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一种新型TrkA受体酪氨酸激酶抑制剂的鉴定。

International Journal of Medicinal Chemistry Pub Date : 2012-01-01 Epub Date: 2012-05-02 DOI:10.1155/2012/412614
Stéphane L Raeppel, Frédéric Gaudette, Hannah Nguyen, Normand Beaulieu, James Wang, Christiane Maroun, Jeffrey M Besterman, Arkadii Vaisburg
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引用次数: 4

摘要

鉴定了一系列靶向TrkA受体酪氨酸激酶的N-(3-(6-取代-氨基吡啶-3-基氧基)苯基)-2-氧-3-苯基咪唑烷-1-羧酰胺。该系列的SAR研究使我们能够设计和合成具有低纳摩尔范围的TrkA激酶抑制活性的化合物，对c-Met的残留活性低，对VEGFR2没有明显的活性。
本文章由计算机程序翻译，如有差异，请以英文原文为准。

Identification of a Novel Series of Potent TrkA Receptor Tyrosine Kinase Inhibitors.

Identification of a Novel Series of Potent TrkA Receptor Tyrosine Kinase Inhibitors.

Identification of a Novel Series of Potent TrkA Receptor Tyrosine Kinase Inhibitors.

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Identification of a Novel Series of Potent TrkA Receptor Tyrosine Kinase Inhibitors.

A novel series of N-(3-(6-substituted-aminopyridin-3-yloxy)phenyl)-2-oxo-3-phenylimidazolidine-1-carboxamides targeting TrkA receptor tyrosine kinase was identified. SAR study of the series allowed us to design and synthesize compounds possessing inhibitory activity of TrkA kinase enzyme in the low nanomolar range with low residual activity against c-Met and with no significant activity against VEGFR2.

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来源期刊
International Journal of Medicinal Chemistry
International Journal of Medicinal Chemistry CHEMISTRY, MEDICINAL-
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期刊介绍： International Journal of Medicinal Chemistry is a peer-reviewed, Open Access journal that publishes original research articles as well as review articles in all areas of chemistry associated with drug discovery, design, and synthesis. International Journal of Medicinal Chemistry is a peer-reviewed, Open Access journal that publishes original research articles as well as review articles in all areas of chemistry associated with drug discovery, design, and synthesis.
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