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

Martin Matthew W.; Lancia David R. Jr.; 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.

首页> 外文期刊>Bioorganic and Medicinal Chemistry Letters >Discovery and optimization of novel piperazines as potent inhibitors of fatty acid synthase (FASN)

【24h】

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

机译：新型哌嗪的发现与优化作为脂肪酸合成酶的有效抑制剂（FASN）

获取原文

获取原文并翻译 | 示例

掌桥外文数据库（机构版） >>

开具论文收录证明 >>

文献代查 >>

页面导航

摘要
著录项
相似文献
相关主题

摘要

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.

机译：报道了一种新型脂肪酸合酶（FASN）抑制剂的新型脂肪酸合酶（FASN）抑制剂的发现，结构 - 活性关系和优化。高通量筛选鉴定了一系列具有结构特征的取代哌嗪，使得能够与FasN KR结构域结合位点的许多效力驱动区域相互作用。源自该系列的是FT113，一种具有强效生化和细胞活性的化合物，其在体内模型中转化为优异的活性。

著录项

来源
《Bioorganic and Medicinal Chemistry Letters》 |2019年第8期|共6页
作者
Martin Matthew W.; Lancia David R. Jr.; 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.;
展开▼
作者单位

FORMA Therapeut 500 Arsenal St Suite 100 Watertown MA 02472 USA;

FORMA Therapeut 500 Arsenal St Suite 100 Watertown MA 02472 USA;

FORMA Therapeut 35 Northeast Ind Rd Branford CT 06405 USA;

FORMA Therapeut 500 Arsenal St Suite 100 Watertown MA 02472 USA;

FORMA Therapeut 500 Arsenal St Suite 100 Watertown MA 02472 USA;

FORMA Therapeut 500 Arsenal St Suite 100 Watertown MA 02472 USA;

FORMA Therapeut 500 Arsenal St Suite 100 Watertown MA 02472 USA;

FORMA Therapeut 500 Arsenal St Suite 100 Watertown MA 02472 USA;

FORMA Therapeut 500 Arsenal St Suite 100 Watertown MA 02472 USA;

FORMA Therapeut 500 Arsenal St Suite 100 Watertown MA 02472 USA;

FORMA Therapeut 35 Northeast Ind Rd Branford CT 06405 USA;

FORMA Therapeut 35 Northeast Ind Rd Branford CT 06405 USA;

FORMA Therapeut 35 Northeast Ind Rd Branford CT 06405 USA;

FORMA Therapeut 35 Northeast Ind Rd Branford CT 06405 USA;

FORMA Therapeut 500 Arsenal St Suite 100 Watertown MA 02472 USA;

FORMA Therapeut 35 Northeast Ind Rd Branford CT 06405 USA;

FORMA Therapeut 500 Arsenal St Suite 100 Watertown MA 02472 USA;

FORMA Therapeut 500 Arsenal St Suite 100 Watertown MA 02472 USA;

展开▼
收录信息
原文格式 PDF
正文语种 eng
中图分类药学;
关键词
Fatty acid synthase; FASN; de novo lipogenesis; Oncology; Piperazines;

机译：脂肪酸合成酶;Fasn;de novo脂肪生成;肿瘤学;哌嗪;

相似文献

外文文献
中文文献
专利

1. Discovery and optimization of novel piperazines as potent inhibitors of fatty acid synthase (FASN) [J] . Martin Matthew W., Lancia David R. Jr., Li Hongbin, Bioorganic and Medicinal Chemistry Letters . 2019,第8期

机译：新型哌嗪的发现与优化作为脂肪酸合成酶的有效抑制剂（FASN）
2. Pharmacological Inhibitors of Fatty Acid Synthase (FASN)-Catalyzed Endogenous Fatty Acid Biogenesis: A New Family of Anti-Cancer Agents? [J] . Ruth Lupu Javier A. Menendez Current Pharmaceutical Biotechnology . 2006,第6期

机译：脂肪酸合酶（FASN）催化内源性脂肪酸生物发生的药理抑制剂：一个新的抗癌药物家族？
3. Polyunsaturated fatty acid suppression of fatty acid synthase (FASN): evidence for dietary modulation of NF-Y binding to the Fasn promoter by SREBP-1c [J] . Teran-Garcia M, Adamson AW, Yu G, The Biochemical Journal . 2007,第Pta3期

机译：脂肪酸合酶（FASN）的多不饱和脂肪酸抑制：饮食调节SREBP-1c调节NF-Y与Fasn启动子结合的证据
4. Targeting fatty acid synthase to inhibit tumor growth and overcome taxane resistance [C] . Joshua J. Souchek, Lindsey Muraskin, Lucas Houser, Visualizing and Quantifying Drug Distribution in Tissue III . 2019

机译：靶向脂肪酸合酶以抑制肿瘤生长并克服紫杉烷抗性
5. Application of organocatalysis to the synthesis of chiral morpholines, piperazines, aziridines, azetidines, beta-fluoroamines, and gamma-fluoroamines; discovery of selective phospholipase D inhibitors with optimized in vivo properties. [D] . O'Reilly, Matthew C. 2014

机译：有机催化在合成手性吗啉，哌嗪，氮丙啶，氮杂环丁烷，β-氟胺和γ-氟胺中的应用；发现具有优化体内特性的选择性磷脂酶D抑制剂。
6. Polyunsaturated fatty acid suppression of fatty acid synthase (FASN): evidence for dietary modulation of NF-Y binding to the Fasn promoter by SREBP-1c [O] . Margarita Teran-Garcia, Aaron W. Adamson, Gang Yu, 2007

机译：脂肪酸合酶（FASN）的多不饱和脂肪酸抑制：饮食调节SREBP-1c调节NF-Y与Fasn启动子结合的证据
7. Polyunsaturated fatty acid suppression of fatty acid synthase (FASN): evidence for dietary modulation of NF-Y binding to the Fasn promoter by SREBP-1c [O] . Teran-Garcia, Margarita, Adamson, Aaron W., Yu, Gang, 2007

机译：脂肪酸合酶（FASN）的多不饱和脂肪酸抑制：饮食调节SREBP-1c调节NF-Y与Fasn启动子结合的证据

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

摘要

著录项

相似文献

相关主题

期刊订阅