Discovery and optimization of novel piperazines as potent inhibitors of fatty acid synthase (FASN).
Basic Information
ID: ALA4400560
Journal: Bioorg Med Chem Lett
Title: Discovery and optimization of novel piperazines as potent inhibitors of fatty acid synthase (FASN).
Authors: Martin MW, Lancia DR, Li H, Schiller SER, Toms AV, Wang Z, Bair KW, Castro J, Fessler S, Gotur D, Hubbs SE, Kauffman GS, Kershaw M, Luke GP, McKinnon C, Yao L, Lu W, Millan DS.
Abstract: 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.
CiteXplore: 30803804
DOI: 10.1016/j.bmcl.2019.02.012
Patent ID: ┄