Retinoic acid derivative based on NO donor and preparation method and application of retinoic acid derivative

The invention provides a retinoic acid derivative based on an NO donor and a preparation method and application of the retinoic acid derivative. A series of novel multi-target retinoic acid derivatives are designed and synthesized by taking a multi-target drug theory as guidance, taking Am580 as a p...

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Bibliographische Detailangaben
Hauptverfasser: WANG YINGYING, TANG KEHUI, DONG HONGBO, ZHANG CHUNRAN, DU WEIHONG, WANG YUCHI, CAO SHENGHUA, LUO HONGBING
Format: Patent
Sprache:chi ; eng
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Zusammenfassung:The invention provides a retinoic acid derivative based on an NO donor and a preparation method and application of the retinoic acid derivative. A series of novel multi-target retinoic acid derivatives are designed and synthesized by taking a multi-target drug theory as guidance, taking Am580 as a parent nucleus, combining structural characteristics of Am580 to select organic nitrate NO donors asNO sources, performing chemical modification on the NO donors to obtain a series of different donors and coupling ester or amido bonds with the parent nucleus. Tests show that the retinoic acid derivatives are higher in activity, lower in toxic and side effects and better in anti-tumor effect. The structural general formula of the retinoic acid derivative based on the NO donor provided by the invention is shown as a formula (I),. 本发明提供了一种基于NO供体的维甲酸类衍生物及其制备方法与应用。本发明以多靶点药物理论为指导,以Am580为母核并结合其结构特点选择了有机硝酸酯类(Organic nitrate)类NO供体作为NO源,通过对NO供体进行化学修饰,得到一系列不同的供体,再通过脂或者酰胺键与母核偶联,设计合成了一系列新型的多靶点维甲酸衍生物,试验表明该类维甲酸衍生物的活性更高、毒副作用更低、抗肿瘤效