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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 the hERG ion channel.
Bilodeau MT, Balitza AE, Koester TJ, Manley PJ, Rodman LD, Buser-Doepner C, Coll KE, Fernandes C, Gibbs JB, Heimbrook DC, Huckle WR, Kohl N, Lynch JJ, Mao X, McFall RC, McLoughlin D, Miller-Stein CM, Rickert KW, Sepp-Lorenzino L, Shipman JM, Subramanian R, Thomas KA, Wong BK, Yu S, Hartman GD. Bilodeau MT, et al. Among authors: huckle wr. J Med Chem. 2004 Dec 2;47(25):6363-72. doi: 10.1021/jm049697f. J Med Chem. 2004. PMID: 15566305
Optimization of a pyrazolo[1,5-a]pyrimidine class of KDR kinase inhibitors: improvements in physical properties enhance cellular activity and pharmacokinetics.
Fraley ME, Rubino RS, Hoffman WF, Hambaugh SR, Arrington KL, Hungate RW, Bilodeau MT, Tebben AJ, Rutledge RZ, Kendall RL, McFall RC, Huckle WR, Coll KE, Thomas KA. Fraley ME, et al. Among authors: huckle wr. Bioorg Med Chem Lett. 2002 Dec 16;12(24):3537-41. doi: 10.1016/s0960-894x(02)00827-2. Bioorg Med Chem Lett. 2002. PMID: 12443771
Paracrine expression of a native soluble vascular endothelial growth factor receptor inhibits tumor growth, metastasis, and mortality rate.
Goldman CK, Kendall RL, Cabrera G, Soroceanu L, Heike Y, Gillespie GY, Siegal GP, Mao X, Bett AJ, Huckle WR, Thomas KA, Curiel DT. Goldman CK, et al. Among authors: huckle wr. Proc Natl Acad Sci U S A. 1998 Jul 21;95(15):8795-800. doi: 10.1073/pnas.95.15.8795. Proc Natl Acad Sci U S A. 1998. PMID: 9671758 Free PMC article.
63 results