Development of Novel Small Chemical Inhibitors for Lck SH Domain with in vitro T-cell Inhibitory Activity

Bulletin of the Korean chemical society

Keun-Hyeung Lee¹  Hyeongjin Cho¹  See-Hyoung Park¹  Mi-Ae Kang¹  Hyeong-Soo Shim¹  Jonghwa Won¹ 

关键词: T-cell inhibition;    Bioavailability;    Antagonist;    Scaffold;    Lck SH2;   

DOI  :  

学科分类：化学（综合）

来源: Korean Chemical Society

【 摘 要 】

We investigated in vitro T-cell inhibitory activity and bioavailability of small chemical inhibitors for Lck SH2 domain, which had a different scaffold such as an amide bond, reduced amide bond, N-methyl amide bond, thioamide bond, and urethane bond. Each of these compounds, with its particular scaffold, showed a different logP value, stability against serum enzyme, stability in buffer solution, and in vitro T-cell inhibitory activity. Overall results indicated that the SH2 inhibitor containing urethane bond can be a new lead compound because of its superior bioavailability, potent in vitro T-cell inhibitory activity, and facile synthesis.

【 授权许可】

Unknown