2,7-naphthyridinone-based MET kinase inhibitors: A promising novel scaffold for antitumor drug development was written by Zhuo, Lin-Sheng;Xu, Hong-Chuang;Wang, Ming-Shu;Zhao, Xing-E.;Ming, Zhi-Hui;Zhu, Xiao-Lei;Huang, Wei;Yang, Guang-Fu. And the article was included in European Journal of Medicinal Chemistry in 2019.Reference of 65169-38-2 This article mentions the following:
As part of our effort to develop new mol. targeted antitumor drug, a novel 2,7-naphthyridone-based MET kinase inhibitor, I, was identified. Knowledge of the binding mode of BMS-777607 in MET led to the design of new inhibitors that utilize novel 2,7-naphthyridone scaffold to conformationally restrain the key pharmacophoric groups (block C). Detailed SAR studies resulted in the discovery of a new MET inhibitor I, displaying favorable in vitro potency and oral bioavailability. More importantly, I exhibited excellent in vivo efficacy (tumor growth inhibition/TGI of 114% and 95% in 50 mg/kg, resp.) both in the U-87 MG and HT-29 xenograft models. The favorable drug-likeness of I indicated that 2,7-naphthyridinone may be used a promising novel scaffold for antitumor drug development. The preclin. studies of I are under way. In the experiment, the researchers used many compounds, for example, 2-Chloro-4-methylpyridine-3-carbonitrile (cas: 65169-38-2Reference of 65169-38-2).
2-Chloro-4-methylpyridine-3-carbonitrile (cas: 65169-38-2) belongs to pyridine derivatives. Pyridines are an important class of heterocycles and occur in polysubstituted forms in many naturally occurring biologically active compounds, drug molecules and chiral ligands. Pyridine derivatives are also useful as small-molecule α-helix mimetics that inhibit protein-protein interactions, as well as functionally selective GABA ligands.Reference of 65169-38-2