Anti-cancer agents in medicinal chemistry最新文献

{"title":"Bioactive Products Targeting C-Met As Potential Antitumour Drugs.","authors":"Liying Zhao, Chunmei Qian, Xiaoqi Ma, Xiaoyu Wang","doi":"10.2174/0118715206346207241217064022","DOIUrl":"10.2174/0118715206346207241217064022","url":null,"abstract":"<p><p>Mesenchymal‒epithelial transition factor (c-Met), a receptortyrosine kinase (RTK), plays a vital role in cell proliferation, migration and invasion, and tumour metastasis.</p><p><strong>Objective: </strong>With increasing duration of treatment, many tumours gradually develop drug resistance. Therefore, novel antitumour drugs need to be developed to treat patients with tumours. Targeting c-met inhibitors may be an effective treatment strategy.</p><p><strong>Methods: </strong>Scientific databases such as ScienceDirect, PubMed, the Wiley Online Library, and Social Sciences Citation Index were used to collect information. All the relevant literature was reviewed, and the available literature was screened. The upstream and downstream pathways of c-Met and their relevance to antitumour effects were searched based on the articles' title, abstract, and full text. The c-Met-targeting drugs with antitumour effects are summarized below. A \"citation within a citation\" or snowballing approach was used in this screening process to identify additional papers that may have been missed in the initial literature screening process. High-quality studies published in peer-reviewed journals were summarized and prioritized for citation in the review.</p><p><strong>Results: </strong>In recent years, research on small-molecule targeted drugs has developed rapidly. Many results have also been achieved in the synthesis and isolation of c-Met inhibitors from natural compounds and traditional Chinese medicines.</p><p><strong>Conclusion: </strong>This article summarizes the developments in anti-c-Met drugs, which are synthesized and isolated from natural compounds and traditional Chinese medicine (TCM). This study provides primary resources for the development of c-Met inhibitors.</p>","PeriodicalId":7934,"journal":{"name":"Anti-cancer agents in medicinal chemistry","volume":" ","pages":"688-696"},"PeriodicalIF":2.6,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142982529","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":"Synergistic Anti-tumorigenic Effects of Cabazitaxel and Usnic Acid Combination on Metastatic Castration-Resistant Prostate Cancer Cells.","authors":"Ceyda Colakoglu Bergel, Isil Ezgi Eryilmaz, Ebrucan Bulut, Rumeysa Fatma Balaban, Unal Egeli, Gulsah Cecener","doi":"10.2174/0118715206336754241015062614","DOIUrl":"10.2174/0118715206336754241015062614","url":null,"abstract":"<p><strong>Background: </strong>Prostate cancer (PC) affects millions of men, causing high mortality rates. Despite the treatment approaches, the options for metastatic castration-resistant prostate cancer (mCRPC), a lethal form of advanced PC, are still limited. Cabazitaxel (Cbx) is the last taxane-derived chemotherapeutic approved for Docetaxel- resistant mCRPC patients. However, its effects are limited due to the activation of several pathways. Therefore, new approaches are needed to increase the efficacy of Cbx. Usnic acid (UA) is a natural product with wellknown anti-tumorigenic and synergistic effects with various chemotherapeutics. Although the cytotoxicity of UA and Cbx has been evaluated on mCRPC cells, the anti-tumorigenic effect of UA combination with any taxane has not been investigated yet. Thus, we aimed to evaluate the possible synergistic effect of Cbx+UA in mCRPC cells.</p><p><strong>Methods: </strong>Cell viability and apoptosis were analyzed using WST-1 and Annexin-V. Morphological changes were visualized by fluorescent staining. Finally, cell cycle, mitochondrial health, and ROS levels were determined.</p><p><strong>Results: </strong>Based on WST-1 results, 25 μM UA exhibited significant additive and synergistic effects with the use of Cbx. Annexin V and cell cycle results showed that UA significantly enhanced the Cbx efficacy at increasing doses compared to using only Cbx (**p<0.01). Moreover, combined treatment significantly increased ROS levels and mitochondrial membrane depolarization compared with Cbx alone (**p<0.01).</p><p><strong>Conclusions: </strong>Thus, the results suggest that UA increased the anti-tumorigenic effects of Cbx on mCRPC cells by increasing apoptosis, causing an increase in intracellular ROS and disrupting mitochondrial health. Consequently, combining UA and Cbx offers a new combined therapeutic strategy for mCRPC treatment.</p>","PeriodicalId":7934,"journal":{"name":"Anti-cancer agents in medicinal chemistry","volume":" ","pages":"610-619"},"PeriodicalIF":2.6,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142982535","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":"Design and Evaluation of 5-oxo-1,2,4-triazole-3-carboxamide Compounds as Promising Anticancer Agents: Synthesis, Characterization, <i>In vitro</i> Cytotoxicity and Molecular Docking Studies.","authors":"Rajitha Balavanthapu, Girija Sastry Vedula","doi":"10.2174/0118715206315373241014101856","DOIUrl":"10.2174/0118715206315373241014101856","url":null,"abstract":"<p><strong>Background: </strong>Cancer presents a significant global health challenge, necessitating effective treatment strategies. While chemotherapy is widely employed, its non-specific nature can induce adverse effects on normal cells, prompting the exploration of targeted therapies. The 1,2,4-triazole scaffold has emerged as a promising element in anticancer drug development due to its structural diversity and potential to target cancer cells.</p><p><strong>Objective: </strong>This study aims to synthesize and evaluate novel derivatives derived from the 1,2,4-triazole scaffold for their potential as anticancer agents. Molecular docking techniques are employed to investigate the interactions between the designed derivatives and specific cancer-related targets, providing insights into potential underlying mechanisms.</p><p><strong>Methods: </strong>The synthesis involves a three-step process to produce 5-oxo-1,2,4-triazole-3-carboxamide derivatives. Various analytical techniques, including NMR and HRMS, validate the successful synthesis. Molecular docking studies utilize X-ray crystal structures of EGFR and CDK-4 obtained from the Protein Data Bank, employing the Schrödinger suite for ligand preparation and Glide's extra-precision docking modes for scoring.</p><p><strong>Results: </strong>The synthesis yields compounds with moderate to good yields, supported by detailed characterization. Molecular docking scores for the derivatives against EGFR and CDK-4 revealed diverse affinities influenced by distinct substituents. Compounds with hydroxyl, and halogen, substitutions exhibited notable binding affinities, while alkyl and amino substitutions showed varying effects. The 1,2,4-triazole derivatives demonstrated potential for targeted cancer therapy.</p><p><strong>Conclusion: </strong>The study highlights the successful synthesis of 5-oxo-1,2,4-triazole-3-carboxamides and their diverse interactions with cancer-related targets. The findings emphasized the potential of these derivatives as candidates for further development as anticancer agents, offering insights into structure-activity relationships. The 1,2,4-triazole scaffold stands out as a promising platform for advancing cancer treatment with enhanced precision and efficacy.</p>","PeriodicalId":7934,"journal":{"name":"Anti-cancer agents in medicinal chemistry","volume":" ","pages":"765-773"},"PeriodicalIF":2.6,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142942894","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":"Unveiling the Potential of S4 on Non-small Cell Lung Cancer Cells: Impact on Proliferation, Apoptosis, Senescence, and Metabolome Profile.","authors":"Turan Demircan, Mervenur Yavuz, Aydın Boluk","doi":"10.2174/0118715206350735241224073200","DOIUrl":"10.2174/0118715206350735241224073200","url":null,"abstract":"<p><strong>Background: </strong>Lung cancer is a highly aggressive tumor with limited therapeutic options. The misregulation of Androgen Receptor (AR) signaling has been observed in lung cancer. Therefore, inhibiting AR signaling is a promising strategy for treating lung cancer.</p><p><strong>Objective: </strong>Selective Androgen Receptor Modulators (SARMs) are small molecule drugs with a high affinity for the AR. S4, a member of SARMs was potentially positioned as a promising therapeutic agent in A549 lung cancer cells owing to its high bioavailability, lesser side effects, and novelty in cancer.</p><p><strong>Methods: </strong>We employed several techniques to investigate the potential anti-carcinogenic effect of S4 on A549 cells at cellular level. The cytotoxicity of S4 was investigated thorough MTT, and the IC₅₀ value was identified as 0.22 mM. Then, the anchorage-dependent and -independent colonization of cells were assessed by colony formation and soft agar assays, respectively. Additionally, migration capacity, apoptosis, proliferation, senescene, cell-cycle progression of cells was examined thoroughly. In addition, gene expression profile and metabolome signature were explored via qRT-PCR and metabolomics, respectively to provide molecular links for S4 mode of action.</p><p><strong>Results: </strong>Our findings demonstrate that S4 inhibited growth, migration, and proliferation while inducing apoptosis. S4 significantly upregulated the <i>BAX, CDKN1A, PUMA,</i> and <i>GADD45A</i> genes while downregulating <i>MKI67, BIRC5,</i> and <i>PCNA</i> expression. S4 treatment drastically altered the metabolome signature, and enrichment of cancer related pathways by altered metabolites was noteworthy.</p><p><strong>Conclusion: </strong>We report the first study evaluating the potential anti-carcinogenic effects of S4 on lung cancer invitro which would bridge the gap on the utility of SARMs as inhibitors of lung cancer. Our results suggest that S4 could be considered as a promising drug candidate to test further for lung cancer treatment.</p>","PeriodicalId":7934,"journal":{"name":"Anti-cancer agents in medicinal chemistry","volume":" ","pages":"785-799"},"PeriodicalIF":2.6,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143021761","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":"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}

{"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}

{"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}

{"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}

{"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 IC₂₅, 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}

{"title":"Advancements in Pyrazine Derivatives as Anticancer Agents: A Comprehensive Review (2010-2024).","authors":"Mohammed Merae Alshahrani","doi":"10.2174/0118715206333399240912071555","DOIUrl":"10.2174/0118715206333399240912071555","url":null,"abstract":"<p><p>Cancer, an intricate and formidable disease, continues to challenge Medical Science with its diverse manifestations and relentless progression. In the pursuit of novel therapeutic strategies, organic heterocyclic compounds have emerged as promising candidates due to their versatile chemical structures and intricate interactions with biological systems. Among these, pyrazine derivatives are characterized by a six-membered aromatic ring containing four carbon and two nitrogen atoms situated in a 1,4-orientation. These compounds garnered significant attention for their potential as anticancer agents. This comprehensive review provides a detailed analysis of the advancements made during this timeframe, encompassing the chemical diversity of pyrazine derivatives, their mechanisms of action at the cellular level, and structure-activity relationships, spanning the years 2010 to 2024. By examining their therapeutic potential, challenges, and future prospects, this review offers valuable insights into the evolving landscape of pyrazine derivatives as potent tools in the fight against cancer.</p>","PeriodicalId":7934,"journal":{"name":"Anti-cancer agents in medicinal chemistry","volume":" ","pages":"151-163"},"PeriodicalIF":2.6,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142339474","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}