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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. Among authors: kendall rl. 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
Evolution of a highly selective and potent 2-(pyridin-2-yl)-1,3,5-triazine Tie-2 kinase inhibitor.
Hodous BL, Geuns-Meyer SD, Hughes PE, Albrecht BK, Bellon S, Bready J, Caenepeel S, Cee VJ, Chaffee SC, Coxon A, Emery M, Fretland J, Gallant P, Gu Y, Hoffman D, Johnson RE, Kendall R, Kim JL, Long AM, Morrison M, Olivieri PR, Patel VF, Polverino A, Rose P, Tempest P, Wang L, Whittington DA, Zhao H. Hodous BL, et al. J Med Chem. 2007 Feb 22;50(4):611-26. doi: 10.1021/jm061107l. Epub 2007 Jan 25. J Med Chem. 2007. PMID: 17253678
61 results