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噻吩及其类似物的抗癌活性研究综述。

A Review on Anticancer Activities of Thiophene and Its Analogs.

机构信息

Institute of Pharmaceutical Research, GLA University, Mathura, Uttar Pradesh, 281406, India.

School of Medical and Allied Sciences, K.R. Mangalam University, Gurgaon, Haryana, 122103, India.

出版信息

Mini Rev Med Chem. 2020;20(19):1944-1965. doi: 10.2174/1389557520666200715104555.

Abstract

Cancer is the world's second-largest cause of mortality and one of the biggest global health concerns. The prevalence and mortality rates of cancer remain high despite significant progress in cancer therapy. The search for more effective, as well as less toxic treatment methods for cancer, is at the focus of current studies. Thiophene and its derivatives have surged as an influential scaffold, which, because of their appreciable diversity in biological activities, has drawn the concerned interest of the researchers in the field of medicinal chemistry. By the affluent introduction of its derivatives, which have antioxidant, anti-inflammatory, antimicrobial, and anticancer activities, the adaptability of the thiophene moiety has been displayed. The nature and positioning of the substitutions significantly impacted thiophene moiety activity. This decent array in the living response account about this moiety has picked plentiful researcher's consideration to inquire about it to its peculiar potential across certain activities. In the field of cancer therapy against different cancer cells, the structure-activity relationship for each of the derivatives showed an excellent understanding of thiophene moiety. Information from the various articles revealed the key role of thiophene moiety and its derivatives to develop the vital lead compound. The essential anticancer mechanisms identified include inhibition of the topoisomerase, inhibition of tyrosine kinase, tubulin interaction and apoptosis induction through the activation of reactive oxygen species. This review is an endeavor to promote the anticancer potential of the derivatives, whether having thiophene or condensed thiophene as a core moiety or as a substituent that can lead in the future to synthesize varieties of chemotherapeutic entities in the field of cancer treatment.

摘要

癌症是全球第二大死亡原因,也是全球最大的健康问题之一。尽管癌症治疗取得了重大进展,但癌症的发病率和死亡率仍然很高。寻找更有效、毒性更低的癌症治疗方法是当前研究的重点。噻吩及其衍生物作为一种有影响力的支架,由于其在生物活性方面的显著多样性,引起了药物化学家领域研究人员的关注。通过丰富的衍生物的引入,这些衍生物具有抗氧化、抗炎、抗菌和抗癌活性,展示了噻吩部分的适应性。取代基的性质和定位对噻吩部分的活性有显著影响。噻吩部分在生命反应中的这种多样性表明,它具有独特的潜力,引起了许多研究人员的关注,对其进行了广泛的研究。在针对不同癌细胞的癌症治疗领域,每种衍生物的结构-活性关系都对噻吩部分有很好的了解。来自不同文章的信息揭示了噻吩部分及其衍生物在开发重要先导化合物方面的关键作用。确定的主要抗癌机制包括抑制拓扑异构酶、抑制酪氨酸激酶、与微管相互作用以及通过激活活性氧诱导细胞凋亡。本文综述旨在促进噻吩及其衍生物的抗癌潜力,无论是作为核心部分还是作为取代基,都可以在未来的癌症治疗领域中合成各种化疗实体。

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