Discovery and optimization of novel piperazines as potent inhibitors of fatty acid synthase (FASN).

Matthew W Martin,David R Lancia,Hongbin Li,Shawn E R Schiller,Angela V Toms,Zhongguo Wang,Kenneth W Bair,Jennifer Castro,Shawn Fessler,Deepali Gotur,Stephen E Hubbs,Goss S Kauffman,Mark Kershaw,George P Luke,Crystal McKinnon,Lili Yao,Wei Lu,David S Millan

Bioorganic & Medicinal Chemistry Letters（2019）

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摘要

•Identified novel and potent inhibitors of FASN KR domain.•Synthesis and structure activity relationships of compounds are reported.•FT113 displays excellent cellular activity and pharmacokinetic properties.•FT113 is a valuable tool to develop POC models of DNL driven disease.

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关键词

Fatty acid synthase,FASN,de novo lipogenesis,Oncology,Piperazines

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