Benzothiazole a privileged scaffold for Cutting-Edges anticancer agents: Exploring drug design, structure-activity relationship, and docking studies,European Journal of Medicinal Chemistry

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Benzothiazole a privileged scaffold for Cutting-Edges anticancer agents: Exploring drug design, structure-activity relationship, and docking studies
European Journal of Medicinal Chemistry ( IF 6.0 ) Pub Date : 2024-09-05 , DOI: 10.1016/j.ejmech.2024.116831
Aayishamma I ₁ , Gurubasavaraja Swamy Purawarga Matada ₁ , Rohit Pal ₁ , Abhishek Ghara ₁ , Nimmagadda Venkata Satya Sai Aishwarya ₁ , Kumaraswamy B ₁ , Ketan R Hosamani ₁ , Manjushree B V ₁ , Haripriya E ₁

Affiliation

Cancer is a major societal, public health, and economic burden in the 21st century, with 9.7 million deaths in 2022 (9.96 million in 2020) and 20 million new cancer cases (19.6 million in 2020). Considering the increasing number of cancer cases and deaths, heterocyclic compounds always paved the gold mine for the development of potential anticancer drugs as these compounds have unique flexibility and dynamic cores. Benzothiazoles and their derivatives have potential anticancer properties, making them a desirable scaffold among different heterocycles. Title structures are a class of chemicals that may bind to various receptors with high affinity, particularly those engaged in oncogenic processes. The use of these compounds allows medicinal chemists to rapidly produce anticancer treatments across a large range of targets over an extended length of time. The current study presents a thorough success story of benzothiazole derivatives as anticancer agents. It discusses the current state of cancer, the profile of benzothiazole-based derivatives synthetic pathways, and its relevance as an anticancer agent on several oncogenic pathways. The structure-activity relationship was also added to offer insight into the connection of biological data with structure and the rational design of more active drugs.

中文翻译：

苯并噻唑是尖端抗癌药物的特权支架：探索药物设计、构效关系和对接研究

癌症是 21 世纪的主要社会、公共卫生和经济负担，2022 年有 970 万人死亡（2020 年为 996 万人），癌症新发病例 2000 万（2020 年为 1960 万人）。考虑到癌症病例和死亡人数的增加，杂环化合物总是为潜在抗癌药物的开发铺平了金矿，因为这些化合物具有独特的灵活性和动态核心。苯并噻唑及其衍生物具有潜在的抗癌特性，使其成为不同杂环之间理想的支架。标题结构是一类化学物质，可以高亲和力与各种受体结合，特别是那些参与致癌过程的受体。这些化合物的使用使药物化学家能够在较长的时间内快速生产针对各种靶点的抗癌治疗药物。目前的研究展示了苯并噻唑衍生物作为抗癌剂的全面成功故事。它讨论了癌症的现状、基于苯并噻唑的衍生物合成途径的概况，以及它作为抗癌剂在几种致癌途径上的相关性。还添加了构效关系，以深入了解生物数据与结构的联系以及更活性药物的合理设计。

更新日期：2024-09-05

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