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Innovative Theranostics Strategies in the Fight Against Lung Cancer.
IF 3.3 3区 医学 Q2 CHEMISTRY, MEDICINAL Pub Date : 2025-03-07 DOI: 10.2174/0113895575338753250228055700
Aashi Jain, Sakshi Soni, Vandana Soni, Sushil Kumar Kashaw

This review delves into the potential of nanotechnology for improved lung cancer diagnosis and treatment. A critical focus is placed on various overexpressed biomarkers within lung tumors. These biomarkers serve as potential targets for nanoparticle-based drug delivery strategies. The review explores two main targeting approaches: passive and active (receptor-based) targeting. Active targeting mechanisms like EGFR, folic acid, and CD44 receptor targeting are specifically discussed. Additionally, the review examines stimuli-responsive systems for targeted drug delivery, including pH, temperature, ligand-attached, and multi-stimuli-responsive systems. Moreover, the role of nanotechnology in theranostics, which combines therapeutic and diagnostic capabilities, is explored and different types of nanocarriers, including lipid-based, polymer-based, metal-based, and magnetic nanoparticles, are examined for their potential applications. The review also highlights advancements in lung cancer diagnostic techniques beyond nanotechnology. This includes emerging tools like biomarkers, biosensors, and artificial intelligence, alongside improvements to established methods. Finally, the review provides a glimpse into ongoing clinical trials and concludes by emphasizing the transformative potential of nanotechnology in improving lung cancer patient outcomes.

{"title":"Innovative Theranostics Strategies in the Fight Against Lung Cancer.","authors":"Aashi Jain, Sakshi Soni, Vandana Soni, Sushil Kumar Kashaw","doi":"10.2174/0113895575338753250228055700","DOIUrl":"https://doi.org/10.2174/0113895575338753250228055700","url":null,"abstract":"<p><p>This review delves into the potential of nanotechnology for improved lung cancer diagnosis and treatment. A critical focus is placed on various overexpressed biomarkers within lung tumors. These biomarkers serve as potential targets for nanoparticle-based drug delivery strategies. The review explores two main targeting approaches: passive and active (receptor-based) targeting. Active targeting mechanisms like EGFR, folic acid, and CD44 receptor targeting are specifically discussed. Additionally, the review examines stimuli-responsive systems for targeted drug delivery, including pH, temperature, ligand-attached, and multi-stimuli-responsive systems. Moreover, the role of nanotechnology in theranostics, which combines therapeutic and diagnostic capabilities, is explored and different types of nanocarriers, including lipid-based, polymer-based, metal-based, and magnetic nanoparticles, are examined for their potential applications. The review also highlights advancements in lung cancer diagnostic techniques beyond nanotechnology. This includes emerging tools like biomarkers, biosensors, and artificial intelligence, alongside improvements to established methods. Finally, the review provides a glimpse into ongoing clinical trials and concludes by emphasizing the transformative potential of nanotechnology in improving lung cancer patient outcomes.</p>","PeriodicalId":18548,"journal":{"name":"Mini reviews in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":3.3,"publicationDate":"2025-03-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143586292","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}
引用次数: 0
Innovative Horizons in Drug Design: Exploring the Synthesis and Medicinal Properties of Heterocyclic Schiff Bases. A Review.
IF 3.3 3区 医学 Q2 CHEMISTRY, MEDICINAL Pub Date : 2025-02-26 DOI: 10.2174/0113895575320413250126041041
Yousaf Khan, Hina Sarfraz, Wajid Rehman, Momin Khan, Liaqat Rasheed, Khursheed Ur Rahman

Schiff bases are an important scaffold for designing drug development. They are characterized by having a carbon-nitrogen double bond. This double bond is synthesized by different synthetic schemes by both the aromatic and aliphatic chains. Bases inspired chemists due to their versatile importance in drug discovery and drug development. A large number of drugs are designed through the heterocyclic Schiff base moieties. This review highlighted the importance of Schiff bases concerning their bioactive importance in drug design. Moreover, amide-iminol tautomerism is a significant tool for the high biological importance of Schiff bases due to the presence of the C=N bond. Furthermore, the reported synthesized heterocyclic scaffolds Schiff bases have a wide range of biological importance. Due to this different biological importance, such as antimicrobial, anticonvulsant, analgesic, antioxidant, antimalarial, anti-inflammatory, anticancer, antidiabetic, and antileishmanial properties, the researcher has shown their interest by synthesizing different heterocyclic Schiff bases. In this review article, biologically active heterocyclic Schiff bases were reviewed intensively concerning drug design and drug development.

{"title":"Innovative Horizons in Drug Design: Exploring the Synthesis and Medicinal Properties of Heterocyclic Schiff Bases. A Review.","authors":"Yousaf Khan, Hina Sarfraz, Wajid Rehman, Momin Khan, Liaqat Rasheed, Khursheed Ur Rahman","doi":"10.2174/0113895575320413250126041041","DOIUrl":"https://doi.org/10.2174/0113895575320413250126041041","url":null,"abstract":"<p><p>Schiff bases are an important scaffold for designing drug development. They are characterized by having a carbon-nitrogen double bond. This double bond is synthesized by different synthetic schemes by both the aromatic and aliphatic chains. Bases inspired chemists due to their versatile importance in drug discovery and drug development. A large number of drugs are designed through the heterocyclic Schiff base moieties. This review highlighted the importance of Schiff bases concerning their bioactive importance in drug design. Moreover, amide-iminol tautomerism is a significant tool for the high biological importance of Schiff bases due to the presence of the C=N bond. Furthermore, the reported synthesized heterocyclic scaffolds Schiff bases have a wide range of biological importance. Due to this different biological importance, such as antimicrobial, anticonvulsant, analgesic, antioxidant, antimalarial, anti-inflammatory, anticancer, antidiabetic, and antileishmanial properties, the researcher has shown their interest by synthesizing different heterocyclic Schiff bases. In this review article, biologically active heterocyclic Schiff bases were reviewed intensively concerning drug design and drug development.</p>","PeriodicalId":18548,"journal":{"name":"Mini reviews in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":3.3,"publicationDate":"2025-02-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143516080","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}
引用次数: 0
The Effects of Antioxidant Approved Drugs and Under Investigation Compounds with Potential of Improving Sleep Disorders and their Associated Comorbidities associated with Oxidative Stress and Inflammation.
IF 3.3 3区 医学 Q2 CHEMISTRY, MEDICINAL Pub Date : 2025-02-14 DOI: 10.2174/0113895575360959250117073046
Panagiotis Theodosis-Nobelos, Fani-Niki Varra, Michail Varras, Eleni A Rekka

Sleep disorders and the resultant sleep deprivation (SD) are very common nowadays, resulting in depressed mood, poor memory and concentration, and various important changes in health, performance and safety. They may provoke further impairment of the cell lining of the blood vessels, as acting as a risk factor for cardiovascular disease (CVD) onset and progression. SD may lead to low neuronal regaining and plasticity, drastically affecting brain function. Thus, SD is a known risk factor for mental, behavioral and developmental disorders. Due to the inflammatory and oxidative stressful nature of SD, immune response modulation and antioxidants could be another therapeutic approach, apart from the already known symptomatic treatment with sedatives. Additionally, many drugs approved for other indications and under investigation, have been revisited due to their wide array of pharmacological activities. This review summarizes the main aspects of SD pathology and SD interrelated comorbidities and presents direct and indirect antioxidant molecules and drugs with multi-targeting potential that could assist in the prevention or management of these factors. A number of research groups have investigated well-known antioxidant compounds with multi-targeting cores, combining structural characteristics with properties including antiinflammatory, metal chelatory, gene transcription and immune modulatory that may add towards the effective SD and its associated comorbidities treatment.

{"title":"The Effects of Antioxidant Approved Drugs and Under Investigation Compounds with Potential of Improving Sleep Disorders and their Associated Comorbidities associated with Oxidative Stress and Inflammation.","authors":"Panagiotis Theodosis-Nobelos, Fani-Niki Varra, Michail Varras, Eleni A Rekka","doi":"10.2174/0113895575360959250117073046","DOIUrl":"https://doi.org/10.2174/0113895575360959250117073046","url":null,"abstract":"<p><p>Sleep disorders and the resultant sleep deprivation (SD) are very common nowadays, resulting in depressed mood, poor memory and concentration, and various important changes in health, performance and safety. They may provoke further impairment of the cell lining of the blood vessels, as acting as a risk factor for cardiovascular disease (CVD) onset and progression. SD may lead to low neuronal regaining and plasticity, drastically affecting brain function. Thus, SD is a known risk factor for mental, behavioral and developmental disorders. Due to the inflammatory and oxidative stressful nature of SD, immune response modulation and antioxidants could be another therapeutic approach, apart from the already known symptomatic treatment with sedatives. Additionally, many drugs approved for other indications and under investigation, have been revisited due to their wide array of pharmacological activities. This review summarizes the main aspects of SD pathology and SD interrelated comorbidities and presents direct and indirect antioxidant molecules and drugs with multi-targeting potential that could assist in the prevention or management of these factors. A number of research groups have investigated well-known antioxidant compounds with multi-targeting cores, combining structural characteristics with properties including antiinflammatory, metal chelatory, gene transcription and immune modulatory that may add towards the effective SD and its associated comorbidities treatment.</p>","PeriodicalId":18548,"journal":{"name":"Mini reviews in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":3.3,"publicationDate":"2025-02-14","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143432838","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}
引用次数: 0
In vivo Pharmacokinetic and ADMET Profiles of Synthetic Antimicrobial Peptides (AMPs): A Review.
IF 3.3 3区 医学 Q2 CHEMISTRY, MEDICINAL Pub Date : 2025-02-11 DOI: 10.2174/0113895575362479241231054240
Muhammad Akram Mohd Noordin, Ahmed Abdulkareem Najm, Herryawan Ryadi Eziwar Dyari, Douglas Law, Sharifah Sakinah Syed Alwi, Azwan Mat Lazim, Yew Hoong Cheah, Thiam Tsui Tee, Shazrul Fazry

The broad-spectrum action and capacity to target drug-resistant infections make synthetic Antimicrobial Peptides (AMPs) popular therapeutic agents. Indeed, the effective use of these peptides in clinical application relies on a thorough understanding of their Pharmacokinetic (PK) and ADMET (Absorption, Distribution, Metabolism, Excretion, and Toxicity) characteristics. Despite growing research on synthetic AMPs, there is a notable gap in the literature specifically addressing their ADMET profiles. Previous reviews have not extensively covered this area, providing a vital opportunity to study synthetic AMPs' pharmacokinetics and safety, which are crucial for their therapeutic development. This review covered research studies that focused on PK and ADMET of synthetic antimicrobial peptides from several databases, including Google Scholar, SCOPUS, PubMed, and Science Direct, within the years 2020 to 2024, and 12 related research papers have been found. AMPs display a wide range of PK behaviors, including rapid renal clearance, liver-centric distribution, broad distribution with low toxicity, high kidney retention, and gradual absorption with dose-dependent toxicity. Overall, the ADMET profiles of AMPs are crucial in assessing their therapeutic potential, and continuous study is necessary to enhance their practical feasibility. An in-depth investigation of the in vivo ADMET and pharmacokinetic profiles of synthetic AMPs is presented in this review to address the current gap in the research. The findings of this study provide important insights for developing synthetic AMPs as effective antimicrobial drugs.

{"title":"In vivo Pharmacokinetic and ADMET Profiles of Synthetic Antimicrobial Peptides (AMPs): A Review.","authors":"Muhammad Akram Mohd Noordin, Ahmed Abdulkareem Najm, Herryawan Ryadi Eziwar Dyari, Douglas Law, Sharifah Sakinah Syed Alwi, Azwan Mat Lazim, Yew Hoong Cheah, Thiam Tsui Tee, Shazrul Fazry","doi":"10.2174/0113895575362479241231054240","DOIUrl":"https://doi.org/10.2174/0113895575362479241231054240","url":null,"abstract":"<p><p>The broad-spectrum action and capacity to target drug-resistant infections make synthetic Antimicrobial Peptides (AMPs) popular therapeutic agents. Indeed, the effective use of these peptides in clinical application relies on a thorough understanding of their Pharmacokinetic (PK) and ADMET (Absorption, Distribution, Metabolism, Excretion, and Toxicity) characteristics. Despite growing research on synthetic AMPs, there is a notable gap in the literature specifically addressing their ADMET profiles. Previous reviews have not extensively covered this area, providing a vital opportunity to study synthetic AMPs' pharmacokinetics and safety, which are crucial for their therapeutic development. This review covered research studies that focused on PK and ADMET of synthetic antimicrobial peptides from several databases, including Google Scholar, SCOPUS, PubMed, and Science Direct, within the years 2020 to 2024, and 12 related research papers have been found. AMPs display a wide range of PK behaviors, including rapid renal clearance, liver-centric distribution, broad distribution with low toxicity, high kidney retention, and gradual absorption with dose-dependent toxicity. Overall, the ADMET profiles of AMPs are crucial in assessing their therapeutic potential, and continuous study is necessary to enhance their practical feasibility. An in-depth investigation of the in vivo ADMET and pharmacokinetic profiles of synthetic AMPs is presented in this review to address the current gap in the research. The findings of this study provide important insights for developing synthetic AMPs as effective antimicrobial drugs.</p>","PeriodicalId":18548,"journal":{"name":"Mini reviews in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":3.3,"publicationDate":"2025-02-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143414539","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}
引用次数: 0
The Role of Renin-Angiotensin System in Diabetic Nephropathy: An Update.
IF 3.3 3区 医学 Q2 CHEMISTRY, MEDICINAL Pub Date : 2025-02-06 DOI: 10.2174/0113895575344980250130062547
André Sanglard, Bárbara Castello Branco Miranda, Ana Luiza França Vieira, Marcus Vinicius Miranda Macedo, Rodrigo Lara Santos, Aléxia Stenner Rodrigues Radicchi Campos, Amanda Campos Piva, Ana Cristina Simões E Silva

Background and aims: Diabetic nephropathy (DN) is an important complication of diabetes, leading to end-stage renal disease (ESRD) worldwide. This review aimed to explore the role of the renin-angiotensin system (RAS) in DN, highlighting current treatments and emerging therapeutic perspectives.

Methods: We conducted a narrative review of the literature up to March 2024, focusing on the classical and alternative RAS axes, their implications in DN, and novel therapeutic approaches. Data were sourced from Scopus, PubMed, Scielo, and Cochrane databases.

Results: The classical RAS axis, involving angiotensin-converting enzyme (ACE), Angiotensin II (Ang II), and the AT1 receptor, promotes vasoconstriction, sodium retention, and fibrosis in DN. Hyperglycemia-induced Ang II increases oxidative stress, contributing to glomerular hyperfiltration and kidney damage. Current treatments include ACE inhibitors and angiotensin receptor blockers (ARBs), which reduce blood pressure and proteinuria, delaying DN progression. In contrast, the alternative RAS axis, featuring ACE2, Ang-(1-7), and the Mas receptor, offers renoprotective effects by counteracting Ang II actions. Ang-(1-7) reduces inflammation, fibrosis, and podocyte apoptosis. ACE2 activators, Ang-(1-7), and Mas receptor agonists show promise in preclinical studies, reducing glomerular fibrosis and improving renal function. Ang-(1-9) and alamandine may also hold potential in future treatments. Emerging therapies, such as the SGLT2 inhibitors, also demonstrate benefits in reducing DN progression.

Conclusion: While ACE inhibitors, ARBs, and SGLT2 inhibitors remain central to DN management, the ACE2-Ang-(1-7)-Mas axis presents a promising therapeutic target. Future research should focus on translating preclinical findings into clinical applications, potentially improving DN treatment.

{"title":"The Role of Renin-Angiotensin System in Diabetic Nephropathy: An Update.","authors":"André Sanglard, Bárbara Castello Branco Miranda, Ana Luiza França Vieira, Marcus Vinicius Miranda Macedo, Rodrigo Lara Santos, Aléxia Stenner Rodrigues Radicchi Campos, Amanda Campos Piva, Ana Cristina Simões E Silva","doi":"10.2174/0113895575344980250130062547","DOIUrl":"https://doi.org/10.2174/0113895575344980250130062547","url":null,"abstract":"<p><strong>Background and aims: </strong>Diabetic nephropathy (DN) is an important complication of diabetes, leading to end-stage renal disease (ESRD) worldwide. This review aimed to explore the role of the renin-angiotensin system (RAS) in DN, highlighting current treatments and emerging therapeutic perspectives.</p><p><strong>Methods: </strong>We conducted a narrative review of the literature up to March 2024, focusing on the classical and alternative RAS axes, their implications in DN, and novel therapeutic approaches. Data were sourced from Scopus, PubMed, Scielo, and Cochrane databases.</p><p><strong>Results: </strong>The classical RAS axis, involving angiotensin-converting enzyme (ACE), Angiotensin II (Ang II), and the AT1 receptor, promotes vasoconstriction, sodium retention, and fibrosis in DN. Hyperglycemia-induced Ang II increases oxidative stress, contributing to glomerular hyperfiltration and kidney damage. Current treatments include ACE inhibitors and angiotensin receptor blockers (ARBs), which reduce blood pressure and proteinuria, delaying DN progression. In contrast, the alternative RAS axis, featuring ACE2, Ang-(1-7), and the Mas receptor, offers renoprotective effects by counteracting Ang II actions. Ang-(1-7) reduces inflammation, fibrosis, and podocyte apoptosis. ACE2 activators, Ang-(1-7), and Mas receptor agonists show promise in preclinical studies, reducing glomerular fibrosis and improving renal function. Ang-(1-9) and alamandine may also hold potential in future treatments. Emerging therapies, such as the SGLT2 inhibitors, also demonstrate benefits in reducing DN progression.</p><p><strong>Conclusion: </strong>While ACE inhibitors, ARBs, and SGLT2 inhibitors remain central to DN management, the ACE2-Ang-(1-7)-Mas axis presents a promising therapeutic target. Future research should focus on translating preclinical findings into clinical applications, potentially improving DN treatment.</p>","PeriodicalId":18548,"journal":{"name":"Mini reviews in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":3.3,"publicationDate":"2025-02-06","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143399473","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}
引用次数: 0
Smart Applications of Lanthanide Chelates-based Luminescent Probes in Bio-Imaging.
IF 3.3 3区 医学 Q2 CHEMISTRY, MEDICINAL Pub Date : 2025-01-29 DOI: 10.2174/0113895575350677250101060606
Maria Chiara Santangelo, Leonardo Lucchesi, Leonardo Papa, Annachiara Rossi, Gaia Egizzo, Giusy Laura Fratello, Lucilla Favero, Mauro Pineschi, Valeria Di Bussolo, Sebastiano Di Pietro

Luminescent Lanthanide (III) (Ln(III)) bioprobes (LLBs) have been extensively used in the last two decades as intracellular molecular probes in bio-imaging for the efficient revelation of analytes, to signal intracellular events (enzymes/protein activity, antigen-antibody interaction), target specific organelles, and determine parameters of particular biophysical interest, to gain important insights on pathologies or diseases. The choice of using a luminescent Ln(III) coordination compound with respect to a common organic fluorophore is intimately connected to how their photophysical sensitization (antenna effect) can be finely tuned and especially triggered to respond (even quantitatively) to a certain biophysical event, condition or analyte. While there are other reviews focused on how to design chromophoric ligands for an efficient sensitization of Ln(III) ions, both in the visible and NIR region, this review is application-driven: it is a small collection of particularly interesting examples where the LLB's emissive information is acquired by imaging the emission intensity and/or the fluorescence lifetime (fluorescence lifetime imaging microscopy, FLIM).

{"title":"Smart Applications of Lanthanide Chelates-based Luminescent Probes in Bio-Imaging.","authors":"Maria Chiara Santangelo, Leonardo Lucchesi, Leonardo Papa, Annachiara Rossi, Gaia Egizzo, Giusy Laura Fratello, Lucilla Favero, Mauro Pineschi, Valeria Di Bussolo, Sebastiano Di Pietro","doi":"10.2174/0113895575350677250101060606","DOIUrl":"https://doi.org/10.2174/0113895575350677250101060606","url":null,"abstract":"<p><p>Luminescent Lanthanide (III) (Ln(III)) bioprobes (LLBs) have been extensively used in the last two decades as intracellular molecular probes in bio-imaging for the efficient revelation of analytes, to signal intracellular events (enzymes/protein activity, antigen-antibody interaction), target specific organelles, and determine parameters of particular biophysical interest, to gain important insights on pathologies or diseases. The choice of using a luminescent Ln(III) coordination compound with respect to a common organic fluorophore is intimately connected to how their photophysical sensitization (antenna effect) can be finely tuned and especially triggered to respond (even quantitatively) to a certain biophysical event, condition or analyte. While there are other reviews focused on how to design chromophoric ligands for an efficient sensitization of Ln(III) ions, both in the visible and NIR region, this review is application-driven: it is a small collection of particularly interesting examples where the LLB's emissive information is acquired by imaging the emission intensity and/or the fluorescence lifetime (fluorescence lifetime imaging microscopy, FLIM).</p>","PeriodicalId":18548,"journal":{"name":"Mini reviews in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":3.3,"publicationDate":"2025-01-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143066810","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}
引用次数: 0
The Application of the Pyrazole Structure in the Structural Modification of Natural Products.
IF 3.3 3区 医学 Q2 CHEMISTRY, MEDICINAL Pub Date : 2025-01-23 DOI: 10.2174/0113895575359419241211092252
Fu-Qun Sun, Ya-Lan Wang, Ke Sun, Fei-Xia Yue, Yun-Xia Sun, Jia-Hong Ju, Zhan-Hui Jin, Qing-Kun Shen, Hong-Yan Guo, Mei-Hui Liu, Zhe-Shan Quan

Most natural products in nature have broad but not exceedingly good biological activities. The pyrazole structure has been introduced into natural products due to its suitability for various synthetic methods and its broad pharmacological activities. This article provides a detailed introduction to the anti-inflammatory, antibacterial, antifungal, antiviral, and anti-Alzheimer disease activities of pyrazole-modified natural product derivatives, particularly their anti-tumor activity. It is worth noting that compared to lead compounds, most natural product derivatives modified with pyrazole exhibit excellent pharmacological activity. Some of these derivatives exhibit outstanding anti-tumor activity, with IC50 values reaching nanomolar levels. This review provides more research directions and choices for future studies on natural products.

{"title":"The Application of the Pyrazole Structure in the Structural Modification of Natural Products.","authors":"Fu-Qun Sun, Ya-Lan Wang, Ke Sun, Fei-Xia Yue, Yun-Xia Sun, Jia-Hong Ju, Zhan-Hui Jin, Qing-Kun Shen, Hong-Yan Guo, Mei-Hui Liu, Zhe-Shan Quan","doi":"10.2174/0113895575359419241211092252","DOIUrl":"https://doi.org/10.2174/0113895575359419241211092252","url":null,"abstract":"<p><p>Most natural products in nature have broad but not exceedingly good biological activities. The pyrazole structure has been introduced into natural products due to its suitability for various synthetic methods and its broad pharmacological activities. This article provides a detailed introduction to the anti-inflammatory, antibacterial, antifungal, antiviral, and anti-Alzheimer disease activities of pyrazole-modified natural product derivatives, particularly their anti-tumor activity. It is worth noting that compared to lead compounds, most natural product derivatives modified with pyrazole exhibit excellent pharmacological activity. Some of these derivatives exhibit outstanding anti-tumor activity, with IC50 values reaching nanomolar levels. This review provides more research directions and choices for future studies on natural products.</p>","PeriodicalId":18548,"journal":{"name":"Mini reviews in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":3.3,"publicationDate":"2025-01-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143033554","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}
引用次数: 0
Drug Repurposing: A Conduit to Unravelling Metabolic Reprogramming for Cancer Treatment. 药物再利用:揭示癌症治疗中代谢重编程的途径。
IF 3.3 3区 医学 Q2 CHEMISTRY, MEDICINAL Pub Date : 2025-01-17 DOI: 10.2174/0113895575339660250106093738
Shristy Chaudhary, Abhilash Rana, Seema Bhatnagar

Metabolic reprogramming is a hallmark of cancer. Distinct and unusual metabolic aberrations occur during tumor development that lead to the growth and development of tumors. Oncogenic signaling pathways eventually converge to regulate three major metabolic pathways in tumor cells i.e., glucose, lipid, and amino acid metabolism. Therefore, identifying and targeting the metabolic nodes of cancer cells can be a promising intervention and therapeutic strategy for patients with malignancies. The long road of new drug discovery for cancer therapy has necessitated relooking alternative strategies such as drug repurposing. Advanced genomic and proteomic technologies for the assessment of cancer-specific biological pathways have led to the discovery of new drug targets, which provide excellent opportunities for drug repurposing. The development of effective, safe, cheaper, and readily available anticancer agents is the need of the hour, and drug repurposing has the potential to break the current drug shortage bottleneck. This review will accordingly cover various metabolic pathways that are aberrant in cancer, and strategies for targeting metabolic reprogramming by using repurposed drugs.

代谢重编程是癌症的一个标志。在肿瘤发育过程中,不同寻常的代谢异常导致肿瘤的生长和发展。致瘤信号通路最终汇聚调节肿瘤细胞中葡萄糖、脂质和氨基酸代谢三大代谢途径。因此,识别和靶向癌细胞的代谢节点可能是一种很有希望的恶性肿瘤患者的干预和治疗策略。癌症治疗新药发现的漫长道路已经需要重新审视替代策略,如药物再利用。用于评估癌症特异性生物学途径的先进基因组学和蛋白质组学技术已经导致新的药物靶点的发现,这为药物再利用提供了极好的机会。开发有效、安全、廉价、易得的抗癌药物是当务之急,药物再利用有可能打破目前药物短缺的瓶颈。这篇综述将涵盖癌症中各种异常的代谢途径,以及通过使用重组药物靶向代谢重编程的策略。
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引用次数: 0
Sustainable Synthesis of Medicinally Important Heterocycles. 药用重要杂环化合物的可持续合成。
IF 3.3 3区 医学 Q2 CHEMISTRY, MEDICINAL Pub Date : 2025-01-16 DOI: 10.2174/0113895575341409241201171848
Dripta De Joardar, Rajarshi Sarkar, Dilip K Maiti

Sustainable chemistry and nature-friendly protocols are not only luxury but has become essential requirement for the modern society as it progresses towards a more responsible future. To match the current needs of the community, industries and in particular chemical industry is looking for novel and cheap strategies that have less adverse effects on the environment. Heterocyclic compounds are one particular motif, which is prevalent in nature. It is found in a wide range of synthetic and natural compounds, both established and in development as potent therapeutic candidates. According to the US retail market in 2014-2015, heterocyclic moieties constitute the basic skeletons for 80% of marketed pharmaceuticals. However, majority of the synthetic methodologies still uses classical approaches with toxic solvents, stoichiometric reagents, reactions with less atom economy etc. Thus, there is an urgent need for green, sustainable alternatives of the classical reactions. In recent years, an array of diverse approaches and technologies have been discovered by the scientific community to address the issue of eco-friendly manufacture of various pharmaceutically and medicinally important heterocyclic molecules. In this context, the current review will summarize various reported green pathways to the heterocyclic architecture, particularly O, N, and S-heterocyclic compounds. The methods highlighted in this article includes reaction in environment friendly nonconventional media, solvent-free approaches, heterogeneous catalysis, organocatalysis, electrochemical reactions, microwave-mediated reactions, ultrasound-based reactions, enzymatic reactions, biocatalysis, and others.

可持续化学和自然友好型协议不仅是奢侈品,而且已经成为现代社会的基本要求,因为它朝着更负责任的未来发展。为了配合社会目前的需要,工业,特别是化学工业正在寻找对环境不利影响较小的新颖和廉价的战略。杂环化合物是自然界中普遍存在的一种特殊基序。它存在于广泛的合成和天然化合物中,无论是已经建立的还是正在开发的强有力的治疗候选者。根据2014-2015年美国零售市场的数据,杂环部分构成了80%上市药品的基本骨架。然而,大多数的合成方法仍然采用经典的方法,使用有毒溶剂、化学计量试剂、原子经济性差的反应等。因此,迫切需要绿色,可持续的替代经典反应。近年来,科学界已经发现了一系列不同的方法和技术来解决各种具有重要药用价值的杂环分子的生态制造问题。在此背景下,本综述将总结各种报道的绿色途径,特别是O, N和s杂环化合物。本文重点介绍的方法包括在环境友好型非常规介质中的反应、无溶剂方法、多相催化、有机催化、电化学反应、微波介导反应、超声反应、酶促反应、生物催化等。
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引用次数: 0
Topical Application onto the Eyelid Skin: Is it a Feasible Delivery Route of Ophthalmic Drugs? 眼睑皮肤外用:眼科药物的一种可行的给药途径吗?
IF 3.3 3区 医学 Q2 CHEMISTRY, MEDICINAL Pub Date : 2025-01-13 DOI: 10.2174/0113895575358373241220043138
Larysa Grygor'yeva, Manuela Colla Carvalheiro, Sandra Simões

Topical application of ophthalmic drugs remains to be the preferred delivery method. Eye drops lead the pharmaceutical forms due to ease of application. Despite the poor bioavailability of drugs administered topically, especially related to the dilution and excretion by tear fluid, the absence of controlled drug delivery, and the poor compliance within pediatric and senior populations, eye drops and ointments are still the first choices in eye--related disorders management. Only a few studies have explored the eyelid skin as a site for drug application and transdermal delivery as an alternative route of administration of ophthalmic drugs. Such works have validated the delivery of drugs into the ocular tissues through the eyelid barrier. The eyelid represents a differentiated skin barrier concerning the thickness, the structure of the stratum corneum, the vasculature, and the amount of lipids. This work intends to question why the eyelid, being an accessible, non-invasive, comfortable route of administration is not considered a feasible route for ophthalmic drugs. The eyelid structure is presented, and the anatomical and physiological distinctive characteristics are presented. The work also presents the research work on topical drug application to the eyelid skin that has been published so far.

眼用药物外用仍是首选的给药方式。眼药水由于易于使用而领先于药物形式。尽管局部给药的生物利用度较差,特别是与泪液的稀释和排泄有关,缺乏控制的药物输送,以及儿童和老年人依从性差,但眼药水和软膏仍然是眼相关疾病管理的首选。只有少数研究探索了眼睑皮肤作为药物施用部位和经皮给药作为眼科药物给药的替代途径。这些工作已经证实了通过眼睑屏障将药物输送到眼部组织。眼睑代表了一种与厚度、角质层结构、脉管系统和脂质含量有关的分化的皮肤屏障。这项工作旨在质疑为什么眼睑,作为一个可接近的,非侵入性的,舒适的给药途径不被认为是一个可行的途径眼科药物。提出了眼睑的结构,并提出了解剖和生理上的鲜明特征。并介绍了迄今为止已发表的关于眼睑皮肤外用药物的研究工作。
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引用次数: 0
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Mini reviews in medicinal chemistry
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