Future medicinal chemistry最新文献_第10页

New cannabidiol structure-related terpene N-acyl-hydrazones with potent antinociceptive and anti-inflammatory activity. 具有有效抗炎和抗炎活性的新型大麻二酚结构相关萜烯n -酰基腙。

IF 3.2 4区医学

Future medicinal chemistry Pub Date : 2025-06-01 Epub Date: 2025-06-16 DOI: 10.1080/17568919.2025.2515821

Graziella Dos Reis Rosa Franco, Isabela Marie Fernandes, Mikaela Lucinda de Souza, Vanessa Silva Gontijo, Marina Amaral Alves, Hygor Marcos Ribeiro de Souza, Carla Gabriely Gaião Do Invencio, Anna Carolina Pereira Lontra, João Pedro Barros de Paiva, Larissa Do Nascimento Dos Santos, Ana Clara Machado da Silva, Thaís Biondino Sardella Giorno, Isabella Alvim Guedes, Laurent Emmanuel Dardenne, Patrícia Dias Fernandes, Claudio Viegas

{"title":"New cannabidiol structure-related terpene N-acyl-hydrazones with potent antinociceptive and anti-inflammatory activity.","authors":"Graziella Dos Reis Rosa Franco, Isabela Marie Fernandes, Mikaela Lucinda de Souza, Vanessa Silva Gontijo, Marina Amaral Alves, Hygor Marcos Ribeiro de Souza, Carla Gabriely Gaião Do Invencio, Anna Carolina Pereira Lontra, João Pedro Barros de Paiva, Larissa Do Nascimento Dos Santos, Ana Clara Machado da Silva, Thaís Biondino Sardella Giorno, Isabella Alvim Guedes, Laurent Emmanuel Dardenne, Patrícia Dias Fernandes, Claudio Viegas","doi":"10.1080/17568919.2025.2515821","DOIUrl":"10.1080/17568919.2025.2515821","url":null,"abstract":"Inflammation is the organism's protective mechanism to restore cellular and tissue homeostasis. Cannabidiol has been reported for its ability to bind to diverse receptors related to or not related to the endocannabinoid system, with good safety being one of the most promising phytocannabinoids for therapeutical purposes. CBD has shown in vitro and in vivo ability to significantly reduce the production of cytokines and other inflammatory mediators, with an unclear mechanism of action. Herein, we report the design and synthesis of a novel series of eight terpene N-acylaryl hydrazone analogues and their pharmacological evaluation for potential antioxidant, antinociceptive, and anti-inflammatory properties. Our results led to the identification of compounds 5a (PQM-242), with significant peripheral and central antinociceptive effects, 5b (PQM-243), and 5g (PQM-248) with antinociceptive activities probably related to the ability of modulation of TRPV1 receptors, and 5c (PQM-244) that seems to have the most promising peripheral antinociceptive profile, showing significant effects on both neurogenic and inflammatory phases of formalin-induced licking test, coupled to potential antioxidant activity. Overall, our experimental data suggest that the new CBD-based architecture is capable of ensuring peripheral and central antinociceptive effects by different modes of action, with no in vivo toxicity and adequate predicted ADME properties.","PeriodicalId":12475,"journal":{"name":"Future medicinal chemistry","volume":" ","pages":"1229-1240"},"PeriodicalIF":3.2,"publicationDate":"2025-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12279265/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144301569","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 quinoline-piperazines fused to a phenylhydrazinecarbothioamide scaffold as promising α-glucosidase inhibitors with anti-diabetic potential. 新型喹啉-哌嗪类苯肼碳硫酰胺支架的设计与合成，作为具有抗糖尿病潜力的α-葡萄糖苷酶抑制剂。

IF 3.2 4区医学

Future medicinal chemistry Pub Date : 2025-06-01 Epub Date: 2025-07-16 DOI: 10.1080/17568919.2025.2521252

Mehran Ghasemi, Fateme Bagheri, Fatemeh Sadat Khajeh Mohammadilar, Aida Iraji, Vahid Lotfi, Reza Karimi, Maryam Dehghan, Somayeh Mojtabavi, Mohammad Ali Faramarzi, Mohammad Mahdavi, Ahmed Al-Harrasi

{"title":"Design and synthesis of novel quinoline-piperazines fused to a phenylhydrazinecarbothioamide scaffold as promising α-glucosidase inhibitors with anti-diabetic potential.","authors":"Mehran Ghasemi, Fateme Bagheri, Fatemeh Sadat Khajeh Mohammadilar, Aida Iraji, Vahid Lotfi, Reza Karimi, Maryam Dehghan, Somayeh Mojtabavi, Mohammad Ali Faramarzi, Mohammad Mahdavi, Ahmed Al-Harrasi","doi":"10.1080/17568919.2025.2521252","DOIUrl":"10.1080/17568919.2025.2521252","url":null,"abstract":"Aims: This study focused on the design, synthesis, and dual in vitro/in silico evaluation of novel quinoline-benzoylhydrazine derivatives as α-glucosidase inhibitor for the management of hyperglycemia and type 2 diabetes mellitus.Materials & methods: A series of quinoline-benzoylhydrazine compounds were synthesized and evaluated as α-glucosidase inhibitors. The most active compound was subjected to the kinetic study plus molecular docking and molecular dynamics simulations to elucidate the mechanism of inhibition and stability.Results: All synthesized compounds exhibited strong α-glucosidase inhibition. Among them, 7j was the most active, with an IC50 value of 1.0 µM, approximately 750-fold more potent than acarbose. SAR confirmed that electron-donating groups increased the inhibitory potency. Molecular docking for 7j disclosed a binding energy value of -11.884 kcal/mol, with π-π stacking interactions with aromatic residues, hydrophobic contacts with Pro309, and hydrogen bonds with His239. MD simulations further indicated that the complex formed between 7j and the enzyme was stable, with limited conformational fluctuations.Conclusion: The results confirm that quinoline-piperazine derivatives bearing phenylhydrazinecarbothioamide moieties are promising scaffolds for α-glucosidase inhibition.","PeriodicalId":12475,"journal":{"name":"Future medicinal chemistry","volume":" ","pages":"1217-1227"},"PeriodicalIF":3.2,"publicationDate":"2025-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12279276/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144642217","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

Therapeutic potential of morpholine-based compounds in neurodegenerative diseases: SAR insights and analysis. 基于吗啡的化合物在神经退行性疾病中的治疗潜力：SAR的见解和分析。

IF 3.4 4区医学

Future medicinal chemistry Pub Date : 2025-06-01 Epub Date: 2025-06-08 DOI: 10.1080/17568919.2025.2515812

Suresh Kumar, Poonam Bishnoi, Naveen Chauhan, Prince Kumar, Ranjana Aggarwal

{"title":"Therapeutic potential of morpholine-based compounds in neurodegenerative diseases: SAR insights and analysis.","authors":"Suresh Kumar, Poonam Bishnoi, Naveen Chauhan, Prince Kumar, Ranjana Aggarwal","doi":"10.1080/17568919.2025.2515812","DOIUrl":"10.1080/17568919.2025.2515812","url":null,"abstract":"Neurodegenerative diseases are progressive conditions marked by the deterioration of neuronal structure and function, often resulting from enzyme dysregulation and disrupted cellular communication, necessitating innovative treatment approaches. Morpholine, a versatile heterocyclic compound, has gained attention for its broad pharmacological activities and its role in modulating critical enzymes implicated in neurodegenerative processes, including acetylcholinesterase (AChE), butyrylcholinesterase (BuChE), and monoamine oxidases (MAO-A and MAO-B). This review presents a structure-based approach to understanding and optimizing morpholine-clubbed heterocycles, offering insights into SAR, synthetic strategies, and pharmacokinetics to facilitate the rational design of anti-neurodegenerative agents. By compiling and analyzing recent advancements (2019-2024), we identify key molecular features that enhance the efficacy, selectivity, and drug likeliness of the derivatives, which are crucial for drug development. Additionally, we discuss an overview of synthetic approaches to prepare diversely functionalized morpholine hybrids, enabling the design of novel and more effective derivatives of enhanced therapeutic potency. Our coverage of various pharmacokinetics properties and in silico studies further aids in optimizing lead compounds for improved bioavailability and reduced toxicity, providing valuable insight into their clinical translatability. By integrating these insights, this review serves as a framework for advancing drug design, providing the way for next-generation morpholine-based therapeutics against neurodegenerative disorders.","PeriodicalId":12475,"journal":{"name":"Future medicinal chemistry","volume":" ","pages":"1439-1455"},"PeriodicalIF":3.4,"publicationDate":"2025-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12296110/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144247334","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

Pyrimidine hybrids with in vivo anticancer therapeutic potential. 具有体内抗癌治疗潜力的嘧啶杂合体。

IF 3.4 4区医学

Future medicinal chemistry Pub Date : 2025-06-01 Epub Date: 2025-06-11 DOI: 10.1080/17568919.2025.2517533

Junna Liu, Xiaoyan Zhang, Yafei Zhuang, Zhi Xu, Wei Zhou

{"title":"Pyrimidine hybrids with in vivo anticancer therapeutic potential.","authors":"Junna Liu, Xiaoyan Zhang, Yafei Zhuang, Zhi Xu, Wei Zhou","doi":"10.1080/17568919.2025.2517533","DOIUrl":"10.1080/17568919.2025.2517533","url":null,"abstract":"Chemotherapy has transformed cancer from a catastrophic disease to a treatable and sometimes curable disease, but multidrug resistance is a predominant obstacle to effective chemotherapy, creating an urgent demand to explore novel anticancer therapeutics. Pyrimidine is necessary to maintain cellular fundamental function and is critical in cancer cell proliferation as well as survival, and some pyrimidine-based agents have been developed as anticancer therapeutics. In particular, pyrimidine hybrids can act on distinct biological targets in cancer cells simultaneously and have potential advantages in increasing anticancer therapeutic efficacy and circumventing drug resistance, indicating that the rational design of pyrimidine hybrids may provide valuable therapeutic interventions for cancer therapy. This review outlines the current scenario of the in vivo anticancer therapeutic potential of pyrimidine hybrids, together with pharmacokinetic properties, toxicity, and modes of action developed from 2020 onwards, aiming to provide potential candidates for further preclinical/clinical evaluations and facilitate the rational design of more candidates.","PeriodicalId":12475,"journal":{"name":"Future medicinal chemistry","volume":" ","pages":"1471-1488"},"PeriodicalIF":3.4,"publicationDate":"2025-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12296079/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144265937","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

Sulfur/selenium-functionalized benzotriazoles as multifunctional antivirals targeting Zika & Chikungunya. 硫/硒功能化苯并三唑作为靶向寨卡病毒和基孔肯雅热的多功能抗病毒药物。

IF 3.4 4区医学

Future medicinal chemistry Pub Date : 2025-06-01 Epub Date: 2025-07-08 DOI: 10.1080/17568919.2025.2525068

Luana S Gomes, Claudio C Cirne-Santos, Caroline de S Barros, Rafael R Batista, Matheus R de P Ignacio, Aldo S de Oliveira, Célia M Ronconi, Izabel C N de Palmer Paixão, Vanessa Nascimento

{"title":"Sulfur/selenium-functionalized benzotriazoles as multifunctional antivirals targeting Zika & Chikungunya.","authors":"Luana S Gomes, Claudio C Cirne-Santos, Caroline de S Barros, Rafael R Batista, Matheus R de P Ignacio, Aldo S de Oliveira, Célia M Ronconi, Izabel C N de Palmer Paixão, Vanessa Nascimento","doi":"10.1080/17568919.2025.2525068","DOIUrl":"10.1080/17568919.2025.2525068","url":null,"abstract":"Aims: Emerging arboviruses such as Zika virus (ZIKV) and Chikungunya virus (CHIKV) remain significant public health threats. This study aimed to evaluate the antiviral potential of six organochalcogen compounds against ZIKV and CHIKV.Materials & methods: Compounds were assessed for cytotoxicity and antiviral activity in Vero cells. Antiviral effects were determined using plaque reduction assays, time-of-addition studies, viral adsorption, and virucidal assays. Molecular docking and density functional theory (DFT) calculations were performed to investigate interactions with viral targets and electronic properties.Results: Compounds 4, 7, 8, and 9 exhibited potent antiviral activity with low cytotoxicity, demonstrating effective inhibition of viral replication with half-maximal effective concentration (EC₅₀) values in the micromolar range and favorable selectivity indices. Mechanistic assays revealed that the compounds interfered with viral adsorption, exhibited virucidal effects, and inhibited multiple stages of the replication cycle. Docking studies confirmed strong binding to key viral enzymes, supported by HOMO (half-maximal effective concentration) - LUMO (lowest unoccupied molecular orbital) analysis.Conclusions: These findings highlight organochalcogen compounds as promising dual-action antiviral candidates with broad-spectrum activity against ZIKV and CHIKV. Further preclinical investigations are warranted to explore their therapeutic potential.","PeriodicalId":12475,"journal":{"name":"Future medicinal chemistry","volume":" ","pages":"1363-1375"},"PeriodicalIF":3.4,"publicationDate":"2025-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12296112/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144583481","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

Methoxy group: a non-lipophilic "scout" for protein pocket finding. 甲氧基：寻找蛋白质口袋的非亲脂性“侦察兵”。

IF 3.2 4区医学

Future medicinal chemistry Pub Date : 2025-05-01 Epub Date: 2025-04-03 DOI: 10.1080/17568919.2025.2485865

Debora Chiodi, Yoshihiro Ishihara

引用次数: 0

Larvicidal potential of Knoevenagel adducts against Aedes aegypti: theoretical study and in vitro validation. Knoevenagel加合物对埃及伊蚊的杀幼虫潜力：理论研究和体外验证。

IF 3.2 4区医学

Future medicinal chemistry Pub Date : 2025-05-01 Epub Date: 2025-05-05 DOI: 10.1080/17568919.2025.2498877

Paloma G Abrantes, Poliana G Abrantes, Renata R Magalhães, Gildilayne M Silva, Natália F Sousa, Marcus T Scotti, Renan T Leite, Jheison M C Francelino, Fabíola C Nunes, Juliana A Vale

{"title":"Larvicidal potential of Knoevenagel adducts against Aedes aegypti: theoretical study and in vitro validation.","authors":"Paloma G Abrantes, Poliana G Abrantes, Renata R Magalhães, Gildilayne M Silva, Natália F Sousa, Marcus T Scotti, Renan T Leite, Jheison M C Francelino, Fabíola C Nunes, Juliana A Vale","doi":"10.1080/17568919.2025.2498877","DOIUrl":"10.1080/17568919.2025.2498877","url":null,"abstract":"Aim: This study investigated the larvicidal potential of Knoevenagel adducts against Aedes aegypti larvae to develop sustainable alternatives for controlling disease vectors like dengue.Methods: Larvicidal activity of Knoevenagel adducts (1a-l) was evaluated on fourth-stage Aedes aegypti larvae. Additional analyses included nitric oxide measurement, cell profiling, toxicity assessment, molecular docking, molecular dynamics simulation, and ADMET (Absorption, Distribution, Metabolism, and Toxicity) evaluation.Results: Compounds 1c and 1g showed high larvicidal efficacy, with LC50 values of 3.39 and 5.13 ppm. Hemolymph analysis revealed altered hemocyte composition, indicating an immune response, though nitric oxide levels remained unchanged. Molecular docking identified strong interactions between the Aedes aegypti FKBP12 enzyme (PDB: 3UQI) and Knoevenagel adducts. Compound 1g had the highest activity probability and binding affinity, while 1c showed strong interactions validated by biological assays. Molecular dynamics confirmed stable interactions of 1c and FKBP12, with both 1c and 1g displaying significant van der Waals contributions. ADMET analysis highlighted 1c as a less toxic compound, with minimal mutagenic risk, favorable pharmacokinetics, and high bioavailability.Conclusions: Knoevenagel adducts 1c and 1g are promising candidates for effective, selective, and environmentally friendly larvicides.","PeriodicalId":12475,"journal":{"name":"Future medicinal chemistry","volume":" ","pages":"999-1011"},"PeriodicalIF":3.2,"publicationDate":"2025-05-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12091929/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143983567","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

Unveiling the research directions for pyrrolidine-based small molecules as versatile antidiabetic and anticancer agents. 揭示了吡咯烷基小分子多功能抗糖尿病和抗癌药物的研究方向。

IF 3.2 4区医学

Future medicinal chemistry Pub Date : 2025-05-01 Epub Date: 2025-05-12 DOI: 10.1080/17568919.2025.2501923

Shiv Kumar, Rupali Kohal, Debarshi Mondal, Shreya Kumari, Preety Kumari, Priya Bisht, Ghanshyam Das Gupta, Sant Kumar Verma

{"title":"Unveiling the research directions for pyrrolidine-based small molecules as versatile antidiabetic and anticancer agents.","authors":"Shiv Kumar, Rupali Kohal, Debarshi Mondal, Shreya Kumari, Preety Kumari, Priya Bisht, Ghanshyam Das Gupta, Sant Kumar Verma","doi":"10.1080/17568919.2025.2501923","DOIUrl":"10.1080/17568919.2025.2501923","url":null,"abstract":"The pyrrolidine moiety, a five-membered saturated nitrogen-containing heterocycle, emerged as a crucial pharmacophore in medicinal chemistry due to its distinctive physicochemical properties, including hydrophilicity, basicity, and structural rigidity. Extensive modifications of pyrrolidine derivatives yielded novel compounds with pronounced antidiabetic and anticancer activities. The structural investigation of pyrrolidine-based molecules demonstrated that substitutions at the N1, 3rd, and 5th positions offer significant opportunities for optimizing biological activity and enhancing target-specific interactions. The synthesis of pyrrolidine-based molecules has been explored in literature; however, structural, target interaction analysis, and pharmacological aspects warranted for the development of targeted small molecule versatile antidiabetic and anticancer agents are lacking. The review addresses this gap by emphasizing the developments in pyrrolidine-based small molecules via structural and target interaction analysis, highlighting their antidiabetic and anticancer activities, and offering a comprehensive perspective on the development of targeted therapeutics. The investigated structural features and pharmacological developments underscore the dual functionality of pyrrolidine-based drugs in managing disorders, such as diabetes and cancer, that share common pathological mechanisms, such as inflammation, oxidative stress, and metabolic dysregulation. This overlap has catalyzed the development of multifunctional pyrrolidine derivatives capable of targeting pathways integral to both conditions, providing a promising avenue for therapeutic innovation.","PeriodicalId":12475,"journal":{"name":"Future medicinal chemistry","volume":" ","pages":"1039-1053"},"PeriodicalIF":3.2,"publicationDate":"2025-05-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12097281/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143987698","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

Recent advances in quinazolinone derivatives: structure, design and therapeutic potential. 喹唑啉酮衍生物的最新进展：结构、设计和治疗潜力。

IF 3.2 4区医学

Future medicinal chemistry Pub Date : 2025-05-01 Epub Date: 2025-05-11 DOI: 10.1080/17568919.2025.2504327

Feyzi Sinan Tokalı

引用次数: 0

The antibreast cancer therapeutic potential of quinazoline hybrids-Part I. 喹唑啉杂合物的抗乳腺癌治疗潜力——第一部分。

IF 3.2 4区医学

Future medicinal chemistry Pub Date : 2025-05-01 Epub Date: 2025-04-30 DOI: 10.1080/17568919.2025.2498881

Wei Chen, Ruo Wang, Yidan Lin, Xiaoqiang Wang, Feili Cai, Mengbo Lin, Jiawen Wang, Hui Zhang, Min Chen

{"title":"The antibreast cancer therapeutic potential of quinazoline hybrids-Part I.","authors":"Wei Chen, Ruo Wang, Yidan Lin, Xiaoqiang Wang, Feili Cai, Mengbo Lin, Jiawen Wang, Hui Zhang, Min Chen","doi":"10.1080/17568919.2025.2498881","DOIUrl":"10.1080/17568919.2025.2498881","url":null,"abstract":"Breast cancer is the most commonly diagnosed cancer in women and is the leading cause of cancer-related mortality among female patients across the world. Chemotherapy is a critical means for breast cancer therapy, and administration of chemotherapy could reduce the risk of recurrence by approximately one-third in early breast cancer. However, multidrug resistance represents a principal obstacle to effective chemotherapeutic interventions against breast cancer and is an increasing clinical challenge, creating an urgent demand to explore innovative chemotherapeutics to combat this formidable disease. Quinazoline hybrids with structural and mechanistic diversity exhibit excellent activity against breast cancers including drug-resistant forms and have the potential to reduce side effects caused by the corresponding pharmacophores. Notably, lapatinib, a quinazoline-furan-sulfone hybrid, has already been launched for breast cancer therapy. Thus, quinazoline hybrids represent a fertile source for the development of novel chemotherapeutics for clinical deployment in the control and eradication of breast cancer. This review emphasizes the current scenario of quinazoline hybrids with antibreast cancer therapeutic potential and focuses on structure-activity relationships (SARs) and modes of action, developed from 2020 onwards, to facilitate the rational discovery of more effective antibreast cancer candidates. [Figure: see text]This review emphasizes the current landscape of quinazoline hybrids with antibreast cancer therapeutic potential, delves into structure-activity relationships and mechanisms of action developed from 2020 onwards, aiming to facilitate the rational discovery of more effective and less toxic candidates.","PeriodicalId":12475,"journal":{"name":"Future medicinal chemistry","volume":" ","pages":"1055-1069"},"PeriodicalIF":3.2,"publicationDate":"2025-05-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12091908/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144011443","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