European Journal of Medicinal Chemistry最新文献

{"title":"Design, synthesis and biological evaluation of triazolothiadiazole derivatives as FSP1 inhibitors for sensitizing cancer cells to ferroptosis","authors":"Wenbin Liu ,&nbsp;Xiaoying Xie ,&nbsp;Haonan Zong ,&nbsp;Yaxu Li ,&nbsp;Yan Ding ,&nbsp;Zhe Liu ,&nbsp;Bingrui Wan ,&nbsp;Ting Xiao ,&nbsp;Feng Lv ,&nbsp;Chunlei Tang ,&nbsp;Lei Yu ,&nbsp;Ping Wang ,&nbsp;Zengwei Lai","doi":"10.1016/j.ejmech.2025.117737","DOIUrl":"10.1016/j.ejmech.2025.117737","url":null,"abstract":"<div><div>Ferroptosis suppressor protein 1 (FSP1) is a recently identified ferroptosis suppressor that functions independently of the glutathione peroxidase reductase 4 (GPX4)-mediated pathway. Mechanistically, FSP1 mitigates ferroptosis by catalyzing the reduction of ubiquinone to ubiquinol and vitamin K (VK) to hydroquinone, thereby reducing lethal lipid peroxidation through the neutralization of free radicals. In this study, we designed and synthesized 32 compounds to systematically explore their structure-activity relationship (SAR) with the aim of identifying potent and novel FSP1 inhibitors. Among these, compound <strong>39</strong>, a triazolothiadiazole derivative, exhibited the most significant inhibitory activity against FSP1, with an IC₅₀ value of 35 nM. In vitro cellular assays demonstrated that compound <strong>39</strong> markedly enhanced RSL3-induced lipid peroxide (LPO) accumulation and sensitized cancer cells from diverse tissue origins to RSL3-induced ferroptosis. Furthermore, by exploiting the FSP1-mediated reduction of VK, compound <strong>39</strong> effectively augmented ferroptosis in HT1080 cells pretreated with RSL3 and VK through its potent inhibition of FSP1 activity. To the best of our knowledge, this study represents the first pharmacochemical investigation dedicated to the systematic design and synthesis of FSP1 inhibitors. Collectively, our findings underscore the profound impact of compound <strong>39</strong> on tumor ferroptosis, providing a promising foundation for the development of FSP1 inhibitors as potential therapeutic agents in cancer treatment.</div></div>","PeriodicalId":314,"journal":{"name":"European Journal of Medicinal Chemistry","volume":"293 ","pages":"Article 117737"},"PeriodicalIF":6.0,"publicationDate":"2025-05-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143933041","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Discovery of novel triphenylphosphonium conjugated pleuromutilin with enhanced anti-MRSA effect and broaden antibacterial spectrum.","authors":"Bo Feng, Huabin Hu, Jin Xiang, Guangxu Wu, Zihao Zhu, Gao Zhang, Jie Zhang, Weidong Pan, Wenxuan Zhang, Tianlei Li, Song Wu","doi":"10.1016/j.ejmech.2025.117731","DOIUrl":"https://doi.org/10.1016/j.ejmech.2025.117731","url":null,"abstract":"Pleuromutilin, a diterpene fungal metabolite, serves as a privileged scaffold for antibiotic discovery. Improving its antibacterial activity and broadening its spectrum remain the primary objectives in developing novel pleuromutilin derivatives. To obtain an ideal candidate, a series of pleuromutilin analogues conjugated to the triphenylphosphonium cation (TPP⁺) were designed and synthesized. Among them, compound a5 demonstrated enhanced anti-MRSA potency and a broadened antibacterial spectrum compared to valnemulin and lefamulin, both in vitro and in vivo. Mechanistic studies revealed that a5 disrupts bacterial membranes and biofilms by elevating intracellular ROS levels—a mechanism distinct from conventional pleuromutilins, which primarily target ribosomal proteins. These findings position a5 as a promising lead compound for developing next-generation broad-spectrum antibacterial agents.","PeriodicalId":314,"journal":{"name":"European Journal of Medicinal Chemistry","volume":"118 1","pages":""},"PeriodicalIF":6.7,"publicationDate":"2025-05-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143933039","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Discovery of LC-SF-14, a selective dual inhibitor of SHP2 and FGFR for the treatment of FGFR2-driven gastric cancer","authors":"Lei Zheng ,&nbsp;Yuhan Wang ,&nbsp;Zheng Jiang ,&nbsp;Shiyan Chen ,&nbsp;Xiansheng Cao ,&nbsp;Xiaohao Huang ,&nbsp;Ruixiang Luo ,&nbsp;Lulu Zheng ,&nbsp;Qin Li ,&nbsp;Linglan Tu ,&nbsp;Jie Li ,&nbsp;Guang Liang ,&nbsp;Lingfeng Chen","doi":"10.1016/j.ejmech.2025.117745","DOIUrl":"10.1016/j.ejmech.2025.117745","url":null,"abstract":"<div><div>Src homology-2 domain-containing phosphatase 2 (SHP2) and fibroblast growth factor receptor 2 (FGFR2) are oncoproteins. Despite the tremendous progress achieved with SHP2 allosteric inhibitors, the efficacy of single-agent SHP2 inhibitor treatments has been shown to be suboptimal, based on recent clinical trial results. A previous study demonstrated the synergistic effect of the allosteric SHP2 inhibitor SHP099 and the FGFR inhibitor BGJ398, suggesting a potential combined targeted therapeutic option for cancer. In this study, we discovered a potent SHP2 and FGFR2 dual inhibitor, LC-SF-14, using a linked pharmacophore strategy and structural optimization. The active compound LC-SF-14 exhibited high inhibitory potency against both targets (71.6 nM and 8.9 nM, respectively) with a high degree of selectivity, as verified by kinase kinome and protein tyrosine phosphatase (PTP) enzyme profiling. LC-SF-14 effectively prevented the phosphorylation of FGFR2 and downstream signaling, resulting in tumor regression <em>in vivo</em>. These results indicate that the bifunctional molecule LC-SF-14, the first PTP- and receptor tyrosine kinase (RTK)-targeted dual inhibitor, is a promising lead for the treatment of cancers bearing SHP2 and FGFR oncogenic drivers.</div></div>","PeriodicalId":314,"journal":{"name":"European Journal of Medicinal Chemistry","volume":"294 ","pages":"Article 117745"},"PeriodicalIF":6.0,"publicationDate":"2025-05-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143933117","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Discovery and optimization of 2-pyridones as dual h-DHFR/EGFRTK inhibitors with immunomodulatory potential; design, synthesis, anti-proliferative activity, and apoptosis inducer","authors":"Ahmed Ragab ,&nbsp;Reham R. Raslan ,&nbsp;Moustafa S. Abusaif ,&nbsp;Hamdy Khamees Thabet ,&nbsp;Yousry A. Ammar ,&nbsp;Nirvana A. Gohar","doi":"10.1016/j.ejmech.2025.117751","DOIUrl":"10.1016/j.ejmech.2025.117751","url":null,"abstract":"<div><div>Liver and colorectal cancers present considerable health challenges, underscoring the need to identify innovative targeted therapeutics. Tumor progression can be prevented by targeting EGFR-TK and <em>h</em>-DHFR as essential molecular targets. In this context, we synthesized a new series of 2-pyridones from the reaction of 2-cyanoacrylamide with active methylene or 2-cyanoacetanilide with activated double bonds under basic conditions. The structure of the synthesized 2-pyridones was confirmed through microanalysis and spectroscopic data. In comparison to doxorubicin, the spiro 2-pyridine derivative <strong>9b</strong> exhibited the highest anti-proliferative activity, demonstrating IC₅₀ values of 6.89 ± 0.4 μM and 5.68 ± 0.3 μM against HepG-2 and Caco-2 cell lines, respectively, with nearly 2-fold increase in efficacy observed in Caco-2 cells. Additionally, compound <strong>9b</strong> demonstrated a significant safety profile concerning normal cells (WI-38), as indicated by selectivity index values of 14.66 and 12.09 against the Caco-2 and HepG-2 cell lines, respectively. Moreover, flow cytometry analysis revealed that compound <strong>9b</strong> halted the cell cycle at the G1/S phase in Caco-2 treated cells, demonstrating an increase in the percentage of cells undergoing both early and late apoptosis. The apoptotic potential was corroborated by the up-regulation of BAX and the down-regulation of Bcl-2 levels. Compound <strong>9b</strong> exhibited significant inhibitory activity against <em>h</em>-DHFR, with an IC₅₀ value of 0.192 ± 0.011 μM, compared to methotrexate (IC₅₀ = 0.191 ± 0.011 μM). Furthermore, compound <strong>9b</strong> demonstrated EGFR inhibitory activity, with IC₅₀ of 0.109 ± 0.005 μM, which is close to the inhibition observed with Lapatinib (IC₅₀ = 0.044 ± 0.002 μM). Compound <strong>9b</strong> had better immunomodulatory properties with significant inhibitory efficacy on TNF-α and IL-6, with IC₅₀ values of 0.40 ± 0.03 pg/mL and 0.60 ± 0.02 pg/mL, respectively. These values indicate a greater potency than the positive control drug Lapatinib, which displayed IC₅₀ values of 0.41 ± 0.03 pg/mL and 0.74 ± 0.05 pg/mL for TNF-α and IL-6, respectively. In addition, in silico metabolism prediction using SwissADME and BioTransformer tools revealed that compound <strong>9b</strong> is a potential inhibitor of CYP2C9 and CYP3A4, and is predicted to undergo metabolic transformations primarily via aromatic hydroxylation and ketone reduction, while maintaining acceptable stability of its ester moiety. Finally, the molecular docking assessment, together with the direct in vitro enzymatic inhibition results, confirmed that the 2-pyridone derivative <strong>9b</strong> can potently bind to and inhibit both EGFR and h-DHFR through favorable binding interactions.</div></div>","PeriodicalId":314,"journal":{"name":"European Journal of Medicinal Chemistry","volume":"294 ","pages":"Article 117751"},"PeriodicalIF":6.0,"publicationDate":"2025-05-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143932585","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Therapeutic potential of dual HDAC6/SIRT2 inhibition in Alzheimer's disease","authors":"Xingyu Wang ,&nbsp;Cunjiang Li ,&nbsp;Lei Chen ,&nbsp;Bin He ,&nbsp;Yan Li","doi":"10.1016/j.ejmech.2025.117733","DOIUrl":"10.1016/j.ejmech.2025.117733","url":null,"abstract":"<div><div>Alzheimer's disease (AD) is a progressive neurodegenerative disorder characterized by hallmark pathological changes such as amyloid β (Aβ) plaques, neurofibrillary tangles (NFTs) due to tau hyperphosphorylation, and neuroinflammation. Current therapeutic approaches focusing on single-target strategies exhibit limited efficacy, necessitating the exploration of novel multi-target approaches. Histone deacetylase 6 (HDAC6) and SIRT2, as two types of cytosolic histone deacetylases, have emerged as promising targets for AD treatment. HDAC6 plays a role in tau protein phosphorylation, while SIRT2 is involved in Aβ production. Both enzymes regulate microtubule proteins, impacting the formation of NFTs and Aβ plaques. Inhibition of HDAC6 reduces tau hyperphosphorylation, improves microtubule stability, and mitigates neuroinflammation, whereas SIRT2 inhibition attenuates Aβ accumulation and neuroinflammation. Recent studies indicate that dual-targeted inhibition of HDAC6 and SIRT2 may exhibit synergistic effects, suggesting it as a promising strategy for AD treatment. This review summarizes the biological roles of HDAC6 and SIRT2 in AD pathology and examines the development of dual-target inhibitors. It also discusses the challenges, including selectivity and toxicity, emphasizing that the development of combined HDAC6 and SIRT2 inhibitors represents a new direction for future AD treatment.</div></div>","PeriodicalId":314,"journal":{"name":"European Journal of Medicinal Chemistry","volume":"294 ","pages":"Article 117733"},"PeriodicalIF":6.0,"publicationDate":"2025-05-09","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143931270","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Rationally designed Pyrazolo[1,5-a]pyrimidines as dual inhibitors of CA IX/XII and CDK6: A novel approach for NSCLC treatment","authors":"Mahmoud S. Elkotamy ,&nbsp;Islam A. Elkelesh ,&nbsp;Simone Giovannuzzi ,&nbsp;Rania S.M. Ismail ,&nbsp;Wessam M. El-Refaie ,&nbsp;Abdulrahman A. Almehizia ,&nbsp;Ahmed M. Naglah ,&nbsp;Alessio Nocentini ,&nbsp;Claudiu T. Supuran ,&nbsp;Mohamed Fares ,&nbsp;Hazem A. Ghabbour ,&nbsp;Rofaida Salem ,&nbsp;Wagdy M. Eldehna ,&nbsp;Hatem A. Abdel-Aziz","doi":"10.1016/j.ejmech.2025.117752","DOIUrl":"10.1016/j.ejmech.2025.117752","url":null,"abstract":"<div><div>Developing novel anticancer agents that target critical pathways in non-small cell lung cancer (NSCLC) presents a considerable challenge. This study synthesized 16 pyrazolo[1,5-<em>a</em>]pyrimidine derivatives with zinc-binding groups through molecular hybridization to achieve dual-target inhibition of tumor-associated carbonic anhydrase (CA) isoforms IX/XII and cyclin-dependent kinase 6 (CDK6). <em>In-vitro</em> assays indicated that sulfonamide-bearing compounds displayed enhanced CA inhibition, with compounds <strong>7d</strong>, <strong>11b</strong>, and <strong>11d</strong> presenting K_i values of 11.2, 18.4, and 19.7 nM for CA IX, while compounds <strong>11a</strong> and <strong>11c</strong> exhibited K_i values of 14.8 and 8.7 nM for CA XII. Cytotoxicity assays conducted on NSCLC cell lines A549 and NCI–H1734 demonstrated that compounds <strong>7c</strong>, <strong>7d</strong>, <strong>7i</strong>, and <strong>11d</strong> exhibited superior activity relative to <strong>Roscovitine</strong> in both cell lines. While these compounds demonstrated limited inhibition of cyclin-dependent kinase 4 (CDK4), <strong>7d</strong> and <strong>11d</strong> effectively inhibited CDK6, with IC₅₀ values of 0.054 and 0.069 μM, respectively, which are comparable to <strong>Palbociclib</strong>. Analyses of the cell cycle and apoptosis demonstrated a strong G1 arrest and a notable induction of apoptosis. Molecular docking confirmed essential binding interactions with CA IX/XII and CDK6, while <em>in-silico</em> ADMET predictions suggested favorable pharmacokinetics, despite potential toxicity concerns. Compounds <strong>7d</strong> and <strong>11d</strong> represent potential dual-target inhibitors for the treatment of NSCLC.</div></div>","PeriodicalId":314,"journal":{"name":"European Journal of Medicinal Chemistry","volume":"293 ","pages":"Article 117752"},"PeriodicalIF":6.0,"publicationDate":"2025-05-09","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143927151","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Identification of isoxazole-based TRPA1 inhibitors with analgesic effects in vivo","authors":"Valentina Albanese ,&nbsp;Matilde Marini ,&nbsp;Martina Tesi ,&nbsp;Lorenzo Landini ,&nbsp;Elisa Bellantoni ,&nbsp;Sandro Cosconati ,&nbsp;Michele Roggia ,&nbsp;Lorenzo Tagliazucchi ,&nbsp;Lorenzo Gnudi ,&nbsp;Valentina Puscio ,&nbsp;Chiara Sturaro ,&nbsp;Chiara Ruzza ,&nbsp;Remo Guerrini ,&nbsp;Pierangelo Geppetti ,&nbsp;Romina Nassini ,&nbsp;Delia Preti ,&nbsp;Francesco De Logu ,&nbsp;Salvatore Pacifico","doi":"10.1016/j.ejmech.2025.117732","DOIUrl":"10.1016/j.ejmech.2025.117732","url":null,"abstract":"<div><div>The transient receptor potential ankyrin 1 (TRPA1) channel has been extensively studied as a potential therapeutic target for the treatment of different pain types, with better efficacy and safety profiles compared to current therapies. Because TRPA1 is implicated in different pathophysiological processes, selective antagonists of this channel could provide therapeutic benefits beyond pain relief. In this study, we report the design and synthesis of a novel series of carboxamide derivatives incorporating an isoxazole moiety, which were evaluated for their ability to inhibit TRPA1-mediated signalling. Among these, we identified the TRPA1 antagonists <strong>12</strong> and <strong>13</strong> displaying nanomolar potency <em>in vitro</em> and significant analgesic effects against the TRPA1 agonist, allyl isothiocyanate and in the formalin test in mice. Docking analyses were also conducted to explore the binding modes of the most representative compounds with the proposed pharmacological target.</div></div>","PeriodicalId":314,"journal":{"name":"European Journal of Medicinal Chemistry","volume":"294 ","pages":"Article 117732"},"PeriodicalIF":6.0,"publicationDate":"2025-05-09","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143927071","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Beyond the classical chiral resolution: Modern enantioselective synthetic strategies used in the preparation of new chiral kinase inhibitors including drugs for autoimmune diseases and antitumoral drugs","authors":"Cesar Emiliano Hoffmann da Silva ,&nbsp;Grace Gosmann ,&nbsp;Rafael Roesler ,&nbsp;Marcela Silva Lopes ,&nbsp;Saulo Fernandes de Andrade","doi":"10.1016/j.ejmech.2025.117730","DOIUrl":"10.1016/j.ejmech.2025.117730","url":null,"abstract":"<div><div>Kinase inhibitors is one of the most approved class by FDA in this century. These proteins are versatile targets that have a huge impact in several pharmacotherapy including against cancer, autoimunne and rare diseases. Thus, the number of patents that aim these targets are increasing and is becoming harder to be innovative in this field. Furthermore, the design of ATP-competitive inhibitors is the major strategy used to develop new kinase inhibitors and there are few regions in the ATP cleft or around it, which are generally explored by the commercially available inhibitor drugs. In this way in this review, we focused in the use of modern enantioselective strategies that were carried out in the last years to prepare new chiral kinase inhibitors as an emerging field that resulted in several new potent innovative approved drugs. Also we suggested new trends in this modern relevant topic and analyzed kinase-drug complexes highlighting the interactions that support the importance of the stereochemistry.</div></div>","PeriodicalId":314,"journal":{"name":"European Journal of Medicinal Chemistry","volume":"293 ","pages":"Article 117730"},"PeriodicalIF":6.0,"publicationDate":"2025-05-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143920569","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Discovery of 3-methacylic acid substituted benzoxaboroles as dual metallo- and serine-β-lactamase inhibitors","authors":"Guo-Qing Liang,&nbsp;Ying-Ying Jiang,&nbsp;Cheng-Long Han,&nbsp;Yao Wang,&nbsp;Si-Yao Wang,&nbsp;Yi-Ting Chen,&nbsp;Gen Li,&nbsp;Guo-Bo Li,&nbsp;You-Cai Xiao","doi":"10.1016/j.ejmech.2025.117723","DOIUrl":"10.1016/j.ejmech.2025.117723","url":null,"abstract":"<div><div>Carbapenem resistance is an ongoing clinical problem, largely driven by production of evolved serine β-lactamases (SBLs) and metallo-β-lactamases (MBLs). We here report a series of new 3-methacrylic acid-substituted benzoxaboroles as dual MBL/SBL inhibitors. Structure-activity relationship studies showed that the new compounds manifested nanomolar inhibition to the SBLs KPC-2 and OXA-48, and single-digit micromolar inhibition to the MBLs VIM-2, NDM-1, and NDM-5. Co-crystallographic analyses revealed their binding modes with VIM-2 and OXA-48, which are similar as those of taniborbactam and xeruborbactam. Bacterial assays demonstrated that compound <strong>10</strong> can potentiate meropenem against multidrug-resistant Gram-negative strains. This work provides new lead compounds and structural basis for developing new drug candidates against MBL/SBL-mediated carbapenem resistance.</div></div>","PeriodicalId":314,"journal":{"name":"European Journal of Medicinal Chemistry","volume":"293 ","pages":"Article 117723"},"PeriodicalIF":6.0,"publicationDate":"2025-05-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143927153","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Corrigendum to “Design and synthesis of novel styrylquinolinium derivatives for the treatment of breast cancer: Targeting the c-Myc G-Quadruplex” [Europ. J. Med. Chem. 291 (2025) 117663]","authors":"Xutong Wang, Yu Liu, Zeyu Gao, Xiaodong Fang, Kejing Ma, Meng Sun, Qiming Li, Bing Wang, Yong Zhang, Xin Zhao, Weina Han","doi":"10.1016/j.ejmech.2025.117719","DOIUrl":"https://doi.org/10.1016/j.ejmech.2025.117719","url":null,"abstract":"The authors regret that during the post-publication review showed that the Western Blot bands in <span><span>Fig. 11</span></span>D were pasted incorrectly, which was caused by the mismatch of file versions during the revision process. Corrected <span><span>Fig. 11</span></span> are listed below.<span><figure><span><img alt=\"Fig. 11\" aria-describedby=\"cap0010\" height=\"509\" src=\"https://ars.els-cdn.com/content/image/1-s2.0-S0223523425004842-fx1.jpg\"/><ol><li><span><span>Download: <span>Download high-res image (1MB)</span></span></span></li><li><span><span>Download: <span>Download full-size image</span></span></span></li></ol></span><span><span><p><span>Fig. 11</span>. Evaluation of the anticancer activity of <strong>W11</strong> in human breast cancer xenografts. (A) Digital photos of mice in the control group, drug-treated group and positive control group on the 21st day of treatment. (B) Digital photos and average weight data of tumor tissue samples. (C) Fluorescence imaging of live animals in the control group, drug-treated group, and positive control group after 21 days of treatment. (D) Expression of c-Myc protein in tumor tissues of the control group, drug-treated group and positive control group after 21 days of treatment. (N ≥ 4; mean ± SD; (∗) <em>P</em> &lt; 0.05, (∗∗) <em>P</em> &lt; 0.01, and (∗∗∗) <em>P</em> &lt; 0.001, significantly different from the control; ns, not significantly different from the control).</p></span></span></figure></span>","PeriodicalId":314,"journal":{"name":"European Journal of Medicinal Chemistry","volume":"25 1","pages":"117719"},"PeriodicalIF":6.7,"publicationDate":"2025-05-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143927152","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}