Archiv der Pharmazie最新文献

{"title":"Current Landscape of Hydroxamic Acid Hybrids With Anti-Colorectal Cancer Potential","authors":"Yanjing Cheng,&nbsp;Yafei Zhuang,&nbsp;Ni Zhu,&nbsp;You Yu,&nbsp;Meichun Hu","doi":"10.1002/ardp.70066","DOIUrl":"https://doi.org/10.1002/ardp.70066","url":null,"abstract":"<div>\u0000 \u0000 <p>Colorectal cancer, also referred to as colon cancer, is a malignant tumor originating from the inner lining of the rectum or colon, the longest segment of the large intestine. As one of the most prevalent digestive system cancers globally, colorectal cancer ranks third among all cancers worldwide, comprising approximately 10% of all new cancer cases, and poses a serious threat to human life and health. Hydroxamic acid hybrids as potential histone deacetylase (HDAC) inhibitors could exert anti-colorectal cancer effects through multiple interconnected pathways, primarily targeting key molecular and cellular processes involved in tumor growth, progression, and metastasis. Moreover, hydroxamic acid hybrids can simultaneously target two or more distinct cancer sites, thereby potentially enhancing therapeutic efficacy, overcoming drug resistance, improving pharmacokinetic properties, and minimizing side effects. This review outlines the current landscape of hydroxamic acid hybrids with potential anti-colorectal cancer properties, developed from 2020 to the present, aiming to open new avenues for exploring novel candidates.</p></div>","PeriodicalId":128,"journal":{"name":"Archiv der Pharmazie","volume":"358 7","pages":""},"PeriodicalIF":4.3,"publicationDate":"2025-07-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144716999","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Structure-Driven Mechanisms and Synergistic Approaches of Polyphyllin VII in Breast Cancer Therapy","authors":"Alaa O. Hamouda,&nbsp;Nadin H. Sarg,&nbsp;Sara I. Ibrahim,&nbsp;Rania Hamdy,&nbsp;Sameh S. M. Soliman,&nbsp;Hany A. Omar","doi":"10.1002/ardp.70064","DOIUrl":"https://doi.org/10.1002/ardp.70064","url":null,"abstract":"<div>\u0000 \u0000 <p>Polyphyllin VII (PP7), a natural saponin derived from the rhizomes of <i>Paris polyphylla</i> (family: Melanthiaceae), possesses a unique steroidal furostane structure that contributes to its versatile pharmacological profile. It is traditionally used in Chinese medicine for treating pain, insect bites, and bleeding. PP7's unique pharmacophoric features and optimal lipophilic–hydrophilic balance underlie its diverse anticancer therapeutic actions, including cell cycle arrest, apoptosis, ferroptosis, and autophagy activation, alongside metastasis and angiogenesis inhibition. PP7 has gained attention for its potent bioactivity in breast cancer and other pathological conditions. In breast cancer, PP7 demonstrates remarkable efficacy, addressing not only tumor growth but also associated complications such as inflammation and osteoporosis. Additionally, PP7 exhibits synergistic effects with chemotherapeutic agents like cisplatin, bortezomib, and gefitinib, enhancing cancer cell apoptosis and mitigating drug resistance. Beyond its anticancer properties, PP7 also displays broad pharmacological activities, including anti-inflammatory, hepatoprotective, and antimicrobial effects. Thus, PP7 holds significant potential for therapeutic application across breast cancer patients with comorbidities. However, further research is necessary to clarify its specific role in breast cancer subtypes, ensure its safety in clinical applications, and optimize its broad-scale biosynthesis. This review highlights the structure-driven mechanisms underlying PP7 actions and its therapeutic potential as a standalone agent or adjunct in breast cancer therapy.</p></div>","PeriodicalId":128,"journal":{"name":"Archiv der Pharmazie","volume":"358 7","pages":""},"PeriodicalIF":3.6,"publicationDate":"2025-07-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144725715","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"5(6)-Benzoyl-Substituted Benzimidazoles and Their Benzimidazolium Salts: Design, Synthesis, Characterization, Crystal Structure, and Some Metabolic Enzymes Inhibition Properties","authors":"Aydın Aktaş,&nbsp;Eda Mehtap Özden,&nbsp;Duygu Barut Celepci,&nbsp;Tugba Taskin-Tok,&nbsp;Funda Sultan Ekti,&nbsp;İlhami Gülçin,&nbsp;Muhittin Aygün,&nbsp;Yetkin Gök,&nbsp;İlhami Çelik","doi":"10.1002/ardp.70063","DOIUrl":"https://doi.org/10.1002/ardp.70063","url":null,"abstract":"<div>\u0000 \u0000 <p>Herein, the synthesis of 1-alkyl-5(6)-benzoyl-substituted benzimidazoles and their 1,3-bisalkylbenzimidazolium halide salts are presented and evaluated for some metabolic enzyme inhibition. All compounds were characterized using various spectroscopic techniques. Single-crystal XRD analysis was performed to determine the molecular structure of two compounds. The newly synthesized compounds exhibited significant inhibitory effects against acetylcholinesterase (AChE) and human carbonic anhydrase isoforms I and II (hCA I and hCA II) enzymes. These compounds demonstrated promising inhibition profiles, with <i>K</i>_i values ranging from 12.4 ± 5.4 to 109.4 ± 49.9 nM for hCA I, 23.1 ± 11.2 to 115.0 ± 17.9 nM for hCA II, and 0.7 ± 0.3 to 4.4 ± 1.0 nM for AChE. In comparison, the reference compound acetazolamide showed <i>K</i>_i values of 30.5 ± 6.7 nM and 37.4 ± 7.8 nM against hCA I and hCA II isoenzymes, respectively. Additionally, tacrine, a known AChE inhibitor, exhibited a <i>K</i>_i value of 5.1 ± 2.7 nM. The dual inhibition of CA and AChE represents a valuable pharmacological approach with a wide range of therapeutic applications. The explanation and evaluation of the enzyme inhibition data obtained in line with the interactions of the synthesized compounds with hCA I, hCA II, and AChE enzymes were carried out by molecular docking studies. In particular, we focused on the three compounds (<b>4e</b>, <b>4f</b>, and <b>4j</b> for hCA I; <b>3g</b>, <b>4f</b>, and <b>4k</b> for hCA II; and <b>4e</b>, <b>4f</b>, <b>4j</b>, and <b>4l</b> for AChE) with the highest potential activity with each enzyme. The physicochemical, ADME, drug-likeness, medicinal chemistry, and toxicity properties of the potential ligands were then predicted so that their drug candidate suitability for further studies is revealed.</p></div>","PeriodicalId":128,"journal":{"name":"Archiv der Pharmazie","volume":"358 7","pages":""},"PeriodicalIF":3.6,"publicationDate":"2025-07-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144725714","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Recent Advances in 1,2,4-Triazole-Based Anticancer Agents: Structural Optimization, Mechanisms, and Therapeutic Potential (2022–2025)","authors":"Nafeesa Naeem,&nbsp;Ehsan Ullah Mughal,&nbsp;Amina Sadiq,&nbsp;Gehan Ahmed Othman,&nbsp;Bushra Shakoor","doi":"10.1002/ardp.70059","DOIUrl":"https://doi.org/10.1002/ardp.70059","url":null,"abstract":"<div>\u0000 \u0000 <p>The 1,2,4-triazole scaffold has emerged as a privileged heterocyclic core in the development of anticancer agents due to its unique physicochemical properties, bioavailability, and diverse biological activities. Over the past few years, significant advancements have been made in the design and structural optimization of 1,2,4-triazole-based anticancer compounds, with a strong focus on their structure–activity relationships (SARs). This review provides a comprehensive overview of the latest developments (2022–2025) in 1,2,4-triazole-containing anticancer agents, emphasizing their mechanisms of action, molecular targets, and therapeutic potential. The discussion encompasses the various modifications introduced into the 1,2,4-triazole core, exploring their impact on anticancer efficacy, selectivity, and pharmacokinetic properties. In particular, recent studies have highlighted the ability of these derivatives to inhibit key cancer-related enzymes (such as kinases, carbonic anhydrases, and topoisomerases), interfere with DNA interactions, and modulate apoptotic and autophagic pathways. This review also presents emerging SAR trends, highlighting key functional group modifications that enhance anticancer potency while minimizing off-target effects. Furthermore, recent <i>in vivo</i> studies and clinical evaluations of promising 1,2,4-triazole derivatives are discussed to assess their translational potential. Lastly, we outline future research directions and challenges in the development of next-generation triazole-based anticancer agents, aiming to bridge the gap between rational drug design and clinical application. This comprehensive analysis underscores the critical role of the 1,2,4-triazole pharmacophore in anticancer drug discovery and provides valuable insights for the design of more potent and selective anticancer therapeutics.</p></div>","PeriodicalId":128,"journal":{"name":"Archiv der Pharmazie","volume":"358 7","pages":""},"PeriodicalIF":4.3,"publicationDate":"2025-07-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144717000","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Design and Synthesis of Ketoconazole Derivatives as Innovative Anti-Infective Agents","authors":"Gioele Renzi,&nbsp;Andrea Angeli,&nbsp;Silvia Selleri,&nbsp;Costanza Spadini,&nbsp;Nicolo’ Mezzasalma,&nbsp;Marcus T. Hull,&nbsp;Steven L. Kelly,&nbsp;Clemente Capasso,&nbsp;Clotilde S. Cabassi,&nbsp;Fabrizio Carta,&nbsp;Claudiu T. Supuran","doi":"10.1002/ardp.70062","DOIUrl":"https://doi.org/10.1002/ardp.70062","url":null,"abstract":"<p>A novel series of compounds was designed and synthesized by combining the distal piperazine nitrogen of the antifungal ketoconazole (KTZ) with primary arylsulfonamides. The aim of this study is to present the basis for a new generation of <i>Malassezia</i> antifungal agents able to inhibit the enzyme lanosterol-14α-demethylase (CYP51; EC 1.14.13.70) as well as a newly emergent therapeutic target: carbonic anhydrases (CAs; EC 4.2.1.1). The final compounds showed effective interactions with the intended targets in vitro, as well as KTZ comparable minimum inhibitory concentrations on yeast strains of the <i>Malassezia</i> genus: <i>Malassezia furfur</i> ATCC 14521; <i>Malassezia globosa</i> ATCC MYA 4612; and <i>Malassezia pachydermatis</i> DSM 6172. Overall, the data obtained account for the reported compounds as promising antifungal candidates with high safety profiles for the management of fungal infections.</p>","PeriodicalId":128,"journal":{"name":"Archiv der Pharmazie","volume":"358 7","pages":""},"PeriodicalIF":4.3,"publicationDate":"2025-07-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://onlinelibrary.wiley.com/doi/epdf/10.1002/ardp.70062","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144716998","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Promising Antimycobacterial Agents: Salicylidenehydrazines","authors":"Oya Unsal Tan,&nbsp;Sıva Krıshna Vagolu,&nbsp;Tone Tønjum,&nbsp;Ozan Kaplan,&nbsp;Rahime Simsek","doi":"10.1002/ardp.70065","DOIUrl":"https://doi.org/10.1002/ardp.70065","url":null,"abstract":"<div>\u0000 \u0000 <p>Tuberculosis (TB) remains a major global health challenge, underscoring the urgent need for new therapeutic options. In this study, a series of salicylidenehydrazine derivatives were synthesized and characterized using spectroscopic techniques. Their antimycobacterial activity was assessed against <i>Mycobacterium tuberculosis</i> H37Rv. Among the 35 synthesized compounds, nine demonstrated significant inhibitory activity, with MIC values ranging from 0.78 to 50 μM. These active molecules were further evaluated against clinical isoniazid-resistant (bearing <i>inhA</i> promoter and/or <i>katG</i> mutations) and multidrug-resistant (MDR) <i>M. tuberculosis</i> strains. A particularly potent compound derived from 2-bromo-4-nitrosalicylaldehyde exhibited an MIC of 0.78 μM against H37Rv and demonstrated low MIC values of 6.25, 1.56, and 1.56 μM against the <i>inhA</i> + , <i>katG</i> + , and MDR strains, respectively. Molecular docking studies were also conducted to investigate the interaction of active compounds with the target enzyme InhA. Overall, the results indicate that salicylidenehydrazine derivatives represent promising lead structures for the development of new anti-TB agents effective against both drug-sensitive and drug-resistant <i>M. tuberculosis</i> strains.</p></div>","PeriodicalId":128,"journal":{"name":"Archiv der Pharmazie","volume":"358 7","pages":""},"PeriodicalIF":4.3,"publicationDate":"2025-07-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144717002","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Revealing a Gold Mine of Bioactive Compounds From Natural Sources Using In Vitro, In Silico, and Network Pharmacology: A Case Study on Cachrys cristata","authors":"Inci Kurt-Celep,&nbsp;Shakeel Ahmed,&nbsp;Mehmet Veysi Cetiz,&nbsp;Abdullahi Ibrahim Uba,&nbsp;Gunes Ak,&nbsp;Selami Selvi,&nbsp;Ahmet Emir,&nbsp;Stefano Dall'Acqua,&nbsp;Gokhan Zengin","doi":"10.1002/ardp.70057","DOIUrl":"https://doi.org/10.1002/ardp.70057","url":null,"abstract":"<div>\u0000 \u0000 <p>The study aimed to explore the chemical composition and assess the wide-ranging biological effects of <i>Cachrys cristata</i> extracts, including ethyl acetate, ethanol, ethanol/water (70%), and water. We evaluated the bioactive potential of these extracts by different chemical techniques such as radical scavenging, reducing power, and metal chelation assays. Additionally, we conducted enzyme inhibition assays to target cholinesterase, tyrosinase, amylase, glucosidase, elastase, collagenase, and hyaluronidase. In the profile analysis, we determined that the main components are phenolic acids, mainly caffeic acid with the highest concentrations. The water extract of the plant showed the highest concentration of phytochemicals and superior antioxidant activity. In addition, the ethanol and ethyl acetate extracts showed the greatest level of inhibition of most of the evaluated enzymes. On the other hand, its potential protective effects against UV-induced oxidative stress, genotoxicity, and extracellular matrix (ECM) degradation were investigated. Different extracts of the plant were evaluated in terms of their effects on DNA damage, cellular viability, ECM enzymes, and matrix metalloproteinases (MMPs). COMET analysis showed that DNA breaks and genotoxicity caused by UV rays were significantly suppressed, especially by the water extract. Furthermore, network pharmacology analyses, in conjunction with in silico molecular docking and molecular dynamics simulations, demonstrated robust ligand–protein interactions and furnished insights into the underlying mechanisms, thereby substantiating the plant's therapeutic potential. Overall, our research highlights the significant potential of <i>C. cristata</i> as a valuable reservoir of bioactive chemicals that can be utilized in the health and wellness industries.</p></div>","PeriodicalId":128,"journal":{"name":"Archiv der Pharmazie","volume":"358 7","pages":""},"PeriodicalIF":4.3,"publicationDate":"2025-07-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144717001","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Design, Synthesis, and Biological Evaluation of Triazole Tethered Coumarin-Indole Fused Chalcone-Isatin Derivatives as a New Class of Anti-Breast Cancer Agents","authors":"Jasreen Kaur Uppal,&nbsp;Rajiv Sharma","doi":"10.1002/ardp.70060","DOIUrl":"https://doi.org/10.1002/ardp.70060","url":null,"abstract":"<div>\u0000 \u0000 <p>Inspired by the anti-breast cancer and anti-tubulin potential of coumarin, indole, chalcone, and isatin moieties, a new series of triazole-tethered coumarin-fused chalcone and isatin hybrids were designed, synthesized, and evaluated for their anti-breast cancer activities. Among the series of hybrid compounds, JKUB2 showed the strongest activity against MCF-7 breast cancer cells with an IC₅₀ value of 1.28 µM. JKUB2 exhibited tubulin polymerization inhibition potential (IC₅₀ = 1.31 µM) and induced apoptosis in breast cancer cells by arresting the cell cycle at the G2/M phase. Apart from that, JKUB2 showed higher selectivity (selectivity index: 6.36) toward MCF-7 cells over normal skin fibroblast cells (L929). Morphological studies further confirmed the capability of JKUB2 to induce cell death via apoptotic pathways. Molecular docking and dynamics simulations studies confirmed the desired interactions of JKUB2 in the colchicine binding site of microtubules, responsible for their polymerization inhibition. Overall, the study represents JKUB2 as a potential anti-breast cancer agent that acts via tubulin polymerization inhibition and induces cell death by apoptotic pathways, and warrants further research as well as acts as an effective hit lead for further development of potent and safer anti-breast cancer agents.</p></div>","PeriodicalId":128,"journal":{"name":"Archiv der Pharmazie","volume":"358 7","pages":""},"PeriodicalIF":4.3,"publicationDate":"2025-07-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144717003","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Substituted D-Galactose-Conjugated Thiazole-Thioureas Derivatives as Promising Antidiabetic Agents: Synthesis, In Vitro Inhibition, and Molecular Simulation for α-Amylase, α-Glucosidase, Protein Glycation, and Oxidative Stress","authors":"Nguyen Dinh Thanh,&nbsp;Vu Ngoc Toan,&nbsp;Duong Ngoc Toan,&nbsp;Vu Minh Trang","doi":"10.1002/ardp.70039","DOIUrl":"https://doi.org/10.1002/ardp.70039","url":null,"abstract":"<div>\u0000 \u0000 <p>A thiourea series (<b>7a–l</b>) containing 4-arylthiazoles and the <span>d</span>-galactose moiety were synthesized and explored for their multi-target inhibition against α<i>-</i>amylase from porcine pancreas and α<i>-</i>glucosidase from <i>Saccharomyces cerevisiae</i>. Among these thioureas, <b>7h</b> was the most potent inhibitor for α-amylase (IC₅₀ of 7.84 ± 0.14 μM) and <b>7c</b> was the most potent inhibitor for α-glucosidase (IC₅₀ of 7.15 ± 0.12 μM). These thioureas also exhibited anti-glycation and antioxidant activity. They were noncytotoxic for NIH-3T3 cells. Induced-fit molecular docking study was applied to the two most potential inhibitors <b>7c</b> and <b>7h</b>. Their active interactions with residues in the catalytic pockets of the corresponding studied enzymes, 1OSE and 3TOP, were suitable to their inhibitory potentials against each tested enzyme. The molecular dynamics simulations validated the in vitro data for these compounds whereas the pharmacokinetics profile (ADMET) revealed the druglike properties of potent inhibitors.</p></div>","PeriodicalId":128,"journal":{"name":"Archiv der Pharmazie","volume":"358 7","pages":""},"PeriodicalIF":4.3,"publicationDate":"2025-07-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144688089","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Isoxazole-Based Compounds Targeting the Taxane-Binding Site of Tubulin","authors":"Miroslav Peřina,&nbsp;Márton A. Kiss,&nbsp;Jakub Bělíček,&nbsp;Veronika Vojáčková,&nbsp;Denisa Veselá,&nbsp;Renáta Minorics,&nbsp;István Zupko,&nbsp;Éva Frank,&nbsp;Radek Jorda","doi":"10.1002/ardp.70031","DOIUrl":"https://doi.org/10.1002/ardp.70031","url":null,"abstract":"<p>Taxanes and other tubulin-targeting medications are essential for treating advanced malignancies, especially in patients undergoing less aggressive chemotherapy. However, their clinical efficacy is often limited by significant off-target toxicity and adverse side effects. In this study, the synthesis and characterisation of novel steroidal A-ring-fused isoxazoles, which were obtained through iodine-mediated oxidative cyclization of dihydrotestosterone (DHT)-derived α,β-unsaturated oximes, are reported. According to mechanistic studies, the most potent compounds induced mitotic arrest and disrupted cytoskeletal integrity at low micromolar concentrations. The lead compound, <b>2j</b>, notably increased the rate of tubulin polymerisation in vitro and stabilised polymerised tubulin in the cells, leading to a G2/M block of the cell cycle. Molecular docking studies indicated that <b>2j</b> is bound preferably to the taxane site on tubulin, forming conserved interactions. MicroScale Thermophoresis was used to further study this binding and showed a nanomolar <i>K</i>_D for <b>2j</b>. The fact that <b>2j</b> maintained its activity in docetaxel-resistant prostate cancer cells, demonstrating its ability to circumvent resistance pathways linked to existing therapies with taxane-like drugs, supports its clinical relevance. Therefore, our results encourage additional research and development for its potential therapeutic use in cancer treatment, particularly in resistant cases.</p>","PeriodicalId":128,"journal":{"name":"Archiv der Pharmazie","volume":"358 7","pages":""},"PeriodicalIF":4.3,"publicationDate":"2025-07-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://onlinelibrary.wiley.com/doi/epdf/10.1002/ardp.70031","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144688090","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}