 2.6 4区 医学
Anti-cancer agents in medicinal chemistry Pub Date : 2025-01-01 DOI: 10.2174/0118715206348821241119100134
Devika Tripathi, Tanya Gupta, Awani Kumar Rai, Prashant Pandey
{"title":"Pioneering a New Era in Oral Cancer Treatment with Electrospun Nanofibers: A Comprehensive Insight.","authors":"Devika Tripathi, Tanya Gupta, Awani Kumar Rai, Prashant Pandey","doi":"10.2174/0118715206348821241119100134","DOIUrl":"10.2174/0118715206348821241119100134","url":null,"abstract":"<p><p>Oral cancer, currently ranked 16th among the most prevalent malignancies worldwide according to GLOBOCAN, presents significant challenges to global oral health. Conventional treatment modalities such as surgery, radiation, and chemotherapy often have limitations, prompting the need for innovative therapeutic approaches. Tissue engineering has emerged as a promising solution aimed at developing biocompatible, functional, and biologically responsive tissue constructs. This approach involves the integration of cells, bioactive compounds, and scaffolds to enhance treatment efficacy. Electrospun nanofibers, mimicking the extracellular matrix, exhibit considerable potential in addressing complex oral health issues by influencing cellular behavior. The versatility of electrospinning technology allows for the fabrication of fiber scaffolds with high surface area, making them ideal for localized delivery of bioactive compounds or pharmaceuticals. Enhancing these electrospun scaffolds with growth factors, nanoparticles, and biologically active substances significantly increases their therapeutic appeal in oral cancer management. This review offers a comprehensive examination of the various applications of electrospun nanofibers in oral cancer therapy. Utilizing electronic databases such as PubMed, CrossREF, and Google Scholar, we conducted an extensive review of relevant literature concerning \"electrospun nanofibers\" and their therapeutic potential in oral cancer treatment. Key topics addressed include engineering methodologies, drug diffusion mechanisms, factors influencing nanofiber scaffold design, toxicity concerns, and clinical implications. The findings underscore the transformative potential of electrospun nanofibers in revolutionizing oral cancer therapy.</p>","PeriodicalId":7934,"journal":{"name":"Anti-cancer agents in medicinal chemistry","volume":" ","pages":"468-489"},"PeriodicalIF":2.6,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142942920","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}
引用次数: 0
Utilizing Indigenous Flora in East Africa for Breast Cancer Treatment: An Overview. 利用东非本土植物治疗乳腺癌:概述。
IF 2.6 4区 医学
Anti-cancer agents in medicinal chemistry Pub Date : 2025-01-01 DOI: 10.2174/0118715206338557240909081833
Esther Ugo Alum, Tabussam Tufail, Daniel Ejim Uti, Patrick Maduabuchi Aja, Christian Emeka Offor, Udu Ama Ibiam, Chris U A Ukaidi, Benedict Nnachi Alum
{"title":"Utilizing Indigenous Flora in East Africa for Breast Cancer Treatment: An Overview.","authors":"Esther Ugo Alum, Tabussam Tufail, Daniel Ejim Uti, Patrick Maduabuchi Aja, Christian Emeka Offor, Udu Ama Ibiam, Chris U A Ukaidi, Benedict Nnachi Alum","doi":"10.2174/0118715206338557240909081833","DOIUrl":"10.2174/0118715206338557240909081833","url":null,"abstract":"<p><strong>Background: </strong>Breast cancer is a significant global health challenge, contributing substantially to cancer- related deaths. Conventional treatment methods, including hormone therapy, chemotherapy, surgical interventions, and radiation, have long been utilized. However, these traditional treatments are often associated with serious side effects and drug resistance, limiting their efficacy.</p><p><strong>Aim: </strong>This review aims to explore the potential of medicinal plants used in breast cancer management in East Africa, focusing on their bioactive compounds and anticancer properties.</p><p><strong>Methods: </strong>A comprehensive literature search was conducted to examine the effectiveness of medicinal plants in treating breast cancer across Kenya, Ethiopia, Uganda, Tanzania, and Rwanda. Relevant studies published between 2003 and 2023 were identified using keywords related to breast cancer and medicinal plants. The search was performed across multiple databases, including Google Scholar, PubMed, Scopus, Web of Science Core Collection, and Science Direct.</p><p><strong>Results: </strong>Numerous natural compounds found in East African medicinal plants including <i>Cymbopogon citratus (Lemongrass,)</i> Tabebuia avellanedae, <i>Prunus africana</i> (African Cherry), <i>Euclea divinorum, Berberis holstii, Withania somnifera</i> (Ashwagandha, <i>Curcuma longa</i> (Turmeric), <i>Garcinia mangostana</i> (Mangosteen, <i>Vitis vinifera</i> (Grapevine), <i>Eugenia jambolana</i> (Java Plum), <i>Moringa oleifera</i> (Drumstick Tree), <i>Camellia sinensis</i> (Tea), <i>Glycine max</i> (Soybean), <i>Catharanthus roseus</i>, Madagascar Periwinkle), <i>Rhus vulgaris</i> (Wild Currant) exhibit significant anticancer properties. These compounds have demonstrated the ability to reduce breast cancer aggressiveness, inhibit cancer cell proliferation, and modulate cancer-related pathways. Current research focuses on these natural and dietary compounds to develop more effective strategies for treating breast cancer.</p><p><strong>Conclusion: </strong>The findings suggested that East African medicinal plants hold promise as complementary treatments for breast cancer, offering potential benefits such as affordability, cultural appropriateness, and sustainability. Further research into these plants and their bioactive compounds could revolutionize breast cancer treatment, improving survival rates and addressing the rising incidence of breast cancer-related fatalities. Other: The review underscores the importance of continued research, conservation, and the integration of ancient healing methods to fully harness the potential of East African flora in breast cancer management.</p>","PeriodicalId":7934,"journal":{"name":"Anti-cancer agents in medicinal chemistry","volume":" ","pages":"99-113"},"PeriodicalIF":2.6,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142279369","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}
引用次数: 0
Doramectin Induces Apoptosis in B16 Melanoma Cells. 多拉菌素诱导 B16 黑色素瘤细胞凋亡
IF 2.6 4区 医学
Anti-cancer agents in medicinal chemistry Pub Date : 2025-01-01 DOI: 10.2174/0118715206325844240909144543
Megan S Crotts, Jena C Jacobs, Robert W Baer, James L Cox
{"title":"Doramectin Induces Apoptosis in B16 Melanoma Cells.","authors":"Megan S Crotts, Jena C Jacobs, Robert W Baer, James L Cox","doi":"10.2174/0118715206325844240909144543","DOIUrl":"10.2174/0118715206325844240909144543","url":null,"abstract":"<p><strong>Introduction/objective: </strong>Metastatic melanoma resists current pharmacological regimens that act through apoptosis. This indicates that therapies acting via non-apoptotic cell-death pathways could be pursued. Doramectin has shown promising results in another cancer of neural crest origin, neuroblastoma, through the inhibition of growth via autophagy. Our research hypothesis is that doramectin induces autophagy in B16F10 melanoma cells.</p><p><strong>Methods: </strong>Cells were treated with doramectin (15 uM) or a combination of both doramectin and a cell-death inhibitor, compared to untreated control cells (media), and then analyzed with MTT analysis. Likewise, MDC analysis was completed to detect autophagy involvement with doramectin treatment. Flow cytometry and TUNEL Assay were conducted to observe cell death-related effects.</p><p><strong>Results: </strong>MTT analysis of doramectin-treated cells displayed a decrease in cell growth compared to control. Apoptotic morphology was prominent in melanoma cells treated with doramectin. Increased autophagy was not detected by fluorometric microscopic analysis. Flow cytometry analysis of doramectin-treated cells showed apoptosis as a major mode of cell death with some necrosis.</p><p><strong>Conclusion: </strong>Doramectin induces a novel cell-death mechanism in melanoma compared to other forms of cancer and should be studied as an effective anti-cancer agent for melanoma treatment.</p>","PeriodicalId":7934,"journal":{"name":"Anti-cancer agents in medicinal chemistry","volume":" ","pages":"244-256"},"PeriodicalIF":2.6,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142456331","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}
引用次数: 0
A Review of Anticancer Potential of Conferone, Diversin and Ferutinin; Which One is Stronger for Cancer Therapy? 康非龙、Diversin 和 Ferutinin 的抗癌潜力综述:哪种抗癌药物更强?
IF 2.6 4区 医学
Anti-cancer agents in medicinal chemistry Pub Date : 2025-01-01 DOI: 10.2174/0118715206328175241022081832
Fariborz Keshmirshekan, Seyed-Mahdi Mohamadi-Zarch, Seyyed Majid Bagheri
{"title":"A Review of Anticancer Potential of Conferone, Diversin and Ferutinin; Which One is Stronger for Cancer Therapy?","authors":"Fariborz Keshmirshekan, Seyed-Mahdi Mohamadi-Zarch, Seyyed Majid Bagheri","doi":"10.2174/0118715206328175241022081832","DOIUrl":"10.2174/0118715206328175241022081832","url":null,"abstract":"<p><strong>Background: </strong>One of the growing diseases in today's human societies is cancer, which has become a major challenge, especially in industrialized and developing countries. Cancer treatments are diverse, but they usually use surgery, chemotherapy, and radiotherapy to improve patients. Existing drugs are usually expensive and, in some cases, are not effective due to drug resistance and side effects. Finding compounds of natural origin can be somewhat effective and useful in helping doctors to treat this disease. <i>Ferula</i> plants, which are traditionally used as spices or for medicinal purposes, can be a good source for finding anti-cancer compounds due to their various compounds, such as monoterpenes, sulfide compounds, and polyphenols. Several studies have shown that compounds found in <i>Ferula</i> plants have significant anticancer effects on various types of cancer cells.</p><p><strong>Objective: </strong>This article was compiled with the aim of collecting evidence and articles related to the anti-cancer effects of three compounds obtained from these plants, namely Conferone, Diversin, and Ferutinin.</p><p><strong>Methods: </strong>This review article was prepared by searching the terms Conferone, Diversin, Ferutinin and cancer and related information was collected through searching electronic databases such as ISI Web of Knowledge, PubMed and Google Scholar until the March of 2024.</p><p><strong>Conclusion: </strong>The results of this review showed that relatively comprehensive studies have been conducted in this field and these studies have shown that these compounds can be used in the design of future anticancer drugs. Among the examined compounds, conferone showed that it has the best effect on cancer cells.</p>","PeriodicalId":7934,"journal":{"name":"Anti-cancer agents in medicinal chemistry","volume":" ","pages":"378-387"},"PeriodicalIF":2.6,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142557039","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}
引用次数: 0
A Promising Paradigm Shift in Cancer Treatment with FGFR Inhibitors. 利用表皮生长因子受体抑制剂治疗癌症的范式转变前景广阔。
IF 2.6 4区 医学
Anti-cancer agents in medicinal chemistry Pub Date : 2025-01-01 DOI: 10.2174/0118715206318833240819031953
Anuradha Mehra, Rekha Sangwan
{"title":"A Promising Paradigm Shift in Cancer Treatment with FGFR Inhibitors.","authors":"Anuradha Mehra, Rekha Sangwan","doi":"10.2174/0118715206318833240819031953","DOIUrl":"10.2174/0118715206318833240819031953","url":null,"abstract":"<p><p>FGFR have been demonstrated to perform a crucial role in biological processes but their overexpression has been perceived as the operator component in the occurrence and progression of different types of carcinoma. Out of all the interest around cancer, FGFR inhibitors have assembled pace over the past few years. Therefore, FGFR inhibitors are one of the main fundamental tools to reverse drug resistance, tumor growth, and angiogenesis. Currently, many FGFR inhibitors are under the development stage or have been developed. Due to great demand and hotspots, different pharmacophores were approached to access structurally diverse FGFR inhibitors. Here, we have selected to present several representative examples such as Naphthyl, Pyrimidine, Pyridazine, Indole, and Quinoline derivatives that illustrate the diversity and advances of FGFR inhibitors in medicinal chemistry. This review focuses on the SAR study of FGFR inhibitors last five years which will be a great future scope that influences the medicinal chemist to work towards more achievements in this area.</p>","PeriodicalId":7934,"journal":{"name":"Anti-cancer agents in medicinal chemistry","volume":" ","pages":"2-23"},"PeriodicalIF":2.6,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142078869","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}
引用次数: 0
The Mesoionic 1,3,4-thiadiazolium Derivative, MI-D, is a Potential Drug for Treating Glioblastoma by Impairing Mitochondrial Functions Linked to Energy Provision in Glioma Cells. 中离子 1,3,4-噻二唑衍生物 MI-D 是一种通过损害胶质瘤细胞中与能量供应相关的线粒体功能来治疗胶质母细胞瘤的潜在药物。
IF 2.6 4区 医学
Anti-cancer agents in medicinal chemistry Pub Date : 2025-01-01 DOI: 10.2174/0118715206329159241010052746
Marília Locatelli Corrêa-Ferreira, Amanda do Rocio Andrade Pires, Juan Vitor Miranda, Eduardo de Freitas Montin, Igor Resendes Barbosa, Aurea Echevarria Aznar Neves Lima, Maria Eliane Merlin Rocha, Glaucia Regina Martinez, Sílvia Maria Suter Correia Cadena
{"title":"The Mesoionic 1,3,4-thiadiazolium Derivative, MI-D, is a Potential Drug for Treating Glioblastoma by Impairing Mitochondrial Functions Linked to Energy Provision in Glioma Cells.","authors":"Marília Locatelli Corrêa-Ferreira, Amanda do Rocio Andrade Pires, Juan Vitor Miranda, Eduardo de Freitas Montin, Igor Resendes Barbosa, Aurea Echevarria Aznar Neves Lima, Maria Eliane Merlin Rocha, Glaucia Regina Martinez, Sílvia Maria Suter Correia Cadena","doi":"10.2174/0118715206329159241010052746","DOIUrl":"10.2174/0118715206329159241010052746","url":null,"abstract":"<p><strong>Background: </strong>Mesoionic compound MI-D possesses important biological activities, such as antiinflammatory and antitumoral against melanoma and hepatocarcinoma. Glioblastoma is the most aggressive and common central nervous system tumor in adults. Currently, chemotherapies are not entirely effective, and the survival of patients diagnosed with glioblastoma is extremely short.</p><p><strong>Objective: </strong>In this study, we aimed to evaluate the cytotoxicity of MI-D in noninvasive A172 glioblastoma cells and establish which changes in functions linked to energy provision are associated with this effect.</p><p><strong>Methods: </strong>Cells A172 were cultured under glycolysis and phosphorylation oxidative conditions and evaluated: viability by the MTT method, oxygen consumption by high-resolution respirometry, levels of pyruvate, lactate, citrate, and ATP, and glutaminase and citrate synthase activities by spectrophotometric methods.</p><p><strong>Results: </strong>Under glycolysis-dependent conditions, MI-D caused significant cytotoxic effects with impaired cell respiration, reducing the maximal capacity of the electron transport chain. However, A172 cells were more susceptible to MI-D effects under oxidative phosphorylation-dependent conditions. At the IC<sub>25</sub>, inhibition of basal and maximal respiration of A172 cells was observed, without stimulation of the glycolytic pathway or Krebs cycle, along with inhibition of the activity of glutaminase enzyme, resulting in a 30% ATP deficit. Additionally, independent of metabolic conditions, MI-D treatment induced cell death in A172 cells by apoptosis machinery/ processes.</p><p><strong>Conclusion: </strong>The impairment of mitochondrial respiration by MI-D under the condition sustained by oxidative phosphorylation may enhance the cytotoxic effect on A172 glioma cells, although the mechanism of cell death relies on apoptosis.</p>","PeriodicalId":7934,"journal":{"name":"Anti-cancer agents in medicinal chemistry","volume":" ","pages":"411-419"},"PeriodicalIF":2.6,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142493102","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}
引用次数: 0
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