Medicinal Chemistry Research最新文献

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An evaluation of spirooxindoles as blocking agents of SARS-CoV-2 spike/ACE2 interaction: synthesis, biological evaluation and computational analysis 螺旋菌吲哚作为SARS-CoV-2刺突/ACE2相互作用阻断剂的评价:合成、生物学评价和计算分析
IF 2.6 4区 医学
Medicinal Chemistry Research Pub Date : 2025-02-23 DOI: 10.1007/s00044-025-03386-5
Albert Enama Ehinak, Maloba M. M. Lobe, Donatus B. Eni, Conrad V. Simoben, Ian Tietjen, Mathieu J. Mbenga Tjegbe, Joel Cassel, Joseph M. Salvino, Luis J. Montaner, Wolfgang Sippl, Simon M. N. Efange, Fidele Ntie-Kang
{"title":"An evaluation of spirooxindoles as blocking agents of SARS-CoV-2 spike/ACE2 interaction: synthesis, biological evaluation and computational analysis","authors":"Albert Enama Ehinak,&nbsp;Maloba M. M. Lobe,&nbsp;Donatus B. Eni,&nbsp;Conrad V. Simoben,&nbsp;Ian Tietjen,&nbsp;Mathieu J. Mbenga Tjegbe,&nbsp;Joel Cassel,&nbsp;Joseph M. Salvino,&nbsp;Luis J. Montaner,&nbsp;Wolfgang Sippl,&nbsp;Simon M. N. Efange,&nbsp;Fidele Ntie-Kang","doi":"10.1007/s00044-025-03386-5","DOIUrl":"10.1007/s00044-025-03386-5","url":null,"abstract":"<div><p>Severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) has gained significant public health attention owing to its devastating effects on lives and livelihoods worldwide. Due to difficult access to vaccines in many developing countries and the inefficiency of vaccines in providing complete protection even with fully vaccinated persons, there remains the need for the development of novel drugs to combat the disease. This study describes the in vitro activity of a library of fifty-five spiro-fused tetrahydroisoquinoline–oxindole hybrids (spirooxindoles) as potential blocking agents of the interaction between the SARS-CoV-2 viral spike and the human angiotensin-converting enzyme 2 (ACE2) receptor, essential for viral transmission. The synthesis was conducted by the Pictet-Spengler condensation of phenethylamine and isatin derivatives, while the screening against spike-ACE2 interaction was done using our previously described AlphaScreen fluorescent assay. The in vitro screening identified compound (<b>11j</b>) as the most active, showing a 50% inhibitory concentration (IC<sub>50</sub>) of 3.6 μM against SARS-CoV-2 spike/ACE2 interaction. Structure-activity relationships explained via molecular docking studies and the computation of binding free energy of each compound with respect to the spike/ACE2 protein-protein interaction showed that the most active compound possesses a bulky naphthyl group, which addresses voluminous hydrophobic regions of the ACE2 binding site and interacts with the hydrophobic residues of the target. Therefore, these compounds could be potentially useful in searching for SARS-CoV-2 spike/ACE2 interaction blocking agents.</p><div><figure><div><div><picture><source><img></source></picture></div></div></figure></div></div>","PeriodicalId":699,"journal":{"name":"Medicinal Chemistry Research","volume":"34 4","pages":"895 - 909"},"PeriodicalIF":2.6,"publicationDate":"2025-02-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://link.springer.com/content/pdf/10.1007/s00044-025-03386-5.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143621949","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
Exploring the potential of isatin hybrids as anticancer agents: recent advances and future prospective 探索isatin杂交体作为抗癌药物的潜力:最新进展和未来展望
IF 2.6 4区 医学
Medicinal Chemistry Research Pub Date : 2025-02-17 DOI: 10.1007/s00044-025-03385-6
Parveen Gahlyan, Tanisha Chauhan, Priyanka Jhajharia, Balaram Pani, Rakesh Kumar
{"title":"Exploring the potential of isatin hybrids as anticancer agents: recent advances and future prospective","authors":"Parveen Gahlyan,&nbsp;Tanisha Chauhan,&nbsp;Priyanka Jhajharia,&nbsp;Balaram Pani,&nbsp;Rakesh Kumar","doi":"10.1007/s00044-025-03385-6","DOIUrl":"10.1007/s00044-025-03385-6","url":null,"abstract":"<div><p>Synthesis of hybrid molecules via molecular hybridization technique has been known to be a promising strategy which involves the blending of two pharmacophoric groups joined via covalent bonds to make a single entity that can serve as chemotherapeutic agents. “Isatin” is an important toolbox for medicinal chemists with high pharmacological profile being known as the “privileged scaffold” in the field of drug development. Various drugs consisting of isatin core have been shown to have pronounced therapeutic effects on several cancers as they have prophylactic role towards free radicals that cause cancer. This report highlights the most recent advances from the past four years in the development of isatin based drugs against several human cancer cell lines such as MCF-7 (breast cancer cell line), A-549 (lung cancer cell line), Hep-G2 (liver cancer cell line) and some other cell lines, respectively.</p><div><figure><div><div><picture><source><img></source></picture></div></div></figure></div></div>","PeriodicalId":699,"journal":{"name":"Medicinal Chemistry Research","volume":"34 4","pages":"827 - 848"},"PeriodicalIF":2.6,"publicationDate":"2025-02-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143622100","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
A mild and catalyst-free α-benzoyloxylation of tertiary amides 叔酰胺的温和无催化剂α-苯甲酰氧基化反应
IF 2.6 4区 医学
Medicinal Chemistry Research Pub Date : 2025-02-12 DOI: 10.1007/s00044-025-03381-w
Md Imdadul H. Khan, Jiaxin Yang, Seong Jong Kim, Hoang V. Le
{"title":"A mild and catalyst-free α-benzoyloxylation of tertiary amides","authors":"Md Imdadul H. Khan,&nbsp;Jiaxin Yang,&nbsp;Seong Jong Kim,&nbsp;Hoang V. Le","doi":"10.1007/s00044-025-03381-w","DOIUrl":"10.1007/s00044-025-03381-w","url":null,"abstract":"<div><p>An α-C–H oxygenation of amides using Togni reagent II and an umpolung strategy is reported. α-Benzoyloxy amides were prepared in moderate-to-high yields from tertiary amides under mild and catalyst-free reaction conditions. All reagents are commercially available, easy to use, and compatible with various functional groups and rings. α-Benzoyloxy amides could be easily transformed into the corresponding α-hydroxy amides in almost quantitative yields. This transformation has significant potential for the synthesis of important compounds in pharmaceutical and agricultural fields.</p><div><figure><div><div><picture><source><img></source></picture></div></div></figure></div></div>","PeriodicalId":699,"journal":{"name":"Medicinal Chemistry Research","volume":"34 4","pages":"849 - 854"},"PeriodicalIF":2.6,"publicationDate":"2025-02-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143622189","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
Novel conjugated 5-alkenyl rhodanine tethered 1,4-benzodioxane derivatives as dual-chitinases inhibitors to hinder the growth of Asian corn borer 新型共轭5-烯基罗丹宁系结1,4-苯二氮杂环衍生物作为双几丁质酶抑制剂抑制亚洲玉米螟的生长
IF 2.6 4区 医学
Medicinal Chemistry Research Pub Date : 2025-02-12 DOI: 10.1007/s00044-025-03382-9
Jinxiu Chen, Dongmei Shi, Zhiyang Jiang, Renxuan Zou, Jingyu Zhang, Qing Han, Na Wang, Zhijian Xu, Qing Yang, Hongxia Duan
{"title":"Novel conjugated 5-alkenyl rhodanine tethered 1,4-benzodioxane derivatives as dual-chitinases inhibitors to hinder the growth of Asian corn borer","authors":"Jinxiu Chen,&nbsp;Dongmei Shi,&nbsp;Zhiyang Jiang,&nbsp;Renxuan Zou,&nbsp;Jingyu Zhang,&nbsp;Qing Han,&nbsp;Na Wang,&nbsp;Zhijian Xu,&nbsp;Qing Yang,&nbsp;Hongxia Duan","doi":"10.1007/s00044-025-03382-9","DOIUrl":"10.1007/s00044-025-03382-9","url":null,"abstract":"<div><p><i>Of</i>ChtI and <i>Of</i>Chi-h are ideal targets for developing agricultural inhibitors against <i>Ostrinia furnacalis</i>. In order to further confirm the importance of conjugated systems in rhodanine derivatives, sixteen novel 1,4-benzodioxane-tethered-rhodanine derivatives were designed and synthesized with or without C=C double bond of 5-alkenyl rhodanine skeleton. Among them, compounds <b>3a</b>–<b>3h</b>, with preserved 5-alkenyl rhodanine skeleton, all exhibited much better inhibitory activities against both <i>Of</i>ChtI and <i>Of</i>Chi-h, compared to that of the corresponding reduced compounds <b>4a</b>–<b>4h</b> without its C=C double bond. The inhibitory mechanism demonstrated that the 5-alkenyl rhodanine conjugated plane was conducive to improving the binding affinity with both two chitinases. Compound <b>3g</b> was identified as the most potential dual-chitinases inhibitor against <i>Of</i>ChtI (<i>K</i><sub>i</sub> = 2.57 μM) and <i>Of</i>Chi-h (<i>K</i><sub>i</sub> = 2.03 μM). The bioassay study also indicated that compound <b>3g</b> displayed the best insecticidal activity against <i>O. furnacalis</i> and distinctive sublethal effect in regulating its growth and development. These 1,4-benzodioxane-tethered-rhodanine derivatives deserved further investigation as novel dual-chitinases inhibitor candidates in the control of <i>O. furnacalis</i>.</p><div><figure><div><div><picture><source><img></source></picture></div></div></figure></div></div>","PeriodicalId":699,"journal":{"name":"Medicinal Chemistry Research","volume":"34 4","pages":"882 - 894"},"PeriodicalIF":2.6,"publicationDate":"2025-02-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143622190","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
Synthesis and evaluation of tetrahydrobenzo[cd]indole derivatives as glycogen phosphorylase inhibitors 四氢苯并[cd]吲哚衍生物糖原磷酸化酶抑制剂的合成及评价
IF 2.6 4区 医学
Medicinal Chemistry Research Pub Date : 2025-02-08 DOI: 10.1007/s00044-025-03384-7
Panarat Arunrattiyakorn, Chanitha Juiprasert, Symeon M. Koulas, Pornthip Boonsri, Thammarat Aree, Maho Yagi-Utsumi, Koichi Kato, Demetres D. Leonidas
{"title":"Synthesis and evaluation of tetrahydrobenzo[cd]indole derivatives as glycogen phosphorylase inhibitors","authors":"Panarat Arunrattiyakorn,&nbsp;Chanitha Juiprasert,&nbsp;Symeon M. Koulas,&nbsp;Pornthip Boonsri,&nbsp;Thammarat Aree,&nbsp;Maho Yagi-Utsumi,&nbsp;Koichi Kato,&nbsp;Demetres D. Leonidas","doi":"10.1007/s00044-025-03384-7","DOIUrl":"10.1007/s00044-025-03384-7","url":null,"abstract":"<div><p>A series of tetrahydrobenzo[<i>cd</i>]indole derivatives was synthesized by condensation of a fungal metabolite hyphodermin A, a naphtho[1,2-<i>c</i>]furan-3,9-dione derivative, and various anilines in methanol. Using this approach, ten analogs (<b>3a</b>–<b>3j</b>) were synthesized and tested as inhibitors against glycogen phosphorylase (GP). While compounds <b>3e</b> and <b>3i</b> bearing hydrophobic bromo and trifluoromethyl groups showed moderated inhibition (<i>K</i><sub>i</sub> = 32.3–57.4 μΜ), compound <b>3g</b> with hydroxy group had the most potent activity with a <i>K</i><sub>i</sub> value of 7.9 ± 0.7 μΜ against human liver GPa. An X-ray crystallography study of the rabbit muscle GPb-<b>3g</b> complexes revealed that this inhibitor binds at a subsite within the indole binding site of GP which has not been previously observed to bind ligands.</p><div><figure><div><div><picture><source><img></source></picture></div></div></figure></div></div>","PeriodicalId":699,"journal":{"name":"Medicinal Chemistry Research","volume":"34 4","pages":"870 - 881"},"PeriodicalIF":2.6,"publicationDate":"2025-02-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143622156","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
Anticancer therapeutic potential of silibinin: current trends, scope and relevance 水飞蓟宾的抗癌潜力:目前的趋势,范围和相关性
IF 2.6 4区 医学
Medicinal Chemistry Research Pub Date : 2025-02-05 DOI: 10.1007/s00044-025-03383-8
Anupam Sharma, Sunil Kumar, Virender Pahil, Babli Mamoria, Mukesh Yadav, Nirmala Sehrawat, Manoj Singh, Anil Kumar Sharma
{"title":"Anticancer therapeutic potential of silibinin: current trends, scope and relevance","authors":"Anupam Sharma,&nbsp;Sunil Kumar,&nbsp;Virender Pahil,&nbsp;Babli Mamoria,&nbsp;Mukesh Yadav,&nbsp;Nirmala Sehrawat,&nbsp;Manoj Singh,&nbsp;Anil Kumar Sharma","doi":"10.1007/s00044-025-03383-8","DOIUrl":"10.1007/s00044-025-03383-8","url":null,"abstract":"<div><p>The use of natural plants as powerful sources for the treatment of chronic illnesses has drawn more attention from researchers to herbal remedies. Silybum marianum, a naturally occurring plant, is the source of silymarin, a flavonolignan which is used to guard against a range of illnesses in both clinical and experimental contexts. Silymarin is easily absorbed and metabolised in phases I and II, according to its pharmacokinetics. Phase II is the site of its conjugation, and it is finally excreted in bile and urine. In a variety of tissues, the primary active components, silymarin and silibinin, provide protection against cancer. Silibinin has been shown to have anti-inflammatory, anti-angiogenic, antioxidant, and anti-metastatic properties. This further helps to block many oncogenic pathways from being activated such as NF-κB, Wnt/β-catenin, PI3K/Akt, and MAPK pathways. Hence, silibinin helps in preventing proliferation of the tumor cells, initiating the cell cycle arrest, and induce cancer cells to die. This review gives the thorough analysis of silibinin in distinct types of cancer such as lung, liver, breast, bladder, prostate, skin and ovarian 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 4","pages":"809 - 824"},"PeriodicalIF":2.6,"publicationDate":"2025-02-05","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143622058","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
A review on efficacy of phytochemicals in the treatment of trypanosomiasis 植物化学物质治疗锥虫病的研究进展
IF 2.6 4区 医学
Medicinal Chemistry Research Pub Date : 2025-02-04 DOI: 10.1007/s00044-025-03379-4
Rutvi Agrawal, Priyanka Jurel, Bhupendra G. Prajapati, Suraj N. Mali, Akash Garg, Omar Awad Alsaidan, Sami I. Alzarea
{"title":"A review on efficacy of phytochemicals in the treatment of trypanosomiasis","authors":"Rutvi Agrawal,&nbsp;Priyanka Jurel,&nbsp;Bhupendra G. Prajapati,&nbsp;Suraj N. Mali,&nbsp;Akash Garg,&nbsp;Omar Awad Alsaidan,&nbsp;Sami I. Alzarea","doi":"10.1007/s00044-025-03379-4","DOIUrl":"10.1007/s00044-025-03379-4","url":null,"abstract":"<div><p>Trypanosomiasis, which is brought on by trypanosome parasites, is still a serious but often ignored health issue, especially in nations with limited resources. It is necessary to create novel, safe, effective, and alternative anti-trypanosomal chemical substances because current treatments have significant adverse reactions, low potency, high levels of toxicity, and drug resistance. Drug regimens that constitute the fundamental basis of contemporary pharmacological therapy have been largely derived from substances that are natural. Plants are mainly revered as ancient medicines worldwide and have contributed to the development of important pharmaceuticals for widespread medical conditions. An innovative approach for obtaining a reliable and potentially rich source of treatment against a variety of infectious diseases has been demonstrated by plant-focused research. This review discusses various phytoconstituents that have been utilized in the treatment of trypanosomiasis. Various recent and earlier studies that have investigated the in-vitro or in-vivo potential of medicinal plants for anti-trypanosomal properties have been discussed. The presence of bioactive plant-based compounds like quinones, flavonoids, phenols, etc., in the essential oils and unrefined extracts of various medicinal herbs, is part of a significant approach associated with the development of novel therapeutics. These substances have been found to be a reliable source of medicinal substances to aid in the treatment of trypanosomiasis. This review emphasizes the use of various plants with their phytoconstituents as an avenue of novel and potent medications against Trypanosomiasis. It discusses various studies of trypanocidal properties of alkaloids, essential oils, phenols, flavonoids, etc., that have been widely utilized against Trypanosoma. The results from both in vitro and in vivo studies demonstrate these natural compounds’ potential as therapeutics for the management of Trypanosoma infections.</p><h3>Graphical abstract</h3><div><figure><div><div><picture><source><img></source></picture></div><div><p>The Graphical abstract summarizes various phytochemicals that have been discussed in the manuscript along with various studies against Trypanosoma infection.</p></div></div></figure></div></div>","PeriodicalId":699,"journal":{"name":"Medicinal Chemistry Research","volume":"34 4","pages":"791 - 808"},"PeriodicalIF":2.6,"publicationDate":"2025-02-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143621973","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
Synthesis, crystal structure, and anticancer activity of organotin(IV) complexes based on chlorine substituted aryl ligands 基于氯取代芳基配体的有机锡配合物的合成、晶体结构和抗癌活性
IF 2.6 4区 医学
Medicinal Chemistry Research Pub Date : 2025-02-04 DOI: 10.1007/s00044-025-03378-5
Xinhua Wu, Lifang Wu, Zhaoquan Li, Wei Tian, Tao Li
{"title":"Synthesis, crystal structure, and anticancer activity of organotin(IV) complexes based on chlorine substituted aryl ligands","authors":"Xinhua Wu,&nbsp;Lifang Wu,&nbsp;Zhaoquan Li,&nbsp;Wei Tian,&nbsp;Tao Li","doi":"10.1007/s00044-025-03378-5","DOIUrl":"10.1007/s00044-025-03378-5","url":null,"abstract":"<div><p>Three series of (dimethyl-, dibutyl-, and diphenyl-) new organotin(IV) complexes based on chlorine substituted aryl ligands were synthesized and characterized by UV, <sup>1</sup>H NMR, <sup>13</sup>C NMR, <sup>119</sup> Sn NMR, HRMS, and X-ray crystallography analysis. MTT results showed that chlorine substitution at different positions on the aryl group exhibited different anticancer activities. Among them, 5-chloro substituents &gt; 3,5-dichloro substituents &gt; 3-chloro substituents on the aryl ring of salicylaldehyde on Schiff base ligand. In addition, different substituents on the tin atom also demonstrated extreme differences in anticancer activities, where dibutyltin &gt; diphenyltin &gt; dimethyltin. Interestingly, the complex <b>LTDB2</b> exhibited excellent anti-proliferative activity against breast cancer MDA-MB-231 cells (superior to cisplatin) and lower toxicity against human embryonic kidney HEK-293 cells in vitro. Flow cytometry showed that <b>LTDB2</b> not only induced apoptosis, but also induced cell cycle arrest in G2 phase. These findings provide new insights for further research and development of novel organotin(IV) complexes as anticancer drugs.</p><div><figure><div><div><picture><source><img></source></picture></div><div><p>Complex <b>LTDB2</b> exhibited excellent anti-proliferative activity against breast cancer MDA-MB-231 cells in vitro and was superior to cisplatin. Flow cytometry showed that <b>LTDB2</b> not only induced apoptosis, but also induced cell cycle arrest in G2 phase.</p></div></div></figure></div></div>","PeriodicalId":699,"journal":{"name":"Medicinal Chemistry Research","volume":"34 4","pages":"855 - 869"},"PeriodicalIF":2.6,"publicationDate":"2025-02-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143621972","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 the antineoplastic potential of novel NSAID derivatives in combatting mammary tumorigenesis: a comprehensive review 探索新型非甾体抗炎药衍生物在对抗乳腺肿瘤发生中的抗肿瘤潜力:全面综述
IF 2.6 4区 医学
Medicinal Chemistry Research Pub Date : 2025-02-01 DOI: 10.1007/s00044-025-03377-6
Rashmi Dewangan, Nidhi Agrawal, S. K. Lanjhiyana, Meenakshi Jaiswal
{"title":"Exploring the antineoplastic potential of novel NSAID derivatives in combatting mammary tumorigenesis: a comprehensive review","authors":"Rashmi Dewangan,&nbsp;Nidhi Agrawal,&nbsp;S. K. Lanjhiyana,&nbsp;Meenakshi Jaiswal","doi":"10.1007/s00044-025-03377-6","DOIUrl":"10.1007/s00044-025-03377-6","url":null,"abstract":"<div><p>Nonsteroidal anti-inflammatory drugs (NSAIDs) are commonly prescribed for pyrexia, dysmenorrhea, operative pain, and arthritic pain due to their analgesic, antipyretic, and anti-inflammatory properties. A recent investigation indicates that NSAIDs may possess prophylactic properties against mammary tumor. Their anti-neoplastic potential is associated with chronic inflammation in the development of tumors. NSAIDs exhibit anti-breast cancer activity potentially by targeting COX-2, an enzyme overexpressed in many solid tumors, or by altering several pathways, including NF-κB, JAK-STAT, MAPK, PI3K/Akt, mTOR, Wnt/β-catenin, and CREB, involved in cell cycle regulation, development, and progression of the tumor. In addition, NSAIDs can alter the expression of pro- and anti-apoptotic proteins that regulate cell survival. Researchers have developed a variety of derivatives, such as ester, phospho-ester, thioester, amide, hydrazide, metal complexes, and salt derivatives, to improve the anticancer activity and selectivity of NSAIDs. These novel derivatives exhibited excellent outcomes in preclinical investigations against various breast cancer cell lines, highlighting enhanced cytotoxicity and bioavailability and minimizing adverse effects as compared to standard NSAIDs. This review emphasizes the anti-breast cancer potential of NSAIDs and their novel derivatives by targeting novel molecular targets in mammary tumorigenesis, focusing on both COX-dependent and independent pathways. Investigating these NSAID derivatives offers an optimistic approach to the development of safer, more efficient anticancer agents for the treatment of breast 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 4","pages":"764 - 790"},"PeriodicalIF":2.6,"publicationDate":"2025-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143621761","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
A multi enzyme study reviewing the role of target enzymes in Alzheimer’s disease and unveiling potential inhibitors with insights on their present and future assessment 多酶研究回顾了目标酶在阿尔茨海默病中的作用,揭示了潜在的抑制剂,并对其目前和未来的评估提出了见解
IF 2.6 4区 医学
Medicinal Chemistry Research Pub Date : 2025-01-31 DOI: 10.1007/s00044-025-03373-w
Syed Bassam Zaki, Sahar Afzal Khan, Ruhi Ali
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