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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. 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
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. 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
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
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. Curr Med Chem. 2004 Mar;11(6):709-19. doi: 10.2174/0929867043455729. Curr Med Chem. 2004. PMID: 15032725 Review.
Kinesin spindle protein (KSP) inhibitors. Part 3: synthesis and evaluation of phenolic 2,4-diaryl-2,5-dihydropyrroles with reduced hERG binding and employment of a phosphate prodrug strategy for aqueous solubility.
Garbaccio RM, Fraley ME, Tasber ES, Olson CM, Hoffman WF, Arrington KL, Torrent M, Buser CA, Walsh ES, Hamilton K, Schaber MD, Fernandes C, Lobell RB, Tao W, South VJ, Yan Y, Kuo LC, Prueksaritanont T, Slaughter DE, Shu C, Heimbrook DC, Kohl NE, Huber HE, Hartman GD. Garbaccio RM, et al. Among authors: fraley me. Bioorg Med Chem Lett. 2006 Apr 1;16(7):1780-3. doi: 10.1016/j.bmcl.2005.12.094. Epub 2006 Jan 24. Bioorg Med Chem Lett. 2006. PMID: 16439122
38 results