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

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

  • Bioorg Med Chem Lett. 2019 Apr 15;29(8):1001-1006. doi: 10.1016/j.bmcl.2019.02.012.
Matthew W Martin 1,  David R Lancia Jr 2,  Hongbin Li 3,  Shawn E R Schiller 2,  Angela V Toms 2,  Zhongguo Wang 2,  Kenneth W Bair 2,  Jennifer Castro 2,  Shawn Fessler 2,  Deepali Gotur 2,  Stephen E Hubbs 3,  Goss S Kauffman 3,  Mark Kershaw 3,  George P Luke 3,  Crystal McKinnon 2,  Lili Yao 3,  Wei Lu 2,  David S Millan 2
Affiliations

Affiliations

  • 1 FORMA Therapeutics, 500 Arsenal Street, Suite 100, Watertown, MA 02472, USA. Electronic address: mmartin@formatherapeutics.com.
  • 2 FORMA Therapeutics, 500 Arsenal Street, Suite 100, Watertown, MA 02472, USA.
  • 3 FORMA Therapeutics, 35 Northeast Industrial Road, Branford, CT 06405, USA.
PMID: 30803804 DOI: 10.1016/j.bmcl.2019.02.012
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.

Keywords

FASN; Fatty acid synthase; Oncology; Piperazines; de novo lipogenesis.

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