Design and synthesis of 3, 7-diarylimidazopyridines as inhibitors of the VEGF-receptor KDR

…, K Rickert, J Shipman, B Shi, L Sepp-Lorenzino…

Index: Wu, Zhicai; Fraley, Mark E.; Bilodeau, Mark T.; Kaufman, Mildred L.; Tasber, Edward S.; Balitza, Adrienne E.; Hartman, George D.; Coll, Kathleen E.; Rickert, Keith; Shipman, Jennifer; Shi, Bin; Sepp-Lorenzino, Laura; Thomas, Kenneth A. Bioorganic and Medicinal Chemistry Letters, 2004 , vol. 14, # 4 p. 909 - 912

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Citation Number: 42

Abstract

As part of an effort to develop inhibitors of KDR, 3,6-diarylpyrazolo[1,5-a]pyrimidines ( 1, Chart 1) have been found to be potent inhibitors of KDR kinase activity. 11 and 12 Compounds of this series had been hindered by poor physical properties, including low solubility, high logP and high protein binding. To address these limitations, an effort was initiated to explore other templates including benzimidazoles 2 and imidazopyridines 3. These cores are likely replacements ...