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Page 1
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
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. J Med Chem. 2004 Dec 2;47(25):6363-72. doi: 10.1021/jm049697f. J Med Chem. 2004. PMID: 15566305
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. 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
3-(Indol-2-yl)indazoles as Chek1 kinase inhibitors: Optimization of potency and selectivity via substitution at C6.
Fraley ME, Steen JT, Brnardic EJ, Arrington KL, Spencer KL, Hanney BA, Kim Y, Hartman GD, Stirdivant SM, Drakas BA, Rickert K, Walsh ES, Hamilton K, Buser CA, Hardwick J, Tao W, Beck SC, Mao X, Lobell RB, Sepp-Lorenzino L, Yan Y, Ikuta M, Munshi SK, Kuo LC, Kreatsoulas C. Fraley ME, et al. Bioorg Med Chem Lett. 2006 Dec 1;16(23):6049-53. doi: 10.1016/j.bmcl.2006.08.118. Epub 2006 Sep 15. Bioorg Med Chem Lett. 2006. PMID: 16978863
Development of 6-substituted indolylquinolinones as potent Chek1 kinase inhibitors.
Huang S, Garbaccio RM, Fraley ME, Steen J, Kreatsoulas C, Hartman G, Stirdivant S, Drakas B, Rickert K, Walsh E, Hamilton K, Buser CA, Hardwick J, Mao X, Abrams M, Beck S, Tao W, Lobell R, Sepp-Lorenzino L, Yan Y, Ikuta M, Murphy JZ, Sardana V, Munshi S, Kuo L, Reilly M, Mahan E. Huang S, et al. Bioorg Med Chem Lett. 2006 Nov 15;16(22):5907-12. doi: 10.1016/j.bmcl.2006.08.053. Epub 2006 Sep 20. Bioorg Med Chem Lett. 2006. PMID: 16990002
Optimization of a pyrazoloquinolinone class of Chk1 kinase inhibitors.
Brnardic EJ, Garbaccio RM, Fraley ME, Tasber ES, Steen JT, Arrington KL, Dudkin VY, Hartman GD, Stirdivant SM, Drakas BA, Rickert K, Walsh ES, Hamilton K, Buser CA, Hardwick J, Tao W, Beck SC, Mao X, Lobell RB, Sepp-Lorenzino L, Yan Y, Ikuta M, Munshi SK, Kuo LC, Kreatsoulas C. Brnardic EJ, et al. Bioorg Med Chem Lett. 2007 Nov 1;17(21):5989-94. doi: 10.1016/j.bmcl.2007.07.051. Epub 2007 Aug 19. Bioorg Med Chem Lett. 2007. PMID: 17804227
Synthesis and evaluation of substituted benzoisoquinolinones as potent inhibitors of Chk1 kinase.
Garbaccio RM, Huang S, Tasber ES, Fraley ME, Yan Y, Munshi S, Ikuta M, Kuo L, Kreatsoulas C, Stirdivant S, Drakas B, Rickert K, Walsh ES, Hamilton KA, Buser CA, Hardwick J, Mao X, Beck SC, Abrams MT, Tao W, Lobell R, Sepp-Lorenzino L, Hartman GD. Garbaccio RM, et al. Bioorg Med Chem Lett. 2007 Nov 15;17(22):6280-5. doi: 10.1016/j.bmcl.2007.09.007. Epub 2007 Sep 7. Bioorg Med Chem Lett. 2007. PMID: 17900896
Development of thioquinazolinones, allosteric Chk1 kinase inhibitors.
Converso A, Hartingh T, Garbaccio RM, Tasber E, Rickert K, Fraley ME, Yan Y, Kreatsoulas C, Stirdivant S, Drakas B, Walsh ES, Hamilton K, Buser CA, Mao X, Abrams MT, Beck SC, Tao W, Lobell R, Sepp-Lorenzino L, Zugay-Murphy J, Sardana V, Munshi SK, Jezequel-Sur SM, Zuck PD, Hartman GD. Converso A, et al. Bioorg Med Chem Lett. 2009 Feb 15;19(4):1240-4. doi: 10.1016/j.bmcl.2008.12.076. Epub 2008 Dec 24. Bioorg Med Chem Lett. 2009. PMID: 19155174
Pyridyl aminothiazoles as potent Chk1 inhibitors: optimization of cellular activity.
Dudkin VY, Wang C, Arrington KL, Fraley ME, Hartman GD, Stirdivant SM, Drakas RA, Rickert K, Walsh ES, Hamilton K, Buser CA, Hardwick J, Tao W, Beck SC, Mao X, Lobell RB, Sepp-Lorenzino L. Dudkin VY, et al. Bioorg Med Chem Lett. 2012 Apr 1;22(7):2613-9. doi: 10.1016/j.bmcl.2012.01.120. Epub 2012 Feb 7. Bioorg Med Chem Lett. 2012. PMID: 22365762
83 results