Eliza de Lucas Chazin, Ligia Souza da Silveira Pinto, Victor Facchinetti, Paula de Aquino Soeiro Portilho, Breno de Souza Bernardes, Claudia Regina Brandão Gomes, Emerson Lucena da Silva, Luina Benevides Lima, Felipe Pantoja Mesquita, Pedro Filho Noronha de Souza, Raquel Carvalho Montenegro, Marcus Vinicius Nora De Souza, Thatyana Rocha Alves Vasconcelos
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In this context, developing new, potent, and more specific treatments against this disease is urgent.</p><p><strong>Methods: </strong>A total of 15 benzoxathiolone-thiazolidinones hybrids were synthesized in a 5-step route and tested for their cytotoxicity against five human cancer cell lines: AGP-01 (gastric), SKMEL- 103 (melanoma), HCT-116 (colon), CAL27 (tongue), and K562 (leukemia), as well as a nontumoral cell line MRC-5.</p><p><strong>Results: </strong>Compounds 3-(6-hydroxy-2-oxobenzo[d][1,3]oxathiol-5-yl)-2-(4-nitrophenyl)thiazolidin- 4-one and 2-(2,4-dichlorophenyl)-3-(6-hydroxy-2-oxobenzo[d][1,3]oxathiol-5-yl)thiazolidin-4-one exhibited good activity against the K562 leukemia cell line, with IC50 values of 4.0 μM and 5.3 μM, respectively. Docking studies demonstrated that these compounds likely bind to the BCRABL1 kinase, a key protein in the pathogenesis of chronic myeloid leukemia (CML).</p><p><strong>Conclusion: </strong>The study suggests these benzoxathiolone-thiazolidinone hybrids could be promising lead compounds for developing new anticancer agents targeting leukemia.</p>","PeriodicalId":11076,"journal":{"name":"Current topics in medicinal chemistry","volume":" ","pages":""},"PeriodicalIF":2.9000,"publicationDate":"2025-06-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Benzoxathiolone-Thiazolidinone Hybrids: A New Class in the Search for Anticancer Agents.\",\"authors\":\"Eliza de Lucas Chazin, Ligia Souza da Silveira Pinto, Victor Facchinetti, Paula de Aquino Soeiro Portilho, Breno de Souza Bernardes, Claudia Regina Brandão Gomes, Emerson Lucena da Silva, Luina Benevides Lima, Felipe Pantoja Mesquita, Pedro Filho Noronha de Souza, Raquel Carvalho Montenegro, Marcus Vinicius Nora De Souza, Thatyana Rocha Alves Vasconcelos\",\"doi\":\"10.2174/0115680266366285250528005320\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p><strong>Background: </strong>Cancer continues to be a significant public health issue and one of the leading causes of death globally. 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Benzoxathiolone-Thiazolidinone Hybrids: A New Class in the Search for Anticancer Agents.
Background: Cancer continues to be a significant public health issue and one of the leading causes of death globally. In this context, developing new, potent, and more specific treatments against this disease is urgent.
Methods: A total of 15 benzoxathiolone-thiazolidinones hybrids were synthesized in a 5-step route and tested for their cytotoxicity against five human cancer cell lines: AGP-01 (gastric), SKMEL- 103 (melanoma), HCT-116 (colon), CAL27 (tongue), and K562 (leukemia), as well as a nontumoral cell line MRC-5.
Results: Compounds 3-(6-hydroxy-2-oxobenzo[d][1,3]oxathiol-5-yl)-2-(4-nitrophenyl)thiazolidin- 4-one and 2-(2,4-dichlorophenyl)-3-(6-hydroxy-2-oxobenzo[d][1,3]oxathiol-5-yl)thiazolidin-4-one exhibited good activity against the K562 leukemia cell line, with IC50 values of 4.0 μM and 5.3 μM, respectively. Docking studies demonstrated that these compounds likely bind to the BCRABL1 kinase, a key protein in the pathogenesis of chronic myeloid leukemia (CML).
Conclusion: The study suggests these benzoxathiolone-thiazolidinone hybrids could be promising lead compounds for developing new anticancer agents targeting leukemia.
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.
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