New electrophiles targeting thiols in a reversible covalent manner

被引:0
|
作者
Ma, Xingyu [1 ,2 ]
Xu, Manyi [1 ,2 ]
Wang, Fengge [1 ,2 ]
Hu, Tingting [1 ,2 ]
Chen, Xinyuan [1 ,2 ]
Zhang, Chong-Jing [1 ,2 ]
机构
[1] Peking Union Med Coll & Chinese Acad Med Sci, Inst Mat Med, State Key Lab Bioact Subst & Funct Nat Med, Beijing 100050, Peoples R China
[2] Peking Union Med Coll & Chinese Acad Med Sci, Inst Mat Med, Beijing Key Lab Act Subst Discovery & Druggabil Ev, Beijing 100050, Peoples R China
基金
中国国家自然科学基金;
关键词
RATIONAL DESIGN; INHIBITOR; CYSTEINES;
D O I
10.1039/d4cc04612a
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
Reversible covalent electrophiles with the advantages of both reversible and covalent interactions receive much attention in the fields of chemical biology and medicinal chemistry. Here, we report two electron-deficient olefins activated by amide and ester, amide-substituted acrylamide and methyl ester-substituted acrylamide, targeting thiols in a reversible covalent manner. Two electron-deficient olefins activated by amide and ester, amide-substituted acrylamide and methyl ester-substituted acrylamide, targeting thiols in a reversible covalent manner were reported.
引用
收藏
页码:12437 / 12440
页数:4
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