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1,3,4-恶二唑:一种作为抗癌剂靶向生长因子、酶和激酶的新兴骨架。

1,3,4-Oxadiazoles: An emerging scaffold to target growth factors, enzymes and kinases as anticancer agents.

作者信息

Bajaj Shalini, Asati Vivek, Singh Jagadish, Roy Partha Pratim

机构信息

Institute of Pharmaceutical Sciences, Guru Ghasidas Vishwavidyalaya (A Central University), Bilaspur, 495009, Chhattisgarh, India.

Institute of Pharmaceutical Sciences, Guru Ghasidas Vishwavidyalaya (A Central University), Bilaspur, 495009, Chhattisgarh, India.

出版信息

Eur J Med Chem. 2015 Jun 5;97:124-41. doi: 10.1016/j.ejmech.2015.04.051. Epub 2015 Apr 27.

Abstract

Five member heterocyclic 1,3,4-oxadiazole nucleus find unique place in medicinal chemistry and plays significant role in producing anticancer activity. The small and simple 1,3,4-oxadiazole nucleus is present in various compounds involved in research aimed at evaluating new products that posses interesting pharmacological properties such as antitumour activity. Mono and 2,5-di-substituted-1,3,4-oxadiazole derivatives have attracted considerable attention owing to their effective biological activity and extensive use. The important mechanism involved during its tumour suppression is related with the inhibition of different growth factors, enzymes and kinases including telomerase enzyme, histone deacetylase (HDAC), methionine aminopeptidase (MetAP), thymidylate synthase (TS), glycogen synthase kinase-3 (GSK), epidermal growth factor (EGF), vascular endothelial growth factor (VEGF) and focal adhesion kinase (FAK). The focused criteria of this review is to highlights the targeted inhibitory activity of 1,3,4-oxadiazole derivatives and their structure activity relationship to generate potential anticancer agents.

摘要

五元杂环1,3,4-恶二唑核在药物化学中占据独特地位,并在产生抗癌活性方面发挥着重要作用。小而简单的1,3,4-恶二唑核存在于各种参与研究的化合物中,这些研究旨在评估具有有趣药理特性(如抗肿瘤活性)的新产品。单取代和2,5-二取代的1,3,4-恶二唑衍生物因其有效的生物活性和广泛应用而备受关注。其肿瘤抑制过程中涉及的重要机制与抑制不同的生长因子、酶和激酶有关,包括端粒酶、组蛋白脱乙酰酶(HDAC)、甲硫氨酸氨基肽酶(MetAP)、胸苷酸合成酶(TS)、糖原合酶激酶-3(GSK)、表皮生长因子(EGF)、血管内皮生长因子(VEGF)和粘着斑激酶(FAK)。本综述的重点标准是突出1,3,4-恶二唑衍生物的靶向抑制活性及其构效关系,以生成潜在的抗癌药物。

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