European Journal of Medicinal Chemistry Reports最新文献

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Anti-cancer potential of non-curcuminoid bioactive from Curcuma caesia Roxb. (Black Turmeric): Targeting cervical cancer via PI3K/Akt pathway modulation 姜黄非姜黄素类生物活性的抗癌潜力。(黑姜黄):通过PI3K/Akt通路调节靶向宫颈癌
European Journal of Medicinal Chemistry Reports Pub Date : 2025-05-14 DOI: 10.1016/j.ejmcr.2025.100273
Bishnu P. Parida , Megha Radhakrishnan , Varsha Goyal , Astha Sharma , Rupesh Zarekar , Mumtaz A. Ansari , Jasmeet Singh , Sunita Singh , Gopeshwar Narayan
{"title":"Anti-cancer potential of non-curcuminoid bioactive from Curcuma caesia Roxb. (Black Turmeric): Targeting cervical cancer via PI3K/Akt pathway modulation","authors":"Bishnu P. Parida ,&nbsp;Megha Radhakrishnan ,&nbsp;Varsha Goyal ,&nbsp;Astha Sharma ,&nbsp;Rupesh Zarekar ,&nbsp;Mumtaz A. Ansari ,&nbsp;Jasmeet Singh ,&nbsp;Sunita Singh ,&nbsp;Gopeshwar Narayan","doi":"10.1016/j.ejmcr.2025.100273","DOIUrl":"10.1016/j.ejmcr.2025.100273","url":null,"abstract":"<div><div><em>Curcuma caesia</em>, or black turmeric, is a significant medicinal plant used in traditional Indian medicine, including Ayurveda and folk practices. Indigenous communities in the northern Indo-Gangetic plains have utilized it for its analgesic, anti-inflammatory, and anti-infective properties. However, the anti-cancer potential of non-curcuminoid bioactive from <em>Curcuma caesia</em> remains underexplored. The current study investigates the anti-cancer potential of non-curcuminoid bioactive compounds derived from <em>Curcuma caesia</em> rhizome extracts, focusing on their effects against cervical cancer.</div><div>Using high-resolution mass spectrometry (HRMS), key compounds were identified from hexane (HECC) and methanolic (MECC) extracts, among which 3,4-dihydrocoumarin and (+)-ar-turmerone were prominent. <em>In vitro</em> cytotoxicity assays demonstrated that both HECC and MECC selectively inhibited the viability of cervical cancer cell lines, sparing non-tumorigenic HEK293T cells. Mechanistic analyses revealed that 3,4-dihydrocoumarin treatment led to mitochondrial membrane hyperpolarization, suppression of intracellular ROS, and cell cycle arrest at subG1 and G1 phases, while (+)-ar-turmerone had antagonistic modulatory effects. Western blotting confirmed downregulation of PI3K and Akt protein expression. Complementary ADME profiling indicated favorable pharmacokinetic properties, while molecular docking supported strong binding affinity of 3,4-dihydrocoumarin to PI3K and Akt targets, reinforcing its mechanism of action.</div><div><em>Curcuma caesia</em> rhizome fractions, especially 3,4-dihydrocoumarin, exhibit anti-cancer properties by modulating key molecular pathways, including the PI3K/Akt pathway.</div></div>","PeriodicalId":12015,"journal":{"name":"European Journal of Medicinal Chemistry Reports","volume":"14 ","pages":"Article 100273"},"PeriodicalIF":0.0,"publicationDate":"2025-05-14","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144088809","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
M7: A novel in vitro CDK1 inhibitor suppressing colorectal cancer cell proliferation, migration and promoting apoptosis M7:一种新型体外CDK1抑制剂抑制结直肠癌细胞增殖、迁移和促进细胞凋亡
European Journal of Medicinal Chemistry Reports Pub Date : 2025-05-13 DOI: 10.1016/j.ejmcr.2025.100271
Lihong Yang , Yipan Zhu , Xinyu Ding , Jing Sun , Xinyu Cao , Zhisong Zhang , Luyuan Li , Jianping Lin
{"title":"M7: A novel in vitro CDK1 inhibitor suppressing colorectal cancer cell proliferation, migration and promoting apoptosis","authors":"Lihong Yang ,&nbsp;Yipan Zhu ,&nbsp;Xinyu Ding ,&nbsp;Jing Sun ,&nbsp;Xinyu Cao ,&nbsp;Zhisong Zhang ,&nbsp;Luyuan Li ,&nbsp;Jianping Lin","doi":"10.1016/j.ejmcr.2025.100271","DOIUrl":"10.1016/j.ejmcr.2025.100271","url":null,"abstract":"<div><h3>Objective</h3><div>Colorectal cancer has a high mortality rate, and drug resistance limits the efficacy of targeted therapies. This study aims to explore the role of M7 in colorectal cancer, identify its targets, and assess its potential as a therapeutic agent.</div></div><div><h3>Methods</h3><div>A multi-stage biochemical screening strategy combined with bio-assay validation was used. In vitro ADP-Glo™ kinase assays verified M7's activity as a potential CDK1 inhibitor.</div></div><div><h3>Results</h3><div>M7 inhibits the proliferation and migration of HCT116 and Lovo cells by down-regulating EMT-related genes, promotes apoptosis by regulating apoptosis-related genes, and targets CDK1, causing G2/M phase arrest.</div></div><div><h3>Conclusions</h3><div>M7, a novel CDK1 inhibitor, shows potential for colorectal cancer drug development.</div></div>","PeriodicalId":12015,"journal":{"name":"European Journal of Medicinal Chemistry Reports","volume":"14 ","pages":"Article 100271"},"PeriodicalIF":0.0,"publicationDate":"2025-05-13","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144088810","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Synthesis of novel derivatives from machilin C/D as antiproliferative agents against triple negative breast cancer 抗三阴性乳腺癌的新衍生物machilin C/D的合成
European Journal of Medicinal Chemistry Reports Pub Date : 2025-05-08 DOI: 10.1016/j.ejmcr.2025.100272
Alyson M. Ackerman , Chibuzor Olewele , Bert C. Lynn , Samuel G. Awuah
{"title":"Synthesis of novel derivatives from machilin C/D as antiproliferative agents against triple negative breast cancer","authors":"Alyson M. Ackerman ,&nbsp;Chibuzor Olewele ,&nbsp;Bert C. Lynn ,&nbsp;Samuel G. Awuah","doi":"10.1016/j.ejmcr.2025.100272","DOIUrl":"10.1016/j.ejmcr.2025.100272","url":null,"abstract":"<div><div>Lignans are small polyphenolic compounds that play an active role in plant defense against pathogens and predators. Recently, lignan machilin D was reported to be effective as an anti-tumorigenic agent in triple negative breast cancer (TNBC) tumor-bearing mice. Previous studies have relied on plant-extracted material limiting scalability and diversification of the natural scaffold. Herein, we describe a generalizable one-pot synthesis of machilin D and its derivatives via an iron chloride-induced dimerization of isoeugenol. Employing this synthetic methodology allowed for a robust diversification campaign to access seven (7) new lignan derivatives of the machilin D family with superior anti-proliferative properties in 2D and 3D TNBC models. Overall, this work enables lignan natural product-based drug discovery as a platform to identify new probes to elucidate lignan targets in biology and therapeutics for aggressive cancers such as TNBC.</div></div>","PeriodicalId":12015,"journal":{"name":"European Journal of Medicinal Chemistry Reports","volume":"14 ","pages":"Article 100272"},"PeriodicalIF":0.0,"publicationDate":"2025-05-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143950386","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Exploring pyridinium-based inhibitors of cholinesterases: A review of synthesis, efficacy, and structural insights 探索以吡啶为基础的胆碱酯酶抑制剂:合成、疗效和结构见解的综述
European Journal of Medicinal Chemistry Reports Pub Date : 2025-04-25 DOI: 10.1016/j.ejmcr.2025.100270
Efraín Polo-Cuadrado , Cristian Rojas-Peña , Karen Acosta-Quiroga , Lorena Camargo-Ayala , Yeray A. Rodríguez-Núñez , Edison Osorio , Jhon J. López , Rhonny Brid-Cuadrado , Margarita Gutierrez
{"title":"Exploring pyridinium-based inhibitors of cholinesterases: A review of synthesis, efficacy, and structural insights","authors":"Efraín Polo-Cuadrado ,&nbsp;Cristian Rojas-Peña ,&nbsp;Karen Acosta-Quiroga ,&nbsp;Lorena Camargo-Ayala ,&nbsp;Yeray A. Rodríguez-Núñez ,&nbsp;Edison Osorio ,&nbsp;Jhon J. López ,&nbsp;Rhonny Brid-Cuadrado ,&nbsp;Margarita Gutierrez","doi":"10.1016/j.ejmcr.2025.100270","DOIUrl":"10.1016/j.ejmcr.2025.100270","url":null,"abstract":"<div><div>Pyridinium-based compounds have emerged as promising multifunctional agents for Alzheimer's disease therapy, demonstrating remarkable dual inhibition of acetylcholinesterase and butyrylcholinesterase. This comprehensive analysis of more than 100 derivatives revealed that strategic structural modifications significantly enhance their therapeutic potential. Disubstituted analogues, representing more than half of the reported compounds, show particular promise, with many achieving exceptional potency below 100 nM, surpassing reference drugs such as donepezil, in optimized cases. Molecular Insights confirmed the presence of important interactions within the catalytic active site (CAS) and peripheral active site (PAS), explaining their robust inhibitory activity and highlighting several successful design approaches. Incorporating cationic groups at the 1,3-positions dramatically improves catalytic site binding, as seen in compounds such as Bb4, with an impressive 6.2 nM activity. Bulky aromatic extensions, such as naphthyl moieties, effectively target peripheral sites, while optimal C7-C12 linkers in bivalent structures enable the simultaneous engagement of both catalytic and peripheral sites. Planar fused-ring systems, particularly β-carboline derivatives, demonstrate enhanced blood-brain barrier penetration, which is a crucial challenge in CNS drug development. These compounds showed potential beyond cholinesterase inhibition, with selected derivatives exhibiting additional benefits against β-amyloid aggregation, oxidative stress, and NMDA) receptor modulation. However, their path to clinical application requires overcoming significant hurdles, particularly in demonstrating reliable blood-brain barrier penetration and establishing comprehensive safety profiles. Future progress depends on rigorous in vivo validation using disease-relevant models coupled with systematic optimization of pharmacokinetic properties. By addressing these challenges, pyridinium-based scaffolds could evolve into valuable multifunctional therapeutics, offering new hope for Alzheimer's patients through their unique combination of mechanisms and tunable chemical properties.</div></div>","PeriodicalId":12015,"journal":{"name":"European Journal of Medicinal Chemistry Reports","volume":"14 ","pages":"Article 100270"},"PeriodicalIF":0.0,"publicationDate":"2025-04-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143898760","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Late-stage functionalization of anticancer agent Daniquidone and the in vitro anticancer activities of the derivatives 抗癌药物丹尼魁酮的后期功能化及其衍生物的体外抗癌活性
European Journal of Medicinal Chemistry Reports Pub Date : 2025-04-14 DOI: 10.1016/j.ejmcr.2025.100269
Geshuyi Chen , Yechun Zeng , Xin Chen , Zhe Chang , Pei Yuan , Haijia Chen , Yongxiu Yang , Xiaolei Liang , Kun Yue , Depeng Zhao
{"title":"Late-stage functionalization of anticancer agent Daniquidone and the in vitro anticancer activities of the derivatives","authors":"Geshuyi Chen ,&nbsp;Yechun Zeng ,&nbsp;Xin Chen ,&nbsp;Zhe Chang ,&nbsp;Pei Yuan ,&nbsp;Haijia Chen ,&nbsp;Yongxiu Yang ,&nbsp;Xiaolei Liang ,&nbsp;Kun Yue ,&nbsp;Depeng Zhao","doi":"10.1016/j.ejmcr.2025.100269","DOIUrl":"10.1016/j.ejmcr.2025.100269","url":null,"abstract":"<div><div>Nitrogen heterocycles play an important role in drugs and natural products. C-H late-stage functionalization (LSF) of N-heterocycles might provide a direct route to construct diversified analogues with potential pharmaceutical activities. Here, we employed a Cu-catalyzed C–H LSF to modify an anticancer drug Daniquidone and successfully converted the N-α position C–H bond into C–O, C–C and C–S bonds. Anticancer activities of all modified compounds <em>in vitro</em> were measured against three cell lines. The results showed that compound <strong>2i</strong> was the most active compound among all derivatives synthesized (IC<sub>50</sub> = 2.14 ± 1.23 μM against OVCAR-3, IC<sub>50</sub> = 4.07 ± 1.09 μM against A2780), <strong>1b</strong>, <strong>1g</strong> and <strong>2j</strong> also exhibit increased activity compared to the parent drug Daniquidone. Besides, molecular docking simulations with <strong>1b</strong>, <strong>1g</strong> and <strong>2j</strong> were conducted to further understand their binding modes.</div></div>","PeriodicalId":12015,"journal":{"name":"European Journal of Medicinal Chemistry Reports","volume":"14 ","pages":"Article 100269"},"PeriodicalIF":0.0,"publicationDate":"2025-04-14","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143844232","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Nanotechnology-based drug delivery for breast cancer treatment: Current applications and future directions 基于纳米技术的给药乳腺癌治疗:当前应用和未来方向
European Journal of Medicinal Chemistry Reports Pub Date : 2025-04-12 DOI: 10.1016/j.ejmcr.2025.100268
Md Abdus Samad , Iftikhar Ahmad , Torki A. Zughaibi , Mohd Suhail , Syed Kashif Zaidi , Fahad A. Al-Abbasi , Shams Tabrez
{"title":"Nanotechnology-based drug delivery for breast cancer treatment: Current applications and future directions","authors":"Md Abdus Samad ,&nbsp;Iftikhar Ahmad ,&nbsp;Torki A. Zughaibi ,&nbsp;Mohd Suhail ,&nbsp;Syed Kashif Zaidi ,&nbsp;Fahad A. Al-Abbasi ,&nbsp;Shams Tabrez","doi":"10.1016/j.ejmcr.2025.100268","DOIUrl":"10.1016/j.ejmcr.2025.100268","url":null,"abstract":"<div><div>Breast cancer (BC) is one of the most prevalent cancers in women worldwide. Limited specificity, systemic toxicity, risk of recurrence, and drug resistance are some of the drawbacks of traditional BC treatment approaches. Therefore, it is crucial to develop more effective, safe, and customized management plans for BC. The application of nanoparticle-based systems, such as liposomes, nanostructured lipid carriers, polymeric micelles, polymeric nanoparticles, dendrimers, and hybrid nanoparticles, has drawn significant interest in BC treatment. Nanomedicine can enhance the efficacy of drugs through active targeting, better tissue penetration, and more efficient tumor suppression <em>via</em> improved retention and permeability. Additionally, gene delivery using hybrid and theranostic nanomedicine has also been explored in BC treatment. Numerous nanomedicines have been used clinically for the treatment of breast cancer, some of which have already received U.S. Food and Drug Administration (USFDA) approval. Here, we focus on nanotechnology-based therapeutic approaches for BC treatment and highlighted their enhanced efficacy and reduced side effects. In addition, we have also explored on the possible utilization of Artificial Intelligence (AI) nanomedicine and bioinspired nanocarriers for BC treatment, which could pave the way for more precise, effective, and personalized therapies by improving nanoparticle design, optimizing drug delivery systems, and leveraging big data analytics.</div></div>","PeriodicalId":12015,"journal":{"name":"European Journal of Medicinal Chemistry Reports","volume":"14 ","pages":"Article 100268"},"PeriodicalIF":0.0,"publicationDate":"2025-04-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143825596","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Zuogui Wan attenuates ovariectomy-induced osteoporosis via the GH/IGF1 axis and related pathways 左归丸通过GH/IGF1轴及其相关通路减轻卵巢切除术所致骨质疏松
European Journal of Medicinal Chemistry Reports Pub Date : 2025-04-07 DOI: 10.1016/j.ejmcr.2025.100264
Yujie Ma , Pei Li , Changheng Song , Yuhan Wang , Qiqi Yan , Ying Yang , Wenjie Li , Xinyu Wan , Ruyuan Zhu , Jiayi Ma , Yanjing Chen , Haixia Liu , Zhiguo Zhang
{"title":"Zuogui Wan attenuates ovariectomy-induced osteoporosis via the GH/IGF1 axis and related pathways","authors":"Yujie Ma ,&nbsp;Pei Li ,&nbsp;Changheng Song ,&nbsp;Yuhan Wang ,&nbsp;Qiqi Yan ,&nbsp;Ying Yang ,&nbsp;Wenjie Li ,&nbsp;Xinyu Wan ,&nbsp;Ruyuan Zhu ,&nbsp;Jiayi Ma ,&nbsp;Yanjing Chen ,&nbsp;Haixia Liu ,&nbsp;Zhiguo Zhang","doi":"10.1016/j.ejmcr.2025.100264","DOIUrl":"10.1016/j.ejmcr.2025.100264","url":null,"abstract":"<div><h3>Introduction</h3><div>Zuogui Wan (ZGW)—one of the classic Chinese formulas—is clinically used to treat osteoporosis (OP). The current investigation aimed to analyze the phytochemical profile of ZGW and to elucidate its mechanisms of action in counteracting OP induced by ovariectomy (OVX) in rats.</div></div><div><h3>Methods</h3><div>The UPLC-MS/MS method was employed to determine the unique qualitative profile of the compounds. OVX rats were subjected to ZGW treatment for 12 weeks. Changes in body weight and bone protective effects were evaluated using various assays, including Vaginal smear assay, HE staining, Micro-CT imaging, and biomechanical testing. The related genes and proteins were validated using RT-qPCR, IHC, and Western blot.</div></div><div><h3>Results</h3><div>The UPLC-MS/MS analysis identified 2091 compounds, and the integral correction diagram showed 23 metabolites. ZGW treatment effectively ameliorated the diminished bone mineral density and compromised bone microstructures observed in OVX rats. Furthermore, ZGW administration to OVX rats increased bone tissue expression levels of RUNX2, BMP2, OSX, OC, and OPG. Moreover, ZGW administration in OVX rats restored the disturbed GH/IGF1 axis. Also, it activated PI3K/AKT signaling pathway and YAP/TAZ signaling pathway.</div></div><div><h3>Conclusion</h3><div>ZGW may exert its anti-OP effects by regulating the GH/IGF1 axis and its related signaling pathways.</div></div>","PeriodicalId":12015,"journal":{"name":"European Journal of Medicinal Chemistry Reports","volume":"14 ","pages":"Article 100264"},"PeriodicalIF":0.0,"publicationDate":"2025-04-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143850133","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Incomplete functionalization of glycodendrimers: Effects on binding affinity with wheat germ agglutinin 糖树状大分子不完全功能化:对与小麦胚芽凝集素结合亲和力的影响
European Journal of Medicinal Chemistry Reports Pub Date : 2025-04-07 DOI: 10.1016/j.ejmcr.2025.100266
Takahiko Matsushita , Naomichi Toda , Tetsuo Koyama , Ken Hatano , Koji Matsuoka
{"title":"Incomplete functionalization of glycodendrimers: Effects on binding affinity with wheat germ agglutinin","authors":"Takahiko Matsushita ,&nbsp;Naomichi Toda ,&nbsp;Tetsuo Koyama ,&nbsp;Ken Hatano ,&nbsp;Koji Matsuoka","doi":"10.1016/j.ejmcr.2025.100266","DOIUrl":"10.1016/j.ejmcr.2025.100266","url":null,"abstract":"<div><div>Multivalent glycoconjugates are critical tools for elucidating lectin interactions and for designing inhibitors that target lectin-mediated biological processes. In this study, pentavalent <em>N</em>-acetylglucosamine (GlcNAc) carbosilane dendrimers (<strong>1a</strong>∼<strong>1c</strong>) were synthesized and efficiently isolated as intermediates during the production of hexavalent GlcNAc carbosilane dendrimers (<strong>2a</strong>∼<strong>2c</strong>) using recycling gel permeation chromatography. Although these pentavalent glycodendrimers were previously separable, they had not been thoroughly characterized. Here, their binding interactions with wheat germ agglutinin (WGA) were examined via fluorometric titration assays, revealing comparable binding affinities to those of their hexavalent counterparts. Statistical analysis further demonstrated significant differences in binding behavior between pentavalent and hexavalent glycodendrimers, as well as the effects of spacer length on lectin interactions. These findings show that partial glycosylation retains strong lectin-binding capacity and provide new insights into the interplay among valency, spacer length, and the overall architecture of glycodendrimers in glycan–lectin interactions.</div></div>","PeriodicalId":12015,"journal":{"name":"European Journal of Medicinal Chemistry Reports","volume":"14 ","pages":"Article 100266"},"PeriodicalIF":0.0,"publicationDate":"2025-04-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143799767","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
1,3,4-Oxadiazole-based EGFR inhibitors as anticancer therapeutics: SAR study and binding mode of interaction analysis 1,3,4-恶二唑基EGFR抑制剂作为抗癌药物:SAR研究和相互作用的结合模式分析
European Journal of Medicinal Chemistry Reports Pub Date : 2025-04-06 DOI: 10.1016/j.ejmcr.2025.100265
Ajeya Samanta , Avik Maji , Abhik Paul , Sai Satyaprakash Mishra , Sourin Nahar , Tapan Kumar Maity
{"title":"1,3,4-Oxadiazole-based EGFR inhibitors as anticancer therapeutics: SAR study and binding mode of interaction analysis","authors":"Ajeya Samanta ,&nbsp;Avik Maji ,&nbsp;Abhik Paul ,&nbsp;Sai Satyaprakash Mishra ,&nbsp;Sourin Nahar ,&nbsp;Tapan Kumar Maity","doi":"10.1016/j.ejmcr.2025.100265","DOIUrl":"10.1016/j.ejmcr.2025.100265","url":null,"abstract":"<div><div>In recent years, cancer has emerged as a significant challenge to the healthcare system, and medicinal researchers are tirelessly working to develop new potential medications to combat this disease. Despite the progress in the diagnosis of the pathophysiology of cancer and several treatment options, it is still the leading cause of death in the 21st century. Researchers have explored numerous molecular targets of cancer, including various protein kinases, phosphatases, and proteins regulating cell cycle and apoptosis. In the meantime, tyrosine kinases (TKs) have evolved as the key enzymes involved in the pathogenesis of solid tumours. Among them, EGFR or ErbB1 has been implicated in several cancers like cancer of the lungs, breast, cervical, liver, colorectal, etc. A fascinating approach to cancer treatment involves inhibiting the expression of EGFR or HER1 TK. The 1,3,4-oxadiazole scaffold is a crucial heterocycle that serves several medicinal roles, including cancer treatment. In the last decade, 1,3,4-oxadiazole hybrids have shown potential as anticancer agents by inhibiting EGFR expression and function. This study delves into the advancement of 1,3,4-oxadiazole-based EGFR inhibitors with SAR studies and their binding mode of interaction analysis. Overall, these results will prove to be a helpful and vital tool for medicinal chemists investigating and working with 1,3,4-oxadiazole-based EGFR inhibitors for anti-cancer action.</div></div>","PeriodicalId":12015,"journal":{"name":"European Journal of Medicinal Chemistry Reports","volume":"14 ","pages":"Article 100265"},"PeriodicalIF":0.0,"publicationDate":"2025-04-06","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143816483","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Nanostructures: An efficient drug delivery platform for therapy of multiple myeloma 纳米结构:治疗多发性骨髓瘤的有效药物输送平台
European Journal of Medicinal Chemistry Reports Pub Date : 2025-04-02 DOI: 10.1016/j.ejmcr.2025.100263
Teodora Eliana Petcov , Vadim V. Silberschmidt , Mădălina Andreea Pandele , Elena Alina Chiticaru , Mariana Ioniță , Marius Manole
{"title":"Nanostructures: An efficient drug delivery platform for therapy of multiple myeloma","authors":"Teodora Eliana Petcov ,&nbsp;Vadim V. Silberschmidt ,&nbsp;Mădălina Andreea Pandele ,&nbsp;Elena Alina Chiticaru ,&nbsp;Mariana Ioniță ,&nbsp;Marius Manole","doi":"10.1016/j.ejmcr.2025.100263","DOIUrl":"10.1016/j.ejmcr.2025.100263","url":null,"abstract":"<div><div>Recent advancements in the biomedical field, particularly in drug delivery technologies, have paved the way for novel approaches to the diagnosis and treatment of multiple myeloma, a hematological malignancy characterized by the clonal proliferation of plasma cells in the bone marrow. Conventional treatments often fail to provide long-term efficacy, leading to a need for more effective therapies. Nanoscale drug delivery platforms demonstrated their potential to facilitate superior drug targeting, reduce systemic toxicity, and enhance therapeutic efficacy by inhibiting the growth of tumor cells. This review aims to highlight the most important features of the nanostructures used for drug delivery and recent advances in several nanostructures, including liposomes, micelles, polymeric and inorganic nanoparticles, carbon-based nanostructures, DNA nanostructures for multiple myeloma, as well as quantum dots, and nanocomposites used to deliver the chemotherapeutic agents. Furthermore, it evaluates the efficacy and mechanisms of internalization of nanostructures as controlled delivery systems for anticancer drugs in the treatment of multiple myeloma. The current review goes one step further to elucidate the potential of nanotechnology to revolutionize multiple myeloma therapy through targeted drug delivery systems based on various nanostructures.</div></div>","PeriodicalId":12015,"journal":{"name":"European Journal of Medicinal Chemistry Reports","volume":"14 ","pages":"Article 100263"},"PeriodicalIF":0.0,"publicationDate":"2025-04-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143816482","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","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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