Design, synthesis and biological evaluation of bicyclic carboxylic acid derivatives as IDO1 inhibitors.

Shi Cai,Xiaojun Yang,Pan Chen,Xueting Liu,Jinpei Zhou,Huibin Zhang

Bioorganic Chemistry（2020）

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摘要

•Twenty-six bicyclic carboxylic acid derivatives were designed and synthesized.•Molecular docking studies were performed.•IDO1 inhibitory activities were evaluated by HeLa and THP-1 cellular assay.•The compound 9c (HeLa IC50 = 2.6 nM, THP-1 IC50 = 11.2 nM) inhibited tumor growth of CT26 model effectively.

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关键词

Immunotheraphy,l-tryptophan,IDO1 inhibitors,Hela cell assay

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