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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.
Afiliação
  • Martin MW; FORMA Therapeutics, 500 Arsenal Street, Suite 100, Watertown, MA 02472, USA. Electronic address: mmartin@formatherapeutics.com.
  • Lancia DR; FORMA Therapeutics, 500 Arsenal Street, Suite 100, Watertown, MA 02472, USA.
  • Li H; FORMA Therapeutics, 35 Northeast Industrial Road, Branford, CT 06405, USA.
  • Schiller SER; FORMA Therapeutics, 500 Arsenal Street, Suite 100, Watertown, MA 02472, USA.
  • Toms AV; FORMA Therapeutics, 500 Arsenal Street, Suite 100, Watertown, MA 02472, USA.
  • Wang Z; FORMA Therapeutics, 500 Arsenal Street, Suite 100, Watertown, MA 02472, USA.
  • Bair KW; FORMA Therapeutics, 500 Arsenal Street, Suite 100, Watertown, MA 02472, USA.
  • Castro J; FORMA Therapeutics, 500 Arsenal Street, Suite 100, Watertown, MA 02472, USA.
  • Fessler S; FORMA Therapeutics, 500 Arsenal Street, Suite 100, Watertown, MA 02472, USA.
  • Gotur D; FORMA Therapeutics, 500 Arsenal Street, Suite 100, Watertown, MA 02472, USA.
  • Hubbs SE; FORMA Therapeutics, 35 Northeast Industrial Road, Branford, CT 06405, USA.
  • Kauffman GS; FORMA Therapeutics, 35 Northeast Industrial Road, Branford, CT 06405, USA.
  • Kershaw M; FORMA Therapeutics, 35 Northeast Industrial Road, Branford, CT 06405, USA.
  • Luke GP; FORMA Therapeutics, 35 Northeast Industrial Road, Branford, CT 06405, USA.
  • McKinnon C; FORMA Therapeutics, 500 Arsenal Street, Suite 100, Watertown, MA 02472, USA.
  • Yao L; FORMA Therapeutics, 35 Northeast Industrial Road, Branford, CT 06405, USA.
  • Lu W; FORMA Therapeutics, 500 Arsenal Street, Suite 100, Watertown, MA 02472, USA.
  • Millan DS; FORMA Therapeutics, 500 Arsenal Street, Suite 100, Watertown, MA 02472, USA.
Bioorg Med Chem Lett ; 29(8): 1001-1006, 2019 04 15.
Article em En | MEDLINE | ID: mdl-30803804
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.
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Piperazinas / Ácido Graxo Sintases Limite: Animals / Humans Idioma: En Ano de publicação: 2019 Tipo de documento: Article
Texto completo
Imprimir
XML
PubMed Links
Buscar no Google

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Piperazinas / Ácido Graxo Sintases Limite: Animals / Humans Idioma: En Ano de publicação: 2019 Tipo de documento: Article