Benzoxathiolone-Thiazolidinone Hybrids: A New Class in the Search for Anticancer Agents.

IF 2.9 4区医学 Q3 CHEMISTRY, MEDICINAL

Current topics in medicinal chemistry Pub Date : 2025-06-16 DOI:10.2174/0115680266366285250528005320

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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引用次数: 0

Abstract

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.

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苯并恶硫龙-噻唑烷酮杂合体：一类新的抗癌药物。

背景：癌症仍然是一个重大的公共卫生问题，也是全球死亡的主要原因之一。在这种情况下，开发新的、有效的、更具体的治疗方法是迫切需要的。方法：采用5步法合成15个苯并恶硫龙-噻唑烷酮杂合体，并检测其对5种人肿瘤细胞系AGP-01（胃癌）、SKMEL- 103（黑色素瘤）、HCT-116（结肠癌）、CAL27（舌癌）、K562（白血病）以及非肿瘤细胞系MRC-5的细胞毒性。结果：化合物3-（6-羟基-2-氧苯并[d][1,3]氧噻吩-5-基）-2-（4-硝基）噻唑烷-4- 1和2-（2,4-二氯苯基）-3-（6-羟基-2-氧噻吩并[d][1,3]氧噻吩-5-基）噻唑烷-4- 1对K562白血病细胞株具有良好的抑制活性，IC50值分别为4.0 μM和5.3 μM。对接研究表明，这些化合物可能与BCRABL1激酶结合，BCRABL1激酶是慢性髓性白血病（CML）发病机制中的关键蛋白。结论：本研究提示这些苯并恶硫龙-噻唑烷酮复合物可能是开发新的白血病抗癌药物的先导化合物。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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来源期刊

Current topics in medicinal chemistry 医学-医药化学

CiteScore

6.40

自引率

2.90%

发文量

186

审稿时长

3-8 weeks

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.