Potent N-(1, 3-thiazol-2-yl) pyridin-2-amine vascular endothelial growth factor receptor tyrosine kinase inhibitors with excellent pharmacokinetics and low affinity for …

MT Bilodeau, AE Balitza, TJ Koester…

Index: Borthwick,A.D. et al. Journal of the Chemical Society, Perkin Transactions 1: Organic and Bio-Organic Chemistry (1972-1999), 1973 , p. 2769 - 2772

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Citation Number: 48

Abstract

... Journal of Medicinal ... Chemistry. ... However, 2 was found to be very potent in an hERG binding assay and exhibited poor pharmacokinetics in dog with a clearance well above hepatic blood flow (Table 1). The lipophilicity of 2 was high (log P = 3.59) and was considered to be a ...

Potent N-(1, 3-thiazol-2-yl) pyridin-2-amine vascular endoth...

[Bilodeau, Mark T.; Balitza, Adrienne E.; Koester, Timothy J.; Manley, Peter J.; Rodman, Leonard D.; Buser-Doepner, Carolyn; Coll, Kathleen E.; Fernandes, Christine; Gibbs, Jackson B.; Heimbrook, David C.; Huckle, William R.; Kohl, Nancy; Lynch, Joseph J.; Mao, Xianzhi; McFall, Rosemary C.; McLoughlin, Debra; Miller-Stein, Cynthia M.; Rickert, Keith W.; Sepp-Lorenzino, Laura; Shipman, Jennifer M.; Subramanian, Raju; Thomas, Kenneth A.; Wong, Bradley K.; Yu, Sean; Hartman, George D. Journal of Medicinal Chemistry, 2004 , vol. 47, # 25 p. 6363 - 6372]