A scaffold replacement approach towards new sirtuin 2 inhibitors.

Tina Seifert,Marcus Malo,Tarja Kokkola,E Johanna L Stéen,Kristian Meinander,Erik A A Wallén,Elina M Jarho,Kristina Luthman

Bioorganic & Medicinal Chemistry（2020）

引用 6|浏览18

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摘要

•Five heterocyclic core structures were explored as chroman-4-one/chromone bioisosteres.•Synthesis and biological evaluation of 24 new derivatives as potential SIRT2 inhibitors.•The new scaffolds provided improved physicochemical properties.•Benzothiadiazine-1,1-dioxide-based derivatives showed good SIRT2 inhibitory activity.•Two compounds showed high inhibitory activity also against SIRT3.

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关键词

Scaffold,Sirtuin,SIRT2,Inhibitor,Benzothiazine-1,1-dioxide,Benzothiadiazine-1,1-dioxides,Saccharin,Quinolin-4-one,Docking

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