Mini reviews in medicinal chemistry最新文献_第5页

Therapeutic Potental of Quinolin-2H-one Hybrids as Anticancer Agents. 喹啉-2H-酮混合物作为抗癌剂的治疗潜力。

IF 3.3 3区医学

Mini reviews in medicinal chemistry Pub Date : 2025-01-01 DOI: 10.2174/0113895575305597240912192037

Naik Soniya, Vasu Soumya, Mamle Desai Shivlingrao, Manickavasagam M, Chellappan Meeramol

{"title":"Therapeutic Potental of Quinolin-2H-one Hybrids as Anticancer Agents.","authors":"Naik Soniya, Vasu Soumya, Mamle Desai Shivlingrao, Manickavasagam M, Chellappan Meeramol","doi":"10.2174/0113895575305597240912192037","DOIUrl":"10.2174/0113895575305597240912192037","url":null,"abstract":"The statistical data related to cancer in recent years has shown a great increase in the number of cases and is likely to further increase in the future. Even after seeking thorough knowledge on the aetiology of cancer and related disorders and attempting to cure it by various methods like gene therapy, T cell therapy, chemotherapy, surgery, hormone therapy, and photodynamic therapy, there has always been disappointment concerning the survival rate. Hence, there is still a great urge for the discovery of novel drugs for the treatment of cancer. Chemotherapy being one of the widely used methods, several drug entities possessing anticancer properties are already in the market but none of them is known to show good efficacy which necessitates researchers to design newer drugs for the treatment of cancer. The urge to synthesize novel anticancer entities directed researchers towards molecular hybridization as one of the novel methods for designing newer drugs. Literature reveals wide research carried out on quinolin-2-one hybrids, possessing anticancer properties through different mechanisms. Tipifarnib and Dovitinib are quinolin-2-one hybrids used to treat cancer, possessing imidazole and benzimidazole heterocyclic rings. Different heterocyclic scaffolds such as pyrone, pyrrole, pyrimidine, pyridine, thiazole, and pyrazole in combination with heterocyclic quinolin-2-one have shown high potential to become lead for newer anticancer agents with better and wider therapeutic properties and lesser side effects. The current review presents information on the different quinolin-2-one hybrids and their effect on different cancer cell lines. It also imparts knowledge of the structural requirements for designing novel anticancer agents.","PeriodicalId":18548,"journal":{"name":"Mini reviews in medicinal chemistry","volume":" ","pages":"386-402"},"PeriodicalIF":3.3,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142349791","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

Olaparib: A Chemosensitizer for the Treatment of Glioblastoma. 奥拉帕利治疗胶质母细胞瘤的化疗增敏剂。

IF 3.3 3区医学

Mini reviews in medicinal chemistry Pub Date : 2025-01-01 DOI: 10.2174/0113895575318854241014101928

Naresh Dhanavath, Priya Bisht, Mohini Santosh Jamadade, Krishna Murti, Pranay Wal, Nitesh Kumar

{"title":"Olaparib: A Chemosensitizer for the Treatment of Glioblastoma.","authors":"Naresh Dhanavath, Priya Bisht, Mohini Santosh Jamadade, Krishna Murti, Pranay Wal, Nitesh Kumar","doi":"10.2174/0113895575318854241014101928","DOIUrl":"10.2174/0113895575318854241014101928","url":null,"abstract":"Glioblastoma (GBM) is the most prevalent and deadly primary brain tumor. The current treatment for GBM includes adjuvant chemotherapy with temozolomide (TMZ), radiation therapy, and surgical tumor excision. There is still an issue because 50% of patients with GBM who get TMZ have low survival rates due to TMZ resistance. The activation of several DNA repair mechanisms, such as Base Excision Repair (BER), DNA Mismatch Repair (MMR), and O-6- Methylguanine-DNA Methyltransferase (MGMT), is the main mechanism via which TMZ resistance develops. The zinc-finger DNA-binding enzyme poly (ADP-ribose) polymerase-1 (PARP1), which is activated by binding to DNA breaks, affects the activation of the MGMT, BER, and MMR pathway deficiency, which results in TMZ resistance in GBM. PARP inhibitors have been studied recently as sensitizing medications to increase TMZ potency. The first member of the PARP inhibitor family to be identified was Olaparib. It inhibits PARP1 and PARP2, which causes apoptosis in cancer cells and DNA strand break. Olaparib is currently investigated as a radio- and/or chemo-sensitizer in addition to being used as a single agent because it may increase the cytotoxic effects of other treatments. This review addresses Olaparib and its significance in treating TMZ resistance in GBM.","PeriodicalId":18548,"journal":{"name":"Mini reviews in medicinal chemistry","volume":" ","pages":"374-385"},"PeriodicalIF":3.3,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142503757","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

An Outline on Benzimidazole Containing Marketed Drugs with Proton Pump Inhibitor and H₁ Receptor Antagonist Activities. 苯并咪唑类具有质子泵抑制剂和H1受体拮抗剂活性的市售药物概述。

IF 3.3 3区医学

Mini reviews in medicinal chemistry Pub Date : 2025-01-01 DOI: 10.2174/0113895575329633240928163509

Sumit Tahlan, Sucheta Singh, Kailash C Pandey, Kuldeep Singh

{"title":"An Outline on Benzimidazole Containing Marketed Drugs with Proton Pump Inhibitor and H1 Receptor Antagonist Activities.","authors":"Sumit Tahlan, Sucheta Singh, Kailash C Pandey, Kuldeep Singh","doi":"10.2174/0113895575329633240928163509","DOIUrl":"10.2174/0113895575329633240928163509","url":null,"abstract":"Heterocyclic compounds are increasingly used in medicinal chemistry because they are the main components of many biological processes and materials. Benzimidazole remains the core center of the heterocyclic chemical group, with essential traits such as six-five-member connected rings and two nitrogen atoms at the 1,3 position in a six-membered benzene and five-membered imidazole- fused ring system. Molecules with benzimidazole derivatives serve important functions as therapeutic agents and have shown excellent results in clinical and biological research. In this comprehensive review, we summarize marketed medications that include the benzimidazole moiety. Here, we discuss two topics: PPIs and H1 receptor antagonists. Benzimidazole derivatives are important in all fields because they have the same isostructural pharmacophore as that of naturally occurring active biomolecules. While PPIs and H1 receptor antagonists are generally safe in the short term, accumulating data suggest that their long-term use may pose concerns. This systematic review aimed to assess global PPI use in the general population. This will help researchers, medicinal chemists, and pharmaceutical scientists to create breakthrough benzimidazole-based drugs. This review can help identify novel lead compounds and optimize existing benzimidazole derivatives to improve medicinal efficacy. Benzimidazole has attracted significant interest because of its high bioavailability, stability, and biological efficiency. This page reveals and discusses typical synthesis processes for marketed pharmaceuticals in the benzimidazole class of scaffolds, MOA, and therapeutic uses.","PeriodicalId":18548,"journal":{"name":"Mini reviews in medicinal chemistry","volume":" ","pages":"440-462"},"PeriodicalIF":3.3,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142951195","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

An Overview of Pyridazinone Analogs: Chemical and Pharmacological Potential. 哒嗪酮类似物概述：化学和药理潜力。

IF 3.3 3区医学

Mini reviews in medicinal chemistry Pub Date : 2025-01-01 DOI: 10.2174/0113895575287746240528072330

Youness Boukharsa, Khalid Karrouchi, Houda Attjioui, M'Hammed Ansar

引用次数: 0

New Insights into the Modifications and Bioactivities of Indole-3- Carboxaldehyde and its Derivatives as a Potential Scaffold for Drug Design: A Mini-Review. 吲哚-3-甲醛及其衍生物作为药物设计潜在支架的修饰和生物活性的新见解：综述

IF 3.3 3区医学

Mini reviews in medicinal chemistry Pub Date : 2025-01-01 DOI: 10.2174/0113895575351704241120060746

Nuhu Abdullahi Mukhtar, Mustapha Suleiman, Helmi Mohammed Al-Maqtari, Kumitaa Theva Das, Ajmal R Bhat, Joazaizulfazli Jamalis

{"title":"New Insights into the Modifications and Bioactivities of Indole-3- Carboxaldehyde and its Derivatives as a Potential Scaffold for Drug Design: A Mini-Review.","authors":"Nuhu Abdullahi Mukhtar, Mustapha Suleiman, Helmi Mohammed Al-Maqtari, Kumitaa Theva Das, Ajmal R Bhat, Joazaizulfazli Jamalis","doi":"10.2174/0113895575351704241120060746","DOIUrl":"10.2174/0113895575351704241120060746","url":null,"abstract":"Indole, a ubiquitous structural motif in bioactive compounds, has played a pivotal role in drug discovery. Among indole derivatives, indole-3-carboxaldehyde (I3A) has emerged as a particularly promising scaffold for the development of therapeutic agents. This review delves into the recent advancements in the chemical modification of I3A and its derivatives, highlighting their potential applications in various therapeutic areas. I3A derivatives have demonstrated a wide range of biological activities, including anti-inflammatory, anti-leishmanial, anti-cancer, anti-bacterial, antifungal, and anti-HIV properties. The structural modifications introduced to the I3A scaffold, such as substitutions on the indole ring (alkylation/arylation/halogenation), variations in the aldehyde group via condensation (Aldol/Claisen/Knoevenagel), and molecular hybridization with other reputable bioactive compounds like coumarins, chalcones, triazoles, and thiophenes, contribute to these activities. Beyond its therapeutic potential, I3A has also found applications as a ligand for Schiff base synthesis, a polymer, and a chromophore. This review provides a comprehensive overview of the latest research on I3A and its derivatives, focusing on the key reactions, modification pathways, reaction conditions, yields, and associated therapeutic activities. By understanding these advancements, researchers can gain valuable insights into the potential applications and future directions for I3A-based drug discovery.","PeriodicalId":18548,"journal":{"name":"Mini reviews in medicinal chemistry","volume":" ","pages":"480-503"},"PeriodicalIF":3.3,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142951215","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

Energy Metabolism Behavior and Response to Microenvironmental Factors of the Experimental Cancer Cell Models Differ from that of Actual Human Tumors. 实验癌细胞模型的能量代谢行为和对微环境因素的反应与实际人类肿瘤不同

IF 3.3 3区医学

Mini reviews in medicinal chemistry Pub Date : 2025-01-01 DOI: 10.2174/0113895575322436240924101642

Rafael Moreno-Sanchez, Jorge Luis Vargas-Navarro, Joaquin Alberto Padilla-Flores, Diana Xochiquetzal Robledo-Cadena, Juan Carlos Granados-Rivas, Rutt Taba, Anton Terasmaa, Giuseppe Leonardo Auditano, Tuuli Kaambre, Sara Rodriguez-Enriquez

{"title":"Energy Metabolism Behavior and Response to Microenvironmental Factors of the Experimental Cancer Cell Models Differ from that of Actual Human Tumors.","authors":"Rafael Moreno-Sanchez, Jorge Luis Vargas-Navarro, Joaquin Alberto Padilla-Flores, Diana Xochiquetzal Robledo-Cadena, Juan Carlos Granados-Rivas, Rutt Taba, Anton Terasmaa, Giuseppe Leonardo Auditano, Tuuli Kaambre, Sara Rodriguez-Enriquez","doi":"10.2174/0113895575322436240924101642","DOIUrl":"10.2174/0113895575322436240924101642","url":null,"abstract":"Analysis of the biochemical differences in the energy metabolism among bi-dimensional (2D) and tri-dimensional (3D) cultured cancer cell models and actual human tumors was undertaken. In 2D cancer cells, the oxidative phosphorylation (OxPhos) fluxes range is 2.5-19 nmol O2/min/mg cellular protein. Hypoxia drastically decreased OxPhos flux by 2-3 times in 2D models, similar to what occurs in mature multicellular tumor spheroids (MCTS), a representative 3D cancer cell model. However, mitochondrial protein contents and enzyme activities were significantly different between both models. Moreover, glycolytic fluxes were also significantly different between 2D and MCTS. The glycolytic flux range in 2D models is 1-34 nmol lactate/min/mg cellular protein, whereas in MCTS the range of glycolysis fluxes is 60-80 nmol lactate/min/mg cellular. In addition, sensitivity to anticancer canonical and metabolic drugs was greater in MCTS than in 2D. Actual solid human tumor samples show lower (1.6-4.5 times) OxPhos fluxes compared to normoxic 2D cancer cell cultures. These observations indicate that tridimensional organization provides a unique microenvironment affecting tumor physiology, which has not been so far faithfully reproduced by the 2D environment. Thus, the analysis of the resemblances and differences among cancer cell models undertaken in the present study raises caution on the interpretation of results derived from 2D cultured cancer cells when they are extended to clinical settings. It also raises awareness about detecting which biological and environmental factors are missing in 2D and 3D cancer cell models to be able to reproduce the actual human tumor behavior.","PeriodicalId":18548,"journal":{"name":"Mini reviews in medicinal chemistry","volume":" ","pages":"319-339"},"PeriodicalIF":3.3,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142469747","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

Promising Inhibitors of Endocannabinoid Degrading Enzymes Sharing a Carbamate Scaffold. 共享氨基甲酸酯支架的内源性大麻素降解酶的有望抑制剂。

IF 3.3 3区医学

Mini reviews in medicinal chemistry Pub Date : 2024-11-25 DOI: 10.2174/0113895575328120241107061303

Shivani Jaiswal, Senthil Raja Ayyannan

{"title":"Promising Inhibitors of Endocannabinoid Degrading Enzymes Sharing a Carbamate Scaffold.","authors":"Shivani Jaiswal, Senthil Raja Ayyannan","doi":"10.2174/0113895575328120241107061303","DOIUrl":"https://doi.org/10.2174/0113895575328120241107061303","url":null,"abstract":"Carbamate has been extensively used as a scaffold in the recent era of drug discovery and is a common structural motif of many approved drugs. The carbamate moiety's unique amide-ester hybrid (-O-CO-NH-) feature offers the designing of specific drug-target interactions. Despite the discovery of numerous carbamate derivatives that act on the endocannabinoid system (ECS), the development of clinically effective carbamates remains a challenge. In this review, we highlight the therapeutic potential of carbamate inhibitors of endocannabinoid degrading enzymes as a breakthrough in discovering neurotherapeutic drugs. We discuss the design strategies and medicinal chemistry aspects involved in developing carbamate-based molecular architectures that modulate the endocannabinoid signaling pathway by interfering with fatty acid amide hydrolase (FAAH), monoacylglycerol lipase (MAGL), and α/β-Hydrolase domain-containing 6 (ABHD6). Additionally, we highlight the dual activity profile of carbamates against FAAH and MAGL, FAAH and cholinesterase, and FAAH and TRPV1 channels. Furthermore, we illustrate the pharmacophores of O-functionalized carbamates and N-cyclic carbamates that are crucial for FAAH and MAGL inhibitory activities, respectively.","PeriodicalId":18548,"journal":{"name":"Mini reviews in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":3.3,"publicationDate":"2024-11-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142730344","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

Trace Elements in Medicinal Metallomics. 药用金属组学中的微量元素。

IF 3.3 3区医学

Mini reviews in medicinal chemistry Pub Date : 2024-09-25 DOI: 10.2174/0113895575333766240912162252

Marina Orlova, Stepan Kalmykov, Tatiana Trofimova, Dmitry Kuznetsov

引用次数: 0

Phytochemicals and Nanotechnology: A Powerful Combination against Breast Cancer. 植物化学物质与纳米技术：抗击乳腺癌的强大组合。

IF 3.3 3区医学

Mini reviews in medicinal chemistry Pub Date : 2024-09-13 DOI: 10.2174/0113895575297312240903055926

Sadat Shafi, Faraha Ahmed, Ayesha Waheed, Syed Sufiyan Ahmad, Sana Khan, Mohammad Ahmed Khan, Faheem Hyder Pottoo, Syed Arman Rabbani, Shailja Singh, Abul Kalam Najmi

{"title":"Phytochemicals and Nanotechnology: A Powerful Combination against Breast Cancer.","authors":"Sadat Shafi, Faraha Ahmed, Ayesha Waheed, Syed Sufiyan Ahmad, Sana Khan, Mohammad Ahmed Khan, Faheem Hyder Pottoo, Syed Arman Rabbani, Shailja Singh, Abul Kalam Najmi","doi":"10.2174/0113895575297312240903055926","DOIUrl":"https://doi.org/10.2174/0113895575297312240903055926","url":null,"abstract":"Considerable advancements have been made in breast cancer therapeutics in the past few decades. However, the advent of chemo-resistance and adverse drug reactions coupled with tumor metastasis and recurrence posed a serious threat to combat this lethal disease. Novel anti-cancer agents, as well as new therapeutic strategies, are needed to complement conventional breast cancer therapies. The quest for developing novel anti-cancer drugs caused an upsurge in exploring and harnessing natural compounds, especially phytochemicals. Various research groups have explored and documented the anti-cancer potential of wide variety of phytochemical groups including flavonoids (curcumin, kaempferol, myricetin, quercetin, naringenin, apigenin, genistein epigallocatechin gallate), stilbenes (resveratrol), carotenoids (crocin, lycopene, lutein), and anthraquinone (Emodin). However, low chemical stability, poor water solubility, and short systemic half-life impede their clinical utility. The implication of nano-technological approaches to decode the pharmacokinetic challenges associated with phytochemical usage, as well as selective drug targeting, have markedly enhanced the pre-clinical anti-cancer activity, thus aiding in their clinical translation. This review documented the recent advances in utilizing phytochemicals for breast cancer prevention and lipidbased nanotechnological approaches for circumventing their pharmacokinetic concerns to enhance their systemic availability, cytotoxicity, and targeted delivery against breast cancer alone as well as in combination with conventional therapeutic agents.","PeriodicalId":18548,"journal":{"name":"Mini reviews in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":3.3,"publicationDate":"2024-09-13","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142290916","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

Chemistry, Analysis, and Biological Aspects of Daprodustat, A New Hypoxia Inducible Factor Prolyl Hydroxylase Inhibitor: A Comprehensive Review 一种新的缺氧诱导因子脯氨酰羟化酶抑制剂--达泊司他（Daprodustat）的化学、分析和生物学方面：全面综述

IF 3.8 3区医学

Mini reviews in medicinal chemistry Pub Date : 2024-04-30 DOI: 10.2174/0113895575293447240424052516

Roshani Patil, Sanjay Sharma

{"title":"Chemistry, Analysis, and Biological Aspects of Daprodustat, A New Hypoxia Inducible Factor Prolyl Hydroxylase Inhibitor: A Comprehensive Review","authors":"Roshani Patil, Sanjay Sharma","doi":"10.2174/0113895575293447240424052516","DOIUrl":"https://doi.org/10.2174/0113895575293447240424052516","url":null,"abstract":"Background: The National Health and Nutrition Examination Survey (NHANES) carried out a survey between 2007-10 and found that as compared to the general population, the prevalence of anemia in chronic kidney disease (CKD) patients was twice high. Daprodustat is an investigational novel drug for the treatment of renal anemia. Objective: The objective of this study is to provide a comprehensive review of chemistry, synthesis, pharmacology, pharmacokinetic, and bioanalytical methods for the analysis of Daprodustat. Methods: To improve understanding, a review was carried out by creating a database of relevant prior research from electronic sources such as ScienceDirect and PubMed. The methodology is shown in the flowchart of the literature selection process. Results: The drug was approved in 2020 for therapeutic purposes in Japan. It is a novel drug approved for the treatment of anemia in chronic kidney disease for oral administration. It is intended for adults who have undergone dialysis for a minimum of four months and are experiencing anemia as a result of chronic kidney disease. Conclusion: This review examines therapeutic, pharmacological, and analytical aspects related to the novel drug Daprodustat.","PeriodicalId":18548,"journal":{"name":"Mini reviews in medicinal chemistry","volume":"43 1","pages":""},"PeriodicalIF":3.8,"publicationDate":"2024-04-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140829260","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