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Anticancer Polymers via the Biginelli Reaction
ACS Macro Letters ( IF 5.1 ) Pub Date : 2020-08-18 , DOI: 10.1021/acsmacrolett.0c00496 Yongsan Li 1 , Tianhao Tan 2 , Yuan Zhao 1 , Yen Wei 1 , Dong Wang 2 , Rongjun Chen 3 , Lei Tao 1
ACS Macro Letters ( IF 5.1 ) Pub Date : 2020-08-18 , DOI: 10.1021/acsmacrolett.0c00496 Yongsan Li 1 , Tianhao Tan 2 , Yuan Zhao 1 , Yen Wei 1 , Dong Wang 2 , Rongjun Chen 3 , Lei Tao 1
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We developed a polymer–drug strategy to explore anticancer polymers. A series of monomers containing groups with potential anticancer activity have been facilely prepared through the Biginelli reaction. These monomers were used to produce water-soluble polymers through convenient radical copolymerization. The resulting polymers are biocompatible and can be directly used to suppress proliferation of different cancer cells without the release of small molecules. Theoretical calculations revealed that Biginelli groups in polymers had strong interaction with the Eg5 protein, which is highly expressed in cancer cells and is closely related to cell mitosis. Subsequent cell experiments confirmed that a screened polymer is efficient in inhibiting mitosis in different cancer cells. Our study of exploring functional polymers via the combination of multicomponent reactions and theoretical calculation resulted in promising anticancer polymers, which might pave a path for de novo designing of functional polymers and have important implications in the fields of organic, computational, and polymer chemistry.
中文翻译：
通过 Biginelli 反应的抗癌聚合物
我们开发了一种聚合物-药物策略来探索抗癌聚合物。通过 Biginelli 反应，已经容易地制备了一系列含有具有潜在抗癌活性的基团的单体。这些单体用于通过方便的自由基共聚来生产水溶性聚合物。所得聚合物具有生物相容性，可直接用于抑制不同癌细胞的增殖，而不会释放小分子。理论计算表明，聚合物中的 Biginelli 基团与 Eg5 蛋白有很强的相互作用，该蛋白在癌细胞中高度表达，与细胞有丝分裂密切相关。随后的细胞实验证实，筛选出的聚合物可有效抑制不同癌细胞的有丝分裂。
更新日期：2020-09-15
中文翻译：
通过 Biginelli 反应的抗癌聚合物
我们开发了一种聚合物-药物策略来探索抗癌聚合物。通过 Biginelli 反应，已经容易地制备了一系列含有具有潜在抗癌活性的基团的单体。这些单体用于通过方便的自由基共聚来生产水溶性聚合物。所得聚合物具有生物相容性，可直接用于抑制不同癌细胞的增殖，而不会释放小分子。理论计算表明，聚合物中的 Biginelli 基团与 Eg5 蛋白有很强的相互作用，该蛋白在癌细胞中高度表达，与细胞有丝分裂密切相关。随后的细胞实验证实，筛选出的聚合物可有效抑制不同癌细胞的有丝分裂。
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