Isatin–azole hybrids and their anticancer activities,Archiv der Pharmazie

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Isatin–azole hybrids and their anticancer activities
Archiv der Pharmazie ( IF 4.3 ) Pub Date : 2019-11-06 , DOI: 10.1002/ardp.201900272
Yani Hou ₁ , Congshan Shang ₁ , Hui Wang ₁ , Jie Yun ₁

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Isatin and azole moieties, which have the ability to form various noncovalent interactions with different therapeutic targets, are common pharmacophores in drug development. Isatin and azole derivatives possess promising in vitro and in vivo anticancer activity, and many of them, such as semaxanib, sunitinib, and carboxyamidotriazole, could be used to treat various cancers. Thus, it is conceivable that hybridization of the isatin moiety with azole may provide a valuable therapeutic intervention for the treatment of cancer. Substantial efforts have been made to develop isatin–azole hybrids as novel anticancer agents, and some of the isatin–azole hybrids exhibited considerable activity. This review emphasizes isatin–azole hybrids with potential anticancer activity, covering articles published between 2010 and 2019. The structure–activity relationships as well as the mechanisms of action are also discussed to provide insights for the rational design of more effective candidates.

中文翻译：

靛红-唑类杂化物及其抗癌活性

靛红和唑部分能够与不同的治疗靶点形成各种非共价相互作用，是药物开发中常见的药效团。靛红和唑类衍生物具有良好的体外和体内抗癌活性，其中许多如 semaxanib、舒尼替尼和羧胺三唑可用于治疗各种癌症。因此，可以想象，靛红部分与唑的杂交可以为治疗癌症提供有价值的治疗干预。已经做出了大量努力来开发作为新型抗癌剂的靛红 - 唑杂化物，并且一些靛红 - 唑杂化物表现出相当大的活性。这篇综述强调了具有潜在抗癌活性的靛红-唑类杂化物，涵盖了 2010 年至 2019 年间发表的文章。

更新日期：2019-11-06

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