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Optimization of the Lead Compound NVP-BHG712 as a Colorectal Cancer Inhibitor
Chemistry - A European Journal ( IF 3.9 ) Pub Date : 2023-02-17 , DOI: 10.1002/chem.202203967
Alix Tröster 1 , Michael DiPrima 2 , Nathalie Jores 1 , Denis Kudlinzki 1, 3 , Sridhar Sreeramulu 1 , Santosh L Gande 1, 3 , Verena Linhard 1 , Damian Ludig 1 , Alexander Schug 1 , Krishna Saxena 1 , Maria Reinecke 4, 5 , Stephanie Heinzlmeir 4 , Matthias S Leisegang 6 , Jan Wollenhaupt 7 , Frank Lennartz 7 , Manfred S Weiss 7 , Bernhard Kuster 4, 5, 8 , Giovanna Tosato 2 , Harald Schwalbe 1, 3
Affiliation  

Towards controlling colon carcinoma: Derivatives of the compound NVP-BHG712 as well as triazine-based molecules prove to be potent inhibitors of the receptor tyrosine kinase EPHA2. Several of these newly synthesized inhibitors showed highly promising effects in controlling human colon carcinoma. Furthermore, these molecules can act as tool compounds to gain a deeper understanding of the role of ephrin receptors in cellular context.

中文翻译:

作为结直肠癌抑制剂的先导化合物 NVP-BHG712 的优化

控制结肠癌:化合物 NVP-BHG712 的衍生物以及基于三嗪的分子被证明是受体酪氨酸激酶 EPHA2 的有效抑制剂。这些新合成的抑制剂中有几种在控制人类结肠癌方面显示出非常有前途的效果。此外,这些分子可以作为工具化合物,以更深入地了解肝配蛋白受体在细胞环境中的作用。
更新日期:2023-02-17
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