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2-取代苯并噻唑骨架类化疗药物的研究进展。

Advances in 2-substituted benzothiazole scaffold-based chemotherapeutic agents.

机构信息

Department of Pharmaceutical Chemistry, School of Pharmaceutical Education and Research (SPER), Jamia Hamdard, New Delhi, India.

Department of Pharmacology, School of Pharmaceutical Education and Research (SPER), Jamia Hamdard, New Delhi, India.

出版信息

Arch Pharm (Weinheim). 2021 Dec;354(12):e2100246. doi: 10.1002/ardp.202100246. Epub 2021 Aug 31.

Abstract

Targeted therapy plays a pivotal role in cancer therapeutics by countering the drawbacks of conventional treatment like adverse events and drug resistance. Over the last decade, heterocyclic derivatives have received considerable attention as cytotoxic agents by modulating various signaling pathways. Benzothiazole is an important heterocyclic scaffold that has been explored for its therapeutic potential. Benzothiazole-based derivatives have emerged as potent inhibitors of enzymes such as EGFR, VEGFR, PI3K, topoisomerases, and thymidylate kinases. Several researchers have designed, synthesized, and evaluated benzothiazole scaffold-based enzyme inhibitors. Of these, several inhibitors have entered various phases of clinical trials. This review describes the recent advances and developments of benzothiazole architecture-based derivatives as potent anticancer agents.

摘要

靶向治疗通过克服传统治疗方法的缺点,如不良反应和耐药性,在癌症治疗中发挥着关键作用。在过去的十年中,杂环衍生物作为细胞毒性剂受到了相当多的关注,通过调节各种信号通路。苯并噻唑是一种重要的杂环支架,因其治疗潜力而受到探索。苯并噻唑衍生物已成为 EGFR、VEGFR、PI3K、拓扑异构酶和胸苷酸激酶等酶的有效抑制剂。一些研究人员设计、合成和评估了基于苯并噻唑支架的酶抑制剂。其中一些抑制剂已经进入了不同的临床试验阶段。本综述描述了基于苯并噻唑结构的衍生物作为有效的抗癌剂的最新进展和发展。

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