Design and synthesis of 7H-pyrrolo[2,3-d]pyrimidines as focal adhesion kinase inhibitors. Part 1 was written by Choi, Ha-Soon;Wang, Zhicheng;Richmond, Wendy;He, Xiaohui;Yang, Kunyong;Jiang, Tao;Sim, Taebo;Karanewsky, Donald;Gu, Xiang-Ju;Zhou, Vicki;Liu, Yi;Ohmori, Osamu;Caldwell, Jeremy;Gray, Nathanael;He, Yun. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2006.Category: pyridine-derivatives This article mentions the following:
(amino)(aryl)pyrrolo[2,3-d]pyrimidines such as I and II and pyridopyrimidines such as III are prepared as inhibitors of focal adhesion kinase (FAK). The structure-activity relationships for pyrrolopyrimidines are determined; electron-donating arylamino substituents at the 2-position and pyridinyl substituents at the 9-position lead to moderately active FAK inhibitors, while oxo-substituted analogs have reduced activities. I, II, and III inhibit FAK with IC50 values of 0.1 μM, 0.1 μM, and 0.2 μM, resp., comparable to the initial lead compound IV (IC50 = 0.1 μM). In the experiment, the researchers used many compounds, for example, 3-Bromo-4-fluoropyridine (cas: 116922-60-2Category: pyridine-derivatives).
3-Bromo-4-fluoropyridine (cas: 116922-60-2) belongs to pyridine derivatives. Pyridine’s the lone pair does not contribute to the aromatic system but importantly influences the chemical properties of pyridine, as it easily supports bond formation via an electrophilic attack. Pyridine derivatives are also useful as small-molecule α-helix mimetics that inhibit protein-protein interactions, as well as functionally selective GABA ligands.Category: pyridine-derivatives