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含氟腙衍生物作为多功能抗阿尔茨海默病药物,具有 CK2 抑制和抗氧化特性。

Organofluorine Hydrazone Derivatives as Multifunctional Anti-Alzheimer's Agents with CK2 Inhibitory and Antioxidant Features.

机构信息

Department of Animal Physiology and Toxicology, The John Paul II Catholic University of Lublin, ul. Konstantynów 1i, 20-708, Lublin, Poland.

Department of Chemistry, University of Massachusetts Boston, 100 Morrissey Blvd, Boston, MA, 02125, USA.

出版信息

ChemMedChem. 2021 Jun 17;16(12):1927-1932. doi: 10.1002/cmdc.202100047. Epub 2021 Apr 8.

Abstract

A set of novel hydrazone derivatives were synthesized and analyzed for their biological activities. The compounds were tested for their inhibitory effect on the phosphorylating activity of the protein kinase CK2, and their antioxidant activity was also determined in three commonly used assays. The hydrazones were evaluated for their radical scavenging against the DPPH, ABTS and peroxyl radicals. Several compounds have been identified as good antioxidants as well as potent protein kinase CK2 inhibitors. Most hydrazones containing a 4-N(CH ) residue or perfluorinated phenyl rings showed high activity in the radical-scavenging assays and possess nanomolar IC values in the kinase assays.

摘要

一组新型腙衍生物被合成并分析其生物活性。这些化合物被测试对蛋白激酶 CK2 的磷酸化活性的抑制作用,并且它们的抗氧化活性也在三种常用的测定方法中进行了测定。这些腙化合物被评估对 DPPH、ABTS 和过氧自由基的清除能力。已经鉴定出几种化合物作为良好的抗氧化剂和有效的蛋白激酶 CK2 抑制剂。含有 4-N(CH ) 基团或全氟苯基环的大多数腙化合物在自由基清除测定中表现出高活性,并且在激酶测定中具有纳摩尔 IC 值。

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