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新型基于 α-酮酰胺的重氮二氢氧化物作为过氧化氢响应性一氧化氮供体,具有抗肺癌活性。

Novel α-ketoamide based diazeniumdiolates as hydrogen peroxide responsive nitric oxide donors with anti-lung cancer activity.

机构信息

Key Laboratory of Carbohydrate Chemistry and Biotechnology, Ministry of Education, School of Biotechnology, Jiangnan University, Wuxi 214122, P. R. China.

School of Chemistry & Materials Science, Jiangsu Key Laboratory of Green Synthetic Chemistry for Functional Materials, Jiangsu Normal University, Xuzhou 221116, P. R. China.

出版信息

Chem Commun (Camb). 2019 Oct 24;55(86):12904-12907. doi: 10.1039/c9cc05266f.

Abstract

A novel type of hydrogen peroxide (H2O2)-activated diazeniumdiolate based on an α-ketoamide moietey was developed as a nitric oxide (NO) donor. KA-NO-4 inhibited lung cancer cells with submicromolar activity. The H2O2-responsive behaviour of KA-NO-4 was thoroughly investigated. The NO-centered mechanism of action of KA-NO-4 was intracellularly studied.

摘要

一种新型的基于α-酮酰胺结构的过氧氢(H2O2)激活的重氮二氧杂环戊烯作为一氧化氮(NO)供体被开发出来。KA-NO-4 以亚微摩尔的活性抑制肺癌细胞。彻底研究了 KA-NO-4 的 H2O2 响应行为。研究了 KA-NO-4 的以 NO 为中心的作用机制。

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