Flaviana Alves Dos Santos, Joelson Germano Crispim, Eduardo Davi Lima da Silva, Arsênio Rodrigues Oliveira, Aldilane Gonçalves da Fonseca, Telma Maria Araújo Moura Lemos, Ana Cristina Lima Leite, Michelle Melgarejo da Rosa, Maira Galdino da Rocha Pitta, Michelly Cristiny Pereira, Ivan Rocha Pitta, Moacyr Jesus Barreto de Melo Rêgo
{"title":"Multimodal Activity of a Novel Compound against Prostate and Pancreatic Cancer.","authors":"Flaviana Alves Dos Santos, Joelson Germano Crispim, Eduardo Davi Lima da Silva, Arsênio Rodrigues Oliveira, Aldilane Gonçalves da Fonseca, Telma Maria Araújo Moura Lemos, Ana Cristina Lima Leite, Michelle Melgarejo da Rosa, Maira Galdino da Rocha Pitta, Michelly Cristiny Pereira, Ivan Rocha Pitta, Moacyr Jesus Barreto de Melo Rêgo","doi":"10.2174/0115680266351687250309020134","DOIUrl":null,"url":null,"abstract":"<p><strong>Background: </strong>Prostate and pancreatic cancers pose significant global health challenges. This study explored the potential of compound 5b, a novel phthalimido-1,3-thiazole derivative, as an anticancer agent against these malignancies.</p><p><strong>Methods: </strong>In vitro, compound 5b exhibited potent cytotoxic activity against both prostate (DU-145 and PC-3) and pancreatic (Panc-1 and Mia Paca-2) cancer cell lines. Notably, it significantly reduced colony formation in PC-3 cells, potentially hindering tumor growth. Furthermore, treatment with compound 5b suppressed cell migration and induced cell cycle arrest in the PC-3 line. Additionally, it triggered cell death through late apoptosis and necrosis at higher concentrations. Safety evaluations in mice revealed no mortality or adverse effects after a 30-day treatment with compound 5b. Key blood parameters (hematology) and biochemical markers of liver and kidney function remained unaltered.</p><p><strong>Results: </strong>Compound 5b significantly reduced colony formation, suppressed cell migration, and induced cell cycle arrest and apoptosis/necrosis in prostate cancer cells. In vivo, safety evaluations showed no adverse effects in treated mice, with blood and biochemical markers remaining normal.</p><p><strong>Conclusion: </strong>These findings suggest that compound 5b holds promise for further development as a therapeutic option for prostate and pancreatic cancers. Its multimodal activity profile, targeting cell viability, migration, cell cycle progression, and cell death, warrants further investigation.</p>","PeriodicalId":11076,"journal":{"name":"Current topics in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":2.9000,"publicationDate":"2025-03-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"Current topics in medicinal chemistry","FirstCategoryId":"3","ListUrlMain":"https://doi.org/10.2174/0115680266351687250309020134","RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q3","JCRName":"CHEMISTRY, MEDICINAL","Score":null,"Total":0}
引用次数: 0
Abstract
Background: Prostate and pancreatic cancers pose significant global health challenges. This study explored the potential of compound 5b, a novel phthalimido-1,3-thiazole derivative, as an anticancer agent against these malignancies.
Methods: In vitro, compound 5b exhibited potent cytotoxic activity against both prostate (DU-145 and PC-3) and pancreatic (Panc-1 and Mia Paca-2) cancer cell lines. Notably, it significantly reduced colony formation in PC-3 cells, potentially hindering tumor growth. Furthermore, treatment with compound 5b suppressed cell migration and induced cell cycle arrest in the PC-3 line. Additionally, it triggered cell death through late apoptosis and necrosis at higher concentrations. Safety evaluations in mice revealed no mortality or adverse effects after a 30-day treatment with compound 5b. Key blood parameters (hematology) and biochemical markers of liver and kidney function remained unaltered.
Results: Compound 5b significantly reduced colony formation, suppressed cell migration, and induced cell cycle arrest and apoptosis/necrosis in prostate cancer cells. In vivo, safety evaluations showed no adverse effects in treated mice, with blood and biochemical markers remaining normal.
Conclusion: These findings suggest that compound 5b holds promise for further development as a therapeutic option for prostate and pancreatic cancers. Its multimodal activity profile, targeting cell viability, migration, cell cycle progression, and cell death, warrants further investigation.
期刊介绍:
Current Topics in Medicinal Chemistry is a forum for the review of areas of keen and topical interest to medicinal chemists and others in the allied disciplines. Each issue is solely devoted to a specific topic, containing six to nine reviews, which provide the reader a comprehensive survey of that area. A Guest Editor who is an expert in the topic under review, will assemble each issue. The scope of Current Topics in Medicinal Chemistry will cover all areas of medicinal chemistry, including current developments in rational drug design, synthetic chemistry, bioorganic chemistry, high-throughput screening, combinatorial chemistry, compound diversity measurements, drug absorption, drug distribution, metabolism, new and emerging drug targets, natural products, pharmacogenomics, and structure-activity relationships. Medicinal chemistry is a rapidly maturing discipline. The study of how structure and function are related is absolutely essential to understanding the molecular basis of life. Current Topics in Medicinal Chemistry aims to contribute to the growth of scientific knowledge and insight, and facilitate the discovery and development of new therapeutic agents to treat debilitating human disorders. The journal is essential for every medicinal chemist who wishes to be kept informed and up-to-date with the latest and most important advances.