Design, synthesis and biological evaluation of new ganglioside GM3 analogues as potential agents for cancer therapy.,European Journal of Medicinal Chemistry

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Design, synthesis and biological evaluation of new ganglioside GM3 analogues as potential agents for cancer therapy.
European Journal of Medicinal Chemistry ( IF 6.0 ) Pub Date : 2020-01-13 , DOI: 10.1016/j.ejmech.2020.112065
Changping Zheng ₁ , Ruyi Huang ₂ , Teodora Bavaro ₃ , Marco Terreni ₃ , Matthieu Sollogoub ₁ , Jianhua Xu ₂ , Yongmin Zhang ₄

Affiliation

Ganglioside GM3 is well known as a tumor-associated carbohydrate antigen on several types of tumors. Many studies have demonstrated that GM3 plays roles in cells proliferation, adhesion, motility and differentiation, which is involved in the process of cancer development. In the present study, we developed methods to synthesize GM3 analogues conveniently. By enzymatic hydrolysis and chemical procedures, two novel analogues and two known analogues were synthesized, containing lactose and glucosamine. Then anti-proliferation and anti-migration activities were evaluated by cytotoxicity assays and wound healing tests, and the data demonstrated that these analogues exhibited anticancer activities. Based on our previous studies, the structure-activity relationships were discussed. This study could provide valuable sight to find new antitumor agents for cancer therapy.

中文翻译：

新神经节苷脂GM3类似物作为癌症治疗的潜在药物的设计，合成和生物学评估。

神经节苷脂GM3是几种类型肿瘤上与肿瘤相关的碳水化合物抗原，众所周知。许多研究表明，GM3在细胞增殖，粘附，运动性和分化中起作用，这参与了癌症的发展过程。在本研究中，我们开发了方便地合成GM3类似物的方法。通过酶促水解和化学方法，合成了两种新的类似物和两种已知的类似物，它们含有乳糖和葡糖胺。然后通过细胞毒性测定和伤口愈合测试评估抗增殖和抗迁移活性，并且数据证明这些类似物表现出抗癌活性。在我们以前的研究的基础上，讨论了构效关系。

更新日期：2020-01-14

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