Medicinal Chemistry Research最新文献

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Discovery of a novel selenamide derivative as potent activator of aldehyde dehydrogenase 2 for cardioprotective applications 发现一种新的selenamide衍生物,作为醛脱氢酶2的有效活化剂,用于心脏保护应用
IF 2.6 4区 医学
Medicinal Chemistry Research Pub Date : 2025-05-03 DOI: 10.1007/s00044-025-03415-3
Yi Yang, Yue Yao, Junyang Huang, Zhan Shi, Xicheng Wang, Wei Li, Yishu Zhang, Jian Li, Yixiang Xu, Xiaokang Li
{"title":"Discovery of a novel selenamide derivative as potent activator of aldehyde dehydrogenase 2 for cardioprotective applications","authors":"Yi Yang,&nbsp;Yue Yao,&nbsp;Junyang Huang,&nbsp;Zhan Shi,&nbsp;Xicheng Wang,&nbsp;Wei Li,&nbsp;Yishu Zhang,&nbsp;Jian Li,&nbsp;Yixiang Xu,&nbsp;Xiaokang Li","doi":"10.1007/s00044-025-03415-3","DOIUrl":"10.1007/s00044-025-03415-3","url":null,"abstract":"<div><p>Aldehyde dehydrogenase 2 (ALDH2), a mitochondrial enzyme, plays a pivotal role in the metabolism of endogenous reactive aldehydes and functions as a crucial defense mechanism against oxidative stress. The inactive ALDH2 rs671 polymorphism has been implicated in an elevated risk of various cardiovascular diseases, such as myocardial infarction, cardiac arrhythmia, coronary heart disease, and heart failure. Alda-1 is currently the most widely recognized ALDH2 activator and its anti-heart failure properties have been extensively reported. However, Alda-1 possesses limitations in terms of pharmacokinetic properties, safety, and bioavailability, which hinder its broad clinical application. Therefore, the development of novel ALDH2 activators represents a promising novel therapeutic approach. In this study, we employed a bioisosteric substitution strategy to modify the amide bond of Alda-1. Consequently, a selenamide derivative <b>A8</b> was discovered to exhibit potent ALDH2 activation activity at the submicromolar level (ALDH2*1: EC<sub>50</sub> = 0.21 ± 0.03 μM; ALDH2*2: EC<sub>50</sub> = 0.31 ± 0.03 μM) and showed reduced cytotoxicity compared to Alda-1 in H9c2 and HepG2 cell lines. Furthermore, <b>A8</b> provided potent protection of cardiomyocytes and showed enhanced efficiency in metabolizing endogenous reactive aldehydes. Our findings present <b>A8</b> as a valuable lead compound for advancing the development of ALDH2 activators, thereby offering new avenues for cardioprotective therapies.</p><div><figure><div><div><picture><source><img></source></picture></div></div></figure></div></div>","PeriodicalId":699,"journal":{"name":"Medicinal Chemistry Research","volume":"34 6","pages":"1332 - 1346"},"PeriodicalIF":2.6,"publicationDate":"2025-05-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144125600","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Benzoxa-[2,1,3]-diazole substituted amino acid hydrazides as therapeutics for drug-resistant Mycobacterium tuberculosis 苯并恶a-[2,1,3]-二唑取代氨基酸肼治疗耐药结核分枝杆菌
IF 2.6 4区 医学
Medicinal Chemistry Research Pub Date : 2025-05-03 DOI: 10.1007/s00044-025-03417-1
Ahmed K. B. Aljohani, Yucheng Lu, Kelly J. Jackson, Paul G. Waddell, Jason H. Gill, Alistair K. Brown, Jonathan D. Sellars
{"title":"Benzoxa-[2,1,3]-diazole substituted amino acid hydrazides as therapeutics for drug-resistant Mycobacterium tuberculosis","authors":"Ahmed K. B. Aljohani,&nbsp;Yucheng Lu,&nbsp;Kelly J. Jackson,&nbsp;Paul G. Waddell,&nbsp;Jason H. Gill,&nbsp;Alistair K. Brown,&nbsp;Jonathan D. Sellars","doi":"10.1007/s00044-025-03417-1","DOIUrl":"10.1007/s00044-025-03417-1","url":null,"abstract":"<div><p>The global burden of tuberculosis is on the rise and continues to be alarmingly high, with a notable prevalence of multidrug-resistant disease. Despite a promising drug development pipeline, the levels of resistance to these therapeutics remain significant, underscoring the need for new, innovative drugs to tackle this clinical issue. Benzoxadiazoles and their derivatives have become a valuable foundation for the development of next-generation antibacterial, antifungal, and anticancer agents. Herein, we explore the benzoxa-[2,1,3]-diazole scaffold as a promising framework for antimycobacterial development. Building on prior work, thirty-two amino acid hydrazide derivatives were synthesised using a modular approach, allowing variation of both the aryl hydrazine and amino acid moieties. These analogues were evaluated for activity against wild-type, isoniazid-resistant, and multidrug-resistant mycobacterial strains using the REMA assay, with several analogues demonstrating notable inhibitory activity. Overall, the series of novel benzoxa-[2,1,3]-diazole amino acid hydrazides demonstrates that through manipulation and optimisation of the amino acid hydrazide moieties, it is feasible to engineer potent compounds with improved antimycobacterial activity against both wild-type bacteria and, crucially, drug-resistant strains of the disease.</p><div><figure><div><div><picture><source><img></source></picture></div></div></figure></div></div>","PeriodicalId":699,"journal":{"name":"Medicinal Chemistry Research","volume":"34 6","pages":"1269 - 1275"},"PeriodicalIF":2.6,"publicationDate":"2025-05-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://link.springer.com/content/pdf/10.1007/s00044-025-03417-1.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144125555","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Design and synthesis of novel 1H-1,2,3-triazolecarbohydrazides and 1,2,4-triazoloazines based on them for anticancer drug discovery 基于它们的新型1h -1,2,3-三唑碳酰肼和1,2,4-三唑嗪的设计与合成,用于抗癌药物的发现
IF 2.6 4区 医学
Medicinal Chemistry Research Pub Date : 2025-05-02 DOI: 10.1007/s00044-025-03419-z
Daria Zakopailo, Yevhen Blashchak, Mykola Тupychak, Nataliya Finiuk, Nazariy Pokhodylo
{"title":"Design and synthesis of novel 1H-1,2,3-triazolecarbohydrazides and 1,2,4-triazoloazines based on them for anticancer drug discovery","authors":"Daria Zakopailo,&nbsp;Yevhen Blashchak,&nbsp;Mykola Тupychak,&nbsp;Nataliya Finiuk,&nbsp;Nazariy Pokhodylo","doi":"10.1007/s00044-025-03419-z","DOIUrl":"10.1007/s00044-025-03419-z","url":null,"abstract":"<div><p>The synthesis of (1<i>H-</i>1,2,3-triazol-4-yl)-1,2,4-triazolazine derivatives was achieved via a multi-step synthesis starting from 1<i>H-</i>1,2,3-triazole-4-carboxylic acids, followed by acylation and ring closure under the influence of POCl₃. The title compounds were tested for cytotoxicity against a range of cancer cell lines, including A549 human lung carcinoma, HCT116 colon carcinoma, Jurkat T-leukemia, and KB3-1 human cervical carcinoma. The compounds demonstrated varying degrees of activity, with several showing potent cytotoxic effects, particularly against human lung carcinoma A549 and human leukemia Jurkat T-cells. The results suggest that ring closure significantly influences the bioactivity of the compounds, enhancing their cytotoxic properties. The study indicates the potential of (1<i>H-</i>1,2,3-triazol-4-yl)-1,2,4-triazolazine derivatives as promising candidates for cancer therapy, especially those with specific substituent patterns that enhance their antiproliferative effects.</p><div><figure><div><div><picture><source><img></source></picture></div></div></figure></div></div>","PeriodicalId":699,"journal":{"name":"Medicinal Chemistry Research","volume":"34 6","pages":"1321 - 1331"},"PeriodicalIF":2.6,"publicationDate":"2025-05-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144125546","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Exploring putative histone deacetylase inhibitors with antiproliferative activity of chrysin derivatives 探索具有抗增殖活性的组蛋白去乙酰化酶抑制剂
IF 2.6 4区 医学
Medicinal Chemistry Research Pub Date : 2025-05-01 DOI: 10.1007/s00044-025-03418-0
Thitiporn Kamloon, Thanaset Senawong, Gulsiri Senawong, Narissara Namwan, Pakit Kumboonma, La-or Somsakeesit, Puracheth Ritchumpon, Mongkol Nontakitticharoen, Pitak Nasomjai, Chanokbhorn Phaosiri
{"title":"Exploring putative histone deacetylase inhibitors with antiproliferative activity of chrysin derivatives","authors":"Thitiporn Kamloon,&nbsp;Thanaset Senawong,&nbsp;Gulsiri Senawong,&nbsp;Narissara Namwan,&nbsp;Pakit Kumboonma,&nbsp;La-or Somsakeesit,&nbsp;Puracheth Ritchumpon,&nbsp;Mongkol Nontakitticharoen,&nbsp;Pitak Nasomjai,&nbsp;Chanokbhorn Phaosiri","doi":"10.1007/s00044-025-03418-0","DOIUrl":"10.1007/s00044-025-03418-0","url":null,"abstract":"<div><p>Thirty-three derivatives of chrysin were designed and synthesized to evaluate biological activities. All compounds were characterized using spectroscopy techniques (IR, <sup>1</sup>H NMR and <sup>13</sup>C NMR). Moreover, twelve new derivatives were fully characterized via the HRMS technique. The derivatives and the lead compound, chrysin (<b>1</b>) were screened against HDAC inhibition at 100 µM. Three derivatives (<b>C22</b>, <b>C23</b> and <b>C24</b>) demonstrated the most effective inhibition against HDACs with the IC<sub>50</sub> values as 27.13 ± 2.74 µM to 47.47 ± 1.13 µM. Furthermore, the HDAC8 inhibitory activity of compounds <b>C22</b> and <b>C23</b> (IC<sub>50</sub> = 75.37 ± 3.42 µM and 79.74 ± 0.41 µM, respectively) were more potent than that of chrysin (<b>1</b>) (IC<sub>50</sub> &gt; 100 µM). A molecular docking study found that the most active compound <b>C22</b> was more selective with HDAC8 (ΔG = −8.54 kcal/mol) than other isoforms (HDAC1, 2 and 3). The carboxyl moiety of the strongest derivatives plays an essential role in chelation with the Zn<sup>2+</sup> cofactor based on metal chelation assay. The Western blot assay confirmed that compounds <b>C23</b> and <b>C24</b> were the best HDACis. The most selective HDAC8 inhibitor, compound <b>C22</b>, showed the IC<sub>50</sub> value as 13.04 ± 1.08 µM against colon cancer cell lines (HCT-116), whereas compound <b>C24</b> exhibited the lowest IC<sub>50</sub> value as 11.96 ± 0.18 µM against the same cancer cell lines. The ClogP values of all derivatives were acceptable for oral administration (ClogP = 3.57 to 4.26). Therefore, the chrysin derivatives <b>C22</b>, <b>C23</b> and <b>C24</b> showed potential for further development as anti-cancer candidates.</p><div><figure><div><div><picture><source><img></source></picture></div></div></figure></div></div>","PeriodicalId":699,"journal":{"name":"Medicinal Chemistry Research","volume":"34 6","pages":"1308 - 1320"},"PeriodicalIF":2.6,"publicationDate":"2025-05-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144125541","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Pharmacological significance of palbociclib and its derivatives in cancer treatment and prevention: an update 帕博西尼及其衍生物在癌症治疗和预防中的药理意义:最新进展
IF 2.6 4区 医学
Medicinal Chemistry Research Pub Date : 2025-04-25 DOI: 10.1007/s00044-025-03411-7
Shagufta, Irshad Ahmad, Laila Zeyad Bazbouz, Noora Ali Nasar, Fatme Ghassan Ibrahim, Dana Mahmoud Alkheder
{"title":"Pharmacological significance of palbociclib and its derivatives in cancer treatment and prevention: an update","authors":"Shagufta,&nbsp;Irshad Ahmad,&nbsp;Laila Zeyad Bazbouz,&nbsp;Noora Ali Nasar,&nbsp;Fatme Ghassan Ibrahim,&nbsp;Dana Mahmoud Alkheder","doi":"10.1007/s00044-025-03411-7","DOIUrl":"10.1007/s00044-025-03411-7","url":null,"abstract":"<div><p>Palbociclib is a selective cyclin-dependent kinases 4 and 6 (CDK4/6) inhibitor that emerged as a significant therapeutic agent in the treatment of hormone receptor-positive, HER2-negative breast cancer. This review comprehensively highlights the pharmacological significance of palbociclib and its recently developed derivatives, focusing on mechanisms of action, chemical synthesis strategies, pharmacological profile and potential benefits in cancer treatment. We explored the rationale behind structural modifications and chemical derivatization of palbociclib that have been developed to enhance its therapeutic efficacy and mitigate side effects. This review offers an update on the latest advancement in palbociclib derivatives and explores their potential to improve therapeutic efficacy with minimal side effects. The detailed analysis of recent developments and ongoing research will support the designing of more efficient CDK4/6 inhibitors and provide direction in development of future cancer treatment. We anticipate that the information provided in this review will be beneficial to readers and scientist working towards development of effective cancer treatment specifically towards next-generation CDK4/6 inhibitors with improved therapeutic and safety profiles.</p><div><figure><div><div><picture><source><img></source></picture></div></div></figure></div></div>","PeriodicalId":699,"journal":{"name":"Medicinal Chemistry Research","volume":"34 6","pages":"1237 - 1252"},"PeriodicalIF":2.6,"publicationDate":"2025-04-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144125708","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Design, synthesis and antitumor activity study of tubulin/HDAC6 dual targeting inhibitor 微管蛋白/HDAC6双靶向抑制剂的设计、合成及抗肿瘤活性研究
IF 2.6 4区 医学
Medicinal Chemistry Research Pub Date : 2025-04-24 DOI: 10.1007/s00044-025-03413-5
Congcong Zheng, Yi Zhang, Yepeng Luan
{"title":"Design, synthesis and antitumor activity study of tubulin/HDAC6 dual targeting inhibitor","authors":"Congcong Zheng,&nbsp;Yi Zhang,&nbsp;Yepeng Luan","doi":"10.1007/s00044-025-03413-5","DOIUrl":"10.1007/s00044-025-03413-5","url":null,"abstract":"<div><p>Cancer combination therapy is a novel strategy to circumvent drug resistance in highly metastatic and advanced malignancies. To this end, we designed and synthesized a series of dual-targeting compounds that target tubulin and HDAC6 simultaneously. Out of them, compound named as <b>6-4</b> possessed potent inhibitory activity against tubulin polymerization and strong antiproliferative activity to the cancer cell lines tested. <b>6-4</b> was able to inhibit tubulin polymerization and disrupt the microtubule network of tumor cells. Significant downregulation of tubulin deacetylation was also observed after the treatment of <b>6-4</b> which indicated its inhibition toward HDAC6. Mechanism studies demonstrated that <b>6-4</b> could arrest cell cycle in G2/M phase and induce apoptosis in a dose-dependent manner. In addition, <b>6-4</b> can suppress metastasis of Hela cells, and significantly inhibit the formation of HUVEC tubes. All these results suggest that <b>6-4</b> should be a promising candidate for the treatment of cancer.</p><div><figure><div><div><picture><source><img></source></picture></div></div></figure></div></div>","PeriodicalId":699,"journal":{"name":"Medicinal Chemistry Research","volume":"34 6","pages":"1293 - 1307"},"PeriodicalIF":2.6,"publicationDate":"2025-04-24","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144125622","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Naturally occurring plant-derived sulfonated and sulfated saponins from 1983 to 2024 1983年至2024年天然存在的植物衍生磺化和磺化皂苷
IF 2.6 4区 医学
Medicinal Chemistry Research Pub Date : 2025-04-19 DOI: 10.1007/s00044-025-03412-6
Bienvenu Tsakem, Shoeshoe Mokhele, Lerato Mosima, Madan Poka, Patrick Hulisani Demana, Rémy Bertrand Teponno, Xavier Siwe Noundou
{"title":"Naturally occurring plant-derived sulfonated and sulfated saponins from 1983 to 2024","authors":"Bienvenu Tsakem,&nbsp;Shoeshoe Mokhele,&nbsp;Lerato Mosima,&nbsp;Madan Poka,&nbsp;Patrick Hulisani Demana,&nbsp;Rémy Bertrand Teponno,&nbsp;Xavier Siwe Noundou","doi":"10.1007/s00044-025-03412-6","DOIUrl":"10.1007/s00044-025-03412-6","url":null,"abstract":"<div><p>A substantial number of molecules have been already characterized from various organisms, such as plants, fungi, bacteria, and other animals; but just few have been already subjected to pharmacological assays. This is one of the reasons why reviewing previous studies will direct future investigations. The continuous chemical investigations of medicinal plants have been leading to a plethora of saponins. Some of these compounds carry one or more sulfonyl or sulfate groups. Such association rarely occurs in the plant kingdom. Till now, no report has summarized these sulfonated saponins isolated from medicinal plants. There is still a gap between the sulfonyl function and biological activities of these saponins. The present review encompasses the naturally occurring saponins containing the sulfonyl group either on the sapogenin or on the sugar moiety. The biosynthetic routes, their spectroscopic characteristics to shed more light on future structure elucidation and their biological activities are reported. It resulted that 141 saponins associating SO<sub>3</sub>H or SO<sub>3</sub><sup>-</sup> groups were reported from medicinal plants largely distributed within Zygophyllaceae and Asparagaceae families. Some of these compounds exhibited interesting biological activities including anticancer, antibacterial, anti-inflammatory and antiviral. It emerges from this review that many sulfonated saponins have been characterized, but just a few have been subjected to biological studies. The mechanism of action of these compounds remains understudied and further investigations need to be undertaken to understand how they act. This review covers reported data from 1983–2024.</p></div>","PeriodicalId":699,"journal":{"name":"Medicinal Chemistry Research","volume":"34 6","pages":"1212 - 1236"},"PeriodicalIF":2.6,"publicationDate":"2025-04-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://link.springer.com/content/pdf/10.1007/s00044-025-03412-6.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144125682","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Acetylcholinesterase Inhibitors from Carbamate and Benzo-fused Heterocyclic Scaffolds: Promising Therapeutics for Alzheimer’s Disease 氨基甲酸酯和苯并杂环支架的乙酰胆碱酯酶抑制剂:阿尔茨海默病的有希望的治疗方法
IF 2.6 4区 医学
Medicinal Chemistry Research Pub Date : 2025-04-18 DOI: 10.1007/s00044-025-03410-8
Amarjith Thiyyar Kandy, Raghul Venkatesan, Devadharuna Mohan, Sajeeth Chadapullykolumbu Ismail, Srikanth Jupudi, Divakar Selvaraj
{"title":"Acetylcholinesterase Inhibitors from Carbamate and Benzo-fused Heterocyclic Scaffolds: Promising Therapeutics for Alzheimer’s Disease","authors":"Amarjith Thiyyar Kandy,&nbsp;Raghul Venkatesan,&nbsp;Devadharuna Mohan,&nbsp;Sajeeth Chadapullykolumbu Ismail,&nbsp;Srikanth Jupudi,&nbsp;Divakar Selvaraj","doi":"10.1007/s00044-025-03410-8","DOIUrl":"10.1007/s00044-025-03410-8","url":null,"abstract":"<div><p>Alzheimer’s disease is the most prevalent type of dementia, characterized by a progressive loss of memory and neurodegeneration that hinders a patient’s ability to perform daily tasks. This paper explores the potential of acetylcholinesterase inhibitors derived from carbamate and benzo-fused heterocyclic scaffolds as potential therapeutics for Alzheimer’s disease. Inhibiting acetylcholinesterase is crucial for enhancing cognitive function in Alzheimer’s patients. The findings indicate that novel compounds featuring the mentioned scaffolds exhibit promising acetylcholinesterase inhibitory efficacy. Several of these compounds display superior half-maximal inhibitory concentration values against acetylcholinesterase compared to FDA-approved acetylcholinesterase inhibitors. The review emphasizes the importance of these compounds in addressing the cholinergic deficits associated with Alzheimer’s disease, where the loss of cholinergic neurons results in reduced acetylcholine levels in the synaptic cleft. Benzimidazole-based thiazole derivatives have demonstrated remarkable inhibitory capabilities against cholinesterase enzymes, with some compounds showing half-maximal inhibitory concentration values as low as 0.10 µM. The review highlights the effectiveness of benzofuran, benzoxazole, indole, indolinone, and coumarin derivatives in inhibiting acetylcholinesterase and providing neuroprotection, making them promising candidates for treating Alzheimer’s disease. Additionally, the review emphasizes the necessity for further research into the mechanisms of action of these substances and their effects on cognitive performance in clinical settings to enhance the quality of life for Alzheimer’s patients. Overall, this work contributes to the ongoing search for effective treatments for Alzheimer’s, stressing the importance of discovering new chemical entities capable of improving neurotransmission and cognitive function.</p><div><figure><div><div><picture><source><img></source></picture></div></div></figure></div></div>","PeriodicalId":699,"journal":{"name":"Medicinal Chemistry Research","volume":"34 6","pages":"1200 - 1211"},"PeriodicalIF":2.6,"publicationDate":"2025-04-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144125612","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Ferrocene-based compounds: promising anticancer and antimalarial agents in modern therapeutics 二茂铁基化合物:现代治疗中有前途的抗癌和抗疟药物
IF 2.6 4区 医学
Medicinal Chemistry Research Pub Date : 2025-04-16 DOI: 10.1007/s00044-025-03408-2
Anchal Sharma, Rupali Rana, Nitish Kumar, Harmandeep kaur gulati,  Jyoti, Aanchal Khanna, Sofia Sharma,  Pooja, Jatinder Vir Singh, Preet Mohinder Singh Bedi
{"title":"Ferrocene-based compounds: promising anticancer and antimalarial agents in modern therapeutics","authors":"Anchal Sharma,&nbsp;Rupali Rana,&nbsp;Nitish Kumar,&nbsp;Harmandeep kaur gulati,&nbsp; Jyoti,&nbsp;Aanchal Khanna,&nbsp;Sofia Sharma,&nbsp; Pooja,&nbsp;Jatinder Vir Singh,&nbsp;Preet Mohinder Singh Bedi","doi":"10.1007/s00044-025-03408-2","DOIUrl":"10.1007/s00044-025-03408-2","url":null,"abstract":"<div><p>Ferrocene, owing to its inherent stability, favourable redox characteristics, and low toxicity, has emerged as a significant structural motif in the field of bioorganometallic chemistry. Two prominent examples of ferrocene’s impact on medicinal chemistry are ferroquine and ferrocifen, both demonstrating remarkable antimalarial and anticancer activities. The enhanced therapeutic properties observed in these drug candidates underscore the profound influence ferrocene can exert on the molecular and biological behaviour of bioactive compounds. This Perspective delves into the scope and limitations of incorporating ferrocene into organic molecules and natural products, examining how such modifications affect their mechanisms of action and overall biological activities. A detailed discussion is provided on the role of ferrocene derivatization in modulating the anticancer, antimalarial, and antimicrobial properties of diverse bioactive moieties. The ultimate goal is to provide insights that contribute to the design and development of safer and more effective ferrocene-based drugs and focusing on their potential to address the critical unmet needs in cancer and malaria treatment.</p><div><figure><div><div><picture><source><img></source></picture></div></div></figure></div></div>","PeriodicalId":699,"journal":{"name":"Medicinal Chemistry Research","volume":"34 6","pages":"1177 - 1199"},"PeriodicalIF":2.6,"publicationDate":"2025-04-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144125559","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Discovery of novel pterostilbene/biphenyl tethered 5-FU based conjugates targeting colorectal cancer: synthesis, cytotoxic and ADMET modeling studies 针对结直肠癌的新型紫荆芪/联苯系5-FU缀合物的发现:合成、细胞毒性和ADMET模型研究
IF 2.6 4区 医学
Medicinal Chemistry Research Pub Date : 2025-04-15 DOI: 10.1007/s00044-025-03401-9
Rubén Becerra-Quintana, Angie Herrera-Ramírez, Andrés F. Yepes, Laura Cadavid-Arango, Wilson Cardona-Galeano
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