Gersy Marie Joelle Oba, Rakesh Sahu, Kamal Shah, Deepika Paliwal, Ashok Kumar Sah, Aman Thakur
{"title":"Current Developments in the Pharmacological Activities and Synthesis of Carbazole Derivatives.","authors":"Gersy Marie Joelle Oba, Rakesh Sahu, Kamal Shah, Deepika Paliwal, Ashok Kumar Sah, Aman Thakur","doi":"10.2174/0113895575407122250822095143","DOIUrl":"https://doi.org/10.2174/0113895575407122250822095143","url":null,"abstract":"<p><p>The growing prevalence of multidrug resistance and its detrimental effects pose a significant threat to public health, which is one reason for the current interest in the introduction of novel agents. To combat this adverse effect and drug resistance, numerous drugs have been developed over time, and their safety is still being evaluated; derivatives or medications based on the carbazole moiety are one of the key contributors. Therefore, this review explores carbazole-based derivatives as possible drugs to treat Alzheimer's, diabetes, inflammation, cancer, and many more, along with their synthetic schemes, SARs, and activity. Some of the carbazole-based drugs available in the market and under clinical trials are also tabulated. By integrating this insight, describe how these compounds are being reinvented as targeted therapeutic agents. This comprehensive analysis is designed to guide researchers in developing next-generation drugs to address various challenges and leverage the unique pharmacological properties of carbazole-derived drugs.</p>","PeriodicalId":18548,"journal":{"name":"Mini reviews in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":3.3,"publicationDate":"2025-09-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145000978","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}
K P Arunraj, K M Haritha, M T Khulood, P Ayisha Sana, K P Khadeeja Thanha, K Pramod
{"title":"The Use of Artificial Intelligence in the Formulation of Effervescent Tablets: A Review.","authors":"K P Arunraj, K M Haritha, M T Khulood, P Ayisha Sana, K P Khadeeja Thanha, K Pramod","doi":"10.2174/0113895575402013250821121137","DOIUrl":"https://doi.org/10.2174/0113895575402013250821121137","url":null,"abstract":"<p><p>Artificial Intelligence (AI) is emerging as a valuable tool in pharmaceutical formulations, including the development of effervescent tablets (ETs). This review highlights how AI techniques are being explored to support ET formulation designs, optimize component ratios, predict disintegration and dissolution behavior, and control reactions through artificial neural networks, support vector machines, and machine learning. These techniques have been applied in recent studies to enhance stability, improve disintegration times, and flavor masking. Computational fluid dynamics simulations of effervescence and dissolution are underexplored for ETs. Data-driven approaches, like response surface modeling, require ingredient concentrations, tablet properties, consumer preferences, and predictive analytics for optimization. However, limited comprehensive datasets, complex reactions, environmental sensitivities, and ethical/regulatory considerations pose challenges. Overcoming these obstacles, as identified in the current literature, could enable AI to innovate ET development and personalization.</p>","PeriodicalId":18548,"journal":{"name":"Mini reviews in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":3.3,"publicationDate":"2025-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145000959","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}
Aishal Shahrukh, Salma Batool, Muhammad Sarfraz, Mohammed B Hawsawi, M Iqbal Choudhary, Rahman Shah Zaib Saleem
{"title":"Natural Products, Synthesis, and Biological Activities of Quinolines (2020-2024).","authors":"Aishal Shahrukh, Salma Batool, Muhammad Sarfraz, Mohammed B Hawsawi, M Iqbal Choudhary, Rahman Shah Zaib Saleem","doi":"10.2174/0113895575408714250822092020","DOIUrl":"https://doi.org/10.2174/0113895575408714250822092020","url":null,"abstract":"<p><p>Quinoline is a biologically important bicyclic scaffold found in many natural products and medicinally relevant molecules. Quinoline-containing compounds continue to feature prominently in recent literature on hit identification and hit-to-lead campaigns targeting various biological pathways, underscoring the need for a review of the latest progress. This review presents recently reported quinoline-containing natural products, various synthetic methods for producing quinoline derivatives, and an overview of their diverse biological activities. The biological properties covered include anticancer, anti-inflammatory, antioxidant, anti-tubercular, α-glucosidase inhibitory, antimicrobial, anti-Alzheimer's, and antimalarial effects. Finally, a selection of representative quinolinebased chemical probes is presented to assist researchers in strategically designing novel quinoline derivatives for diverse biological applications.</p>","PeriodicalId":18548,"journal":{"name":"Mini reviews in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":3.3,"publicationDate":"2025-08-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145000925","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}
Zihan Chen, Ka Fai Leong, Yuhan Xie, Alessandra Gianoncelli, Giovanni Ribaudo, Paolo Coghi
{"title":"Triterpenoid Compounds and Their Derivatives: Emerging Pharmacological Agents for Arthritis Treatment.","authors":"Zihan Chen, Ka Fai Leong, Yuhan Xie, Alessandra Gianoncelli, Giovanni Ribaudo, Paolo Coghi","doi":"10.2174/0113895575389522250825063702","DOIUrl":"https://doi.org/10.2174/0113895575389522250825063702","url":null,"abstract":"<p><p>Arthritis has become a global public health issue due to its diverse risk factors and high prevalence. Therefore, there is a demand for more effective drugs to improve these situations. Triterpenoids have attracted the interest of researchers because of their broad spectrum of biological activities and pharmacological effects. The aim of this review is to provide an updated overview of the potential of triterpenoids and of their derivatives as therapeutic agents against Rheumatoid Arthritis (RA) and Osteoarthritis (OA), based on their anti-inflammatory and immunomodulatory properties. This review discusses the chemical and pharmacological properties of triterpenoids and their derivatives, focusing on the different mechanisms by which this class of compounds achieves therapeutic benefits in arthritis. The conclusions indicate that triterpenoids and their derivatives have a favorable potential therapeutic effect on arthritis.</p>","PeriodicalId":18548,"journal":{"name":"Mini reviews in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":3.3,"publicationDate":"2025-08-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145000938","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}
{"title":"Coumarin-based Strategies for Breast Cancer: A Multifaceted Perspective.","authors":"Yash Sharma, Sourav Kalra, Ankit Vashisht, Rajiv Sharma","doi":"10.2174/0113895575394059250813074806","DOIUrl":"https://doi.org/10.2174/0113895575394059250813074806","url":null,"abstract":"<p><p>Breast cancer remains the most prevalent cancer among women worldwide, with increasing toxicity and resistance to current therapies posing a serious challenge to healthcare systems. The urgent demand for more effective and safer treatments has highlighted coumarin, a naturally occurring compound with a unique ring structure, due to its promising potential in combating breast cancer. Over the past three decades, numerous synthetic coumarin derivatives have been developed to enhance therapeutic efficacy. This review provides a comprehensive analysis of 18 reported coumarin- based compounds, focusing on their design strategies, mechanisms of action, and structureactivity relationships (SAR). Molecular docking studies targeting key enzymes, including tyrosine kinases, topoisomerases, and serine/threonine kinases, were examined to evaluate binding affinities and interaction patterns. Substitutions at the 3- and 6-positions of the coumarin scaffold were found to impact target binding significantly. Critical interactions, including hydrogen bonding, van der Waals forces, and hydrophobic contacts, were correlated with experimental anticancer activities, offering valuable insights into ligand-protein complex stabilization. Overall, the analysis underscores the potential of coumarin derivatives as promising leads for the rational design of novel anticancer agents with improved efficacy and selectivity.</p>","PeriodicalId":18548,"journal":{"name":"Mini reviews in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":3.3,"publicationDate":"2025-08-27","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145000964","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}
{"title":"Bruton's Tyrosine Kinase Inhibitors: A Versatile Therapeutic Approach for Cancer, Autoimmune Disorders, GVHD, and COVID-19.","authors":"Swati Paliwal, Uma Agarwal, Rajiv Kumar Tonk","doi":"10.2174/0113895575409452250815095743","DOIUrl":"https://doi.org/10.2174/0113895575409452250815095743","url":null,"abstract":"<p><p>Recent trends have shown the development of various medicinally important compounds that specifically target B-cell receptor (BCR) pathways at various segments that have a major role in Bruton's tyrosine kinase (BTK) receptor, which belongs to the family of kinases. These kinases are usually situated close to the cell membrane due to which they participate in upstream processing of BCR signalling. Various molecules have been potentialized to target these signalling pathways of these kinase receptors in order to achieve a pharmacological effect. Given the central role of BTK in immunity, BTK inhibition represents a promising therapeutic approach for the treatment of multiple diseases. BTK inhibitors work by regulating B-cell receptor signalling along with inflammatory pathways and immune cell interactions, offering more advanced treatment options compared to traditional therapies. In addition to BTK inhibitors, an extensive knowledge of the pharmacological mechanisms underlying the blockage of these receptors is necessary in order to more accurately forecast when and where a patient could need combination therapy or just one medication. Efforts have been made to facilitate translational discoveries, drug re-purposing concepts, and further development of precision medicine products. This thorough literature study has focused on studies published until June 2025.</p>","PeriodicalId":18548,"journal":{"name":"Mini reviews in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":3.3,"publicationDate":"2025-08-27","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145000983","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}
{"title":"Synthesis of Phenothiazine Derivatives and their Diverse Biological Activities: A Review.","authors":"Prabhjot Kaur, Divya Utreja, Shivali Sharma","doi":"10.2174/0113895575405792250813070957","DOIUrl":"https://doi.org/10.2174/0113895575405792250813070957","url":null,"abstract":"<p><p>The increasing resistance of causative agents to current treatments has made infectious disease management more challenging. Heterocyclic compounds have garnered considerable attention due to their numerous significant medical and biological applications. Research interest in heterocyclic compounds is rapidly increasing due to extensive synthetic studies and their functional utility. Phenothiazine (PTZ), an organic thiazine compound, has a broad range of biological activities, including antimicrobial, antimalarial, antipsychotic, anti-inflammatory, and antiemetic effects. Additionally, modifications to the phenothiazine structure have enhanced its efficacy, making it a potential candidate for addressing drug-resistant infections. This review examines recent synthesis methods, including catalytic and microwave-assisted techniques, which have expanded the applications of phenothiazine derivatives. The article also discusses structure-activity relationships, which help optimize the pharmacological properties of these compounds for future therapeutic use.</p>","PeriodicalId":18548,"journal":{"name":"Mini reviews in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":3.3,"publicationDate":"2025-08-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144960749","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}
{"title":"Role of Calmodulin in Neurodegeneration and Neuroprotection.","authors":"Natalya Kurochkina, Parvathi Rudrabhatla","doi":"10.2174/0113895575403663250812115441","DOIUrl":"https://doi.org/10.2174/0113895575403663250812115441","url":null,"abstract":"<p><p>Intracellular calcium (Ca2+) levels are critical in maintaining cellular activities and are tightly regulated. Neuronal degeneration and regeneration rely on calcium-binding proteins. Calmodulin (CaM) is a calcium sensor and the primary regulator of receptors and ion channels that maintain calcium homeostasis. The calmodulin binding domains are present in proteins that serve as risk factors and biomarkers associated with Alzheimer's disease, Parkinson's disease, Huntington's disease, Amyotrophic Lateral Sclerosis, and other neurodegenerative diseases, suggesting calmodulin ligands as emerging therapeutic targets for treatment. Inhibiting CaM to develop new therapies has drawbacks, as CaM is a ubiquitous molecule involved in many regulatory pathways. Recently, new strategies for disrupting CaM interactions with its targets have shown promising approaches to treatment. The structures of human CaM, its binding proteins, and inhibitors are well studied, with particular emphasis on the conservation of CaM amino acid sequences and the ability to bind protein fragments of high sequence variability, which exhibit common characteristics of amphipathic helices carrying basic amino acids. In this review, we discuss structural characteristics of CaM and its ligands in the context of transcriptional regulation. Specific binding of CaM to (1) basic region/helix-loop-helix/leucine zipper and (2) helix-turn-helix high mobility group box containing Sox families of transcription factors highlights common features of CaM binding sequences, which suggest their regulatory functions. We describe key proteins involved in neurodegeneration and transcription factors subject to calmodulin regulation that are candidates for the development of new approaches to treating neuronal diseases.</p>","PeriodicalId":18548,"journal":{"name":"Mini reviews in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":3.3,"publicationDate":"2025-08-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144960743","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}
{"title":"Luteolin for the Treatment of Organ Fibrosis: A Mini Review.","authors":"Nailong Wang, Wei Lan","doi":"10.2174/0113895575408729250811073556","DOIUrl":"https://doi.org/10.2174/0113895575408729250811073556","url":null,"abstract":"<p><p>Luteolin is a naturally occurring flavonoid that exhibits significant potential in mitigating organ fibrosis. This review consolidates evidence from studies demonstrating the antifibrotic effects of luteolin in hepatic, renal, cardiac, pulmonary, dermal, subretinal, and pancreatic fibrosis. Mechanistically, luteolin targets key pathways that drive fibrosis, including the TGF-β/Smad, STAT3, NF- κB, and AMPK signaling pathways, while suppressing oxidative stress, inflammation, and fibroblast activation. In hepatic fibrosis, luteolin inhibits hepatic stellate cell activation, reduces collagen synthesis, and counteracts ferroptosis by modulating the SLC7A11 and GPX4 pathways. Renal fibrosis is alleviated through the regulation of the SIRT1/FOXO3 and AMPK/NLRP3/TGF-β pathways, thereby attenuating ECM accumulation and inflammation. Cardiac benefits arise from luteolin's modulation of NO-cGMP, AKT/GSK-3, and Nrf2/NF-κB axes, improving myocardial function. Pulmonary fibrosis models highlight the ability of luteolin to inhibit TGF-β1-induced Smad3 phosphorylation and inflammatory cytokine release. Additionally, luteolin demonstrates efficacy in skin and subretinal fibrosis by targeting TGF-β/Smad and YAP/TAZ pathways. Toxicology and pharmacokinetic studies indicate favorable safety profiles. Despite promising preclinical outcomes, clinical data remain scarce. The multi-target engagement, low toxicity, and broad bioactivity of luteolin position it as a compelling candidate for antifibrotic therapy. Further clinical research is warranted to translate these findings into therapeutic applications for fibrotic disorders.</p>","PeriodicalId":18548,"journal":{"name":"Mini reviews in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":3.3,"publicationDate":"2025-08-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144960709","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}
Soha H Emam, Eman M Ahmed, Nadia A Khalil, Basma A Mohammad, Nirvana A Gohar
{"title":"Pyridazine and Pyridazinone in Medicinal Chemistry: Synthesis and Antiinflammatory Pathways Targeting TxA2, TNF-α, and IL-6.","authors":"Soha H Emam, Eman M Ahmed, Nadia A Khalil, Basma A Mohammad, Nirvana A Gohar","doi":"10.2174/0113895575404189250811070603","DOIUrl":"https://doi.org/10.2174/0113895575404189250811070603","url":null,"abstract":"<p><p>Inflammation is a fundamental biological reaction to harmful stimuli, which is crucial in the initiation and advancement of different diseases, including rheumatoid arthritis, cardiovascular conditions, neurological disorders such as Alzheimer's and Parkinson's, and multiple cancer types. Chronic inflammation, in particular, contributes to irreversible tissue damage and the progression of disease. Thus, the suppression of key inflammatory mediators has become a promising therapeutic approach. Thromboxane A2 (TxA2), tumor necrosis factor-alpha (TNF-α), and interleukin-6 (IL-6) are among the mediators that have been thoroughly investigated for their roles in regulating immune responses and sustaining inflammation; therefore, targeting these mediators offers substantial therapeutic potential. In recent years, significant attention has been focused on heterocyclic compounds, especially pyridazine and pyridazinone derivatives, owing to their structural diversity and extensive biological activity. These scaffolds have shown significant effectiveness in regulating inflammatory pathways by limiting TxA2 production, reducing TNF-α release, and disrupting IL-6 signaling. This review presents a comprehensive overview of pyridazine and pyridazinone-based compounds as potential anti-inflammatory agents. It highlights both traditional and current synthetic strategies used in their development and explores their mechanisms of action with respect to key inflammatory targets. Additionally, the study examines recent pharmacological assessments and preclinical results, offering insights into the medicinal uses of these substances. A brief perspective on future research directions is also included, emphasizing the need for further structural optimization, in vivo validation, and clinical translation. Collectively, these results highlight the potential of pyridazine and pyridazinone derivatives in the development of advanced anti-inflammatory pharmaceuticals.</p>","PeriodicalId":18548,"journal":{"name":"Mini reviews in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":3.3,"publicationDate":"2025-08-13","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144855765","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}