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A novel orally bioavailable inhibitor of kinase insert domain-containing receptor induces antiangiogenic effects and prevents tumor growth in vivo.
Sepp-Lorenzino L, Rands E, Mao X, Connolly B, Shipman J, Antanavage J, Hill S, Davis L, Beck S, Rickert K, Coll K, Ciecko P, Fraley M, Hoffman W, Hartman G, Heimbrook D, Gibbs J, Kohl N, Thomas K. Sepp-Lorenzino L, et al. Cancer Res. 2004 Jan 15;64(2):751-6. doi: 10.1158/0008-5472.can-03-2871. Cancer Res. 2004. PMID: 14744794
Optimization of the indolyl quinolinone class of KDR (VEGFR-2) kinase inhibitors: effects of 5-amido- and 5-sulphonamido-indolyl groups on pharmacokinetics and hERG binding.
Fraley ME, Arrington KL, Buser CA, Ciecko PA, Coll KE, Fernandes C, Hartman GD, Hoffman WF, Lynch JJ, McFall RC, Rickert K, Singh R, Smith S, Thomas KA, Wong BK. Fraley ME, et al. Among authors: thomas ka. Bioorg Med Chem Lett. 2004 Jan 19;14(2):351-5. doi: 10.1016/j.bmcl.2003.11.007. Bioorg Med Chem Lett. 2004. PMID: 14698157
Potent 2-[(pyrimidin-4-yl)amine}-1,3-thiazole-5-carbonitrile-based inhibitors of VEGFR-2 (KDR) kinase.
Sisko JT, Tucker TJ, Bilodeau MT, Buser CA, Ciecko PA, Coll KE, Fernandes C, Gibbs JB, Koester TJ, Kohl N, Lynch JJ, Mao X, McLoughlin D, Miller-Stein CM, Rodman LD, Rickert KW, Sepp-Lorenzino L, Shipman JM, Thomas KA, Wong BK, Hartman GD. Sisko JT, et al. Among authors: thomas ka. Bioorg Med Chem Lett. 2006 Mar 1;16(5):1146-50. doi: 10.1016/j.bmcl.2005.11.089. Epub 2005 Dec 20. Bioorg Med Chem Lett. 2006. PMID: 16368234
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: thomas ka. J Med Chem. 2004 Dec 2;47(25):6363-72. doi: 10.1021/jm049697f. J Med Chem. 2004. PMID: 15566305
Property-based design of KDR kinase inhibitors.
Fraley ME, Hoffman WF, Arrington KL, Hungate RW, Hartman GD, McFall RC, Coll KE, Rickert K, Thomas KA, McGaughey GB. Fraley ME, et al. Among authors: thomas ka. Curr Med Chem. 2004 Mar;11(6):709-19. doi: 10.2174/0929867043455729. Curr Med Chem. 2004. PMID: 15032725 Review.
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