1630808-89-7Relevant academic research and scientific papers
Discovery and optimization of novel piperazines as potent inhibitors of fatty acid synthase (FASN)
Martin, Matthew W.,Lancia, David R.,Li, Hongbin,Schiller, Shawn E.R.,Toms, Angela V.,Wang, Zhongguo,Bair, Kenneth W.,Castro, Jennifer,Fessler, Shawn,Gotur, Deepali,Hubbs, Stephen E.,Kauffman, Goss S.,Kershaw, Mark,Luke, George P.,McKinnon, Crystal,Yao, Lili,Lu, Wei,Millan, David S.
, p. 1001 - 1006 (2019)
The discovery, structure-activity relationships, and optimization of a novel class of fatty acid synthase (FASN) inhibitors is reported. High throughput screening identified a series of substituted piperazines with structural features that enable interactions with many of the potency-driving regions of the FASN KR domain binding site. Derived from this series was FT113, a compound with potent biochemical and cellular activity, which translated into excellent activity in in vivo models.
NOVEL COMPOUNDS AND COMPOSITIONS FOR INHIBITION OF FASN
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Page/Page column 245; 246; 331, (2014/10/18)
The present invention relates to compounds and composition for inhibition of FASN, their synthesis, applications, and antidotes. An illustrative compound of the invention is shown below:
