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芳基取代的二氢嘧啶对驱动蛋白Eg5的作用:一种癌症治疗的新方法

Aryl-Substituted Dihydro-Pyrimidines Effecting Kinesin Eg5 as Novel Approach for Cancer Treatment.

作者信息

Chlorou Dialekti, Pontiki Eleni

机构信息

Laboratory of Pharmaceutical Chemistry, Faculty of Health Sciences, School of Pharmacy, Aristotle University of Thessaloniki, 54124 Thessaloniki, Greece.

出版信息

Molecules. 2025 Aug 3;30(15):3256. doi: 10.3390/molecules30153256.

Abstract

Cancer is one of the most lethal diseases of this century. Unfortunately, many anticancer agents have harsh side effects or fail to work against cancer any longer due to tolerance. Dihydropyrimidinones are promising structures containing a pyrimidine ring. Targeting Eg5 is their most well-known activity. Inhibition of this enzyme gives them the privilege of strong cytotoxic activity with less side effects. Phenyl ring is a group that can be found in the majority of organic molecules and possesses preferable pharmacokinetic and pharmacodynamic characteristics. This review studies DHPM derivatives that are substituted with a phenyl ring and possess antiproliferative ability by inhibiting Eg5. The compounds are able to inhibit different cancer cell lines, and some are more potent than the standard drug. The biological results are in accordance with the docking studies.

摘要

癌症是本世纪最致命的疾病之一。不幸的是,许多抗癌药物有严重的副作用,或者由于耐受性而不再对癌症起作用。二氢嘧啶酮是含有嘧啶环的有前景的结构。靶向驱动蛋白5(Eg5)是它们最广为人知的活性。抑制这种酶赋予它们具有强细胞毒性活性且副作用较小的优势。苯环是大多数有机分子中都能找到的基团,具有较好的药代动力学和药效学特性。本综述研究了被苯环取代并通过抑制Eg5具有抗增殖能力的二氢嘧啶酮衍生物。这些化合物能够抑制不同的癌细胞系,有些比标准药物更有效。生物学结果与对接研究一致。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/30b4/12348194/bc19a9178e09/molecules-30-03256-g004.jpg

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