Identification of potent and selective VEGFR receptor tyrosine kinase inhibitors having new amide isostere headgroups.

Gaudette F; Raeppel S; Nguyen

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Identification of potent and selective VEGFR receptor tyrosine kinase inhibitors having new amide isostere headgroups.

机译：鉴定具有新酰胺等排头基的有效和选择性的VEGFR受体酪氨酸激酶抑制剂。

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A novel series of malonamide-type dual VEGFR2/c-Met inhibitors in which one of the amide bonds was replaced by an amide isostere-a trifluoroethylamine unit, was designed, synthesized, and evaluated for their enzymatic and cellular inhibition of VEGFR2 and c-Met enzymes. Optimization of these molecular entities resulted in identification of potent and selective inhibitors of VEGFR2 enzyme.

机译：设计，合成并评估了一系列新的丙二酰胺型双VEGFR2 / c-Met抑制剂，其中一个酰胺键被一个酰胺等位物（一个三氟乙胺单元）取代，并评估了它们对VEGFR2和c-的酶促和细胞抑制作用酶。这些分子实体的优化导致鉴定出VEGFR2酶的有效和选择性抑制剂。

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《Bioorganic and Medicinal Chemistry Letters》 |2010年第3期|共5页
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Gaudette F; Raeppel S; Nguyen;
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1. Identification of potent and selective VEGFR receptor tyrosine kinase inhibitors having new amide isostere headgroups. [J] . Gaudette F, Raeppel S, Nguyen Bioorganic and Medicinal Chemistry Letters . 2010,第3期

机译：鉴定具有新酰胺等排头基的有效和选择性的VEGFR受体酪氨酸激酶抑制剂。
2. 50 POSTER Unique enzymatic profile of a potent and selective VEGFR/PDGFR tyrosine kinase inhibitor, TAK-593: potent pseudo-irreversibility against VEGFR and PDGFR [J] . H.Miki, H.Iwata, M.Amamo, European Journal of Cancer Supplements . 2008,第12期

机译：50 POSTER强效和选择性VEGFR / PDGFR酪氨酸激酶抑制剂TAK-593的独特酶学特征：针对VEGFR和PDGFR的强假不可逆性
3. 50 POSTER Unique enzymatic profile of a potent and selective VEGFR/PDGFR tyrosine kinase inhibitor, TAK-593: potent pseudo-irreversibility against VEGFR and PDGFR [J] . H.Miki, H.Iwata, M.Amamo, European Journal of Cancer Supplements . 2008,第12期

机译：50 POSTER强效和选择性VEGFR / PDGFR酪氨酸激酶抑制剂TAK-593的独特酶学特征：针对VEGFR和PDGFR的强假不可逆性
4. Taking Quinazoline as a General Support-Nog to Design Potent and Selective Kinase Inhibitors: Application to FMS-like Tyrosine Kinase 3 [C] . Wei-Wei Li, Luo-Ding Yu, Li-Juan Chen, ICMSI;International conference of molecular simulations and applied informatics technologies . 2010

机译：以喹唑啉作为一般支持物来设计有效和选择性激酶抑制剂：在类似FMS的酪氨酸激酶3中的应用
5. Pharmacological Characterization of TAS05567, a Potent and Selective Inhibitor of Spleen Tyrosine Kinase, in Animal Models of Inflammatory Diseases and B-cell Malignancies [D] . 林宏明 2019

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6. Discovery of fruquintinib a potent and highly selective small molecule inhibitor of VEGFR 1 2 3 tyrosine kinases for cancer therapy [O] . Qiaoling Sun, Jinghong Zhou, Zheng Zhang, 2014

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机译：新型有效口服活性选择性选择性VEGFR-2酪氨酸激酶抑制剂：N-苯基-N- {4-（4-喹啉氧基）苯基}脲的合成，结构活性关系和抗肿瘤活性

Identification of potent and selective VEGFR receptor tyrosine kinase inhibitors having new amide isostere headgroups.

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