Polyfunctional Thiazole/Thiazolidinone Derivatives as a New Class of Heterocyclic Compounds with Novel Mechanisms of Anticancer Activity.

S Pasichnyk, A Lozynskyi, R Lesyk, V Matviiv, B Snizhko
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Abstract

Thiazole and thiazolidinone derivatives constitute an important class of heterocyclic compounds, widely investigated in modern medicinal chemistry for their diverse biological activities and significant potential for structural modification. Particular attention has focused on their anticancer properties and the design of multifunctional hybrid molecules with improved pharmacological profiles. This review summarizes recent advances in the synthesis and biological evaluation of functionally substituted condensed and non-condensed thiazole/thiazolidinone derivatives with anticancer activity. Available literature demonstrates that many of these compounds exhibit pronounced cytotoxic and pro-apoptotic effects across various tumor models. Their biological activity is associated with interactions with multiple molecular targets, including PPARγ receptors, integrins, PI3K/mtOR signaling pathways, histone deacetylases, matrix metalloproteina- ses, StAt3, and Pim-kinases. These multitarget mechanisms highlight the potential of these heterocyclic scaffolds for developing innovative anticancer agents. Analysis of structure-activity relationships has revealed promising directions for further optimization of the lead compounds. Overall, thiazole and thiazolidinone derivatives remain attractive plat- forms for the rational design of new anticancer drugs with improved selectivity and reduced toxicity.

多官能团噻唑/噻唑烷酮衍生物:一类具有抗癌活性新机制的杂环化合物。
噻唑和噻唑烷酮衍生物是一类重要的杂环化合物,因其多样的生物活性和巨大的结构修饰潜力而在现代药物化学中得到广泛研究。特别关注的是它们的抗癌特性和设计具有改进药理特征的多功能杂交分子。本文综述了具有抗癌活性的功能取代缩合和非缩合噻唑/噻唑烷酮衍生物的合成和生物学评价的最新进展。现有文献表明,许多这些化合物在各种肿瘤模型中表现出明显的细胞毒性和促凋亡作用。它们的生物活性与多个分子靶点的相互作用有关,包括PPARγ受体、整合素、PI3K/mtOR信号通路、组蛋白去乙酰化酶、基质金属蛋白、StAt3和pim激酶。这些多靶点机制突出了这些杂环支架在开发创新抗癌药物方面的潜力。结构-活性关系的分析为进一步优化先导化合物揭示了有希望的方向。总的来说,噻唑和噻唑烷酮衍生物仍然是合理设计具有提高选择性和降低毒性的新型抗癌药物的有吸引力的平台。
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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