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Page 1
Pyridyl-pyrimidine benzimidazole derivatives as potent, selective, and orally bioavailable inhibitors of Tie-2 kinase.
Cee VJ, Cheng AC, Romero K, Bellon S, Mohr C, Whittington DA, Bak A, Bready J, Caenepeel S, Coxon A, Deak HL, Fretland J, Gu Y, Hodous BL, Huang X, Kim JL, Lin J, Long AM, Nguyen H, Olivieri PR, Patel VF, Wang L, Zhou Y, Hughes P, Geuns-Meyer S. Cee VJ, et al. Among authors: caenepeel s. Bioorg Med Chem Lett. 2009 Jan 15;19(2):424-7. doi: 10.1016/j.bmcl.2008.11.056. Epub 2008 Nov 20. Bioorg Med Chem Lett. 2009. PMID: 19062275
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. Among authors: caenepeel s. J Med Chem. 2007 Feb 22;50(4):611-26. doi: 10.1021/jm061107l. Epub 2007 Jan 25. J Med Chem. 2007. PMID: 17253678
Alkynylpyrimidine amide derivatives as potent, selective, and orally active inhibitors of Tie-2 kinase.
Cee VJ, Albrecht BK, Geuns-Meyer S, Hughes P, Bellon S, Bready J, Caenepeel S, Chaffee SC, Coxon A, Emery M, Fretland J, Gallant P, Gu Y, Hodous BL, Hoffman D, Johnson RE, Kendall R, Kim JL, Long AM, McGowan D, Morrison M, Olivieri PR, Patel VF, Polverino A, Powers D, Rose P, Wang L, Zhao H. Cee VJ, et al. Among authors: caenepeel s. J Med Chem. 2007 Feb 22;50(4):627-40. doi: 10.1021/jm061112p. Epub 2007 Jan 25. J Med Chem. 2007. PMID: 17253679
Synthesis, structural analysis, and SAR studies of triazine derivatives as potent, selective Tie-2 inhibitors.
Hodous BL, Geuns-Meyer SD, Hughes PE, Albrecht BK, Bellon S, Caenepeel S, Cee VJ, Chaffee SC, Emery M, Fretland J, Gallant P, Gu Y, Johnson RE, Kim JL, Long AM, Morrison M, Olivieri PR, Patel VF, Polverino A, Rose P, Wang L, Zhao H. Hodous BL, et al. Among authors: caenepeel s. Bioorg Med Chem Lett. 2007 May 15;17(10):2886-9. doi: 10.1016/j.bmcl.2007.02.067. Epub 2007 Feb 25. Bioorg Med Chem Lett. 2007. PMID: 17350837
Structure-based design of a novel series of potent, selective inhibitors of the class I phosphatidylinositol 3-kinases.
Smith AL, D'Angelo ND, Bo YY, Booker SK, Cee VJ, Herberich B, Hong FT, Jackson CL, Lanman BA, Liu L, Nishimura N, Pettus LH, Reed AB, Tadesse S, Tamayo NA, Wurz RP, Yang K, Andrews KL, Whittington DA, McCarter JD, Miguel TS, Zalameda L, Jiang J, Subramanian R, Mullady EL, Caenepeel S, Freeman DJ, Wang L, Zhang N, Wu T, Hughes PE, Norman MH. Smith AL, et al. Among authors: caenepeel s. J Med Chem. 2012 Jun 14;55(11):5188-219. doi: 10.1021/jm300184s. Epub 2012 May 23. J Med Chem. 2012. PMID: 22548365
Synthesis and structure-activity relationships of dual PI3K/mTOR inhibitors based on a 4-amino-6-methyl-1,3,5-triazine sulfonamide scaffold.
Wurz RP, Liu L, Yang K, Nishimura N, Bo Y, Pettus LH, Caenepeel S, Freeman DJ, McCarter JD, Mullady EL, Miguel TS, Wang L, Zhang N, Andrews KL, Whittington DA, Jiang J, Subramanian R, Hughes PE, Norman MH. Wurz RP, et al. Among authors: caenepeel s. Bioorg Med Chem Lett. 2012 Sep 1;22(17):5714-20. doi: 10.1016/j.bmcl.2012.06.078. Epub 2012 Jul 3. Bioorg Med Chem Lett. 2012. PMID: 22832322
Selective class I phosphoinositide 3-kinase inhibitors: optimization of a series of pyridyltriazines leading to the identification of a clinical candidate, AMG 511.
Norman MH, Andrews KL, Bo YY, Booker SK, Caenepeel S, Cee VJ, D'Angelo ND, Freeman DJ, Herberich BJ, Hong FT, Jackson CL, Jiang J, Lanman BA, Liu L, McCarter JD, Mullady EL, Nishimura N, Pettus LH, Reed AB, Miguel TS, Smith AL, Stec MM, Tadesse S, Tasker A, Aidasani D, Zhu X, Subramanian R, Tamayo NA, Wang L, Whittington DA, Wu B, Wu T, Wurz RP, Yang K, Zalameda L, Zhang N, Hughes PE. Norman MH, et al. Among authors: caenepeel s. J Med Chem. 2012 Sep 13;55(17):7796-816. doi: 10.1021/jm300846z. Epub 2012 Aug 30. J Med Chem. 2012. PMID: 22897589
The imidazo[1,2-a]pyridine ring system as a scaffold for potent dual phosphoinositide-3-kinase (PI3K)/mammalian target of rapamycin (mTOR) inhibitors.
Stec MM, Andrews KL, Bo Y, Caenepeel S, Liao H, McCarter J, Mullady EL, San Miguel T, Subramanian R, Tamayo N, Whittington DA, Wang L, Wu T, Zalameda LP, Zhang N, Hughes PE, Norman MH. Stec MM, et al. Among authors: caenepeel s. Bioorg Med Chem Lett. 2015 Oct 1;25(19):4136-42. doi: 10.1016/j.bmcl.2015.08.016. Epub 2015 Aug 8. Bioorg Med Chem Lett. 2015. PMID: 26298499
Discovery and optimization of a series of benzothiazole phosphoinositide 3-kinase (PI3K)/mammalian target of rapamycin (mTOR) dual inhibitors.
D'Angelo ND, Kim TS, Andrews K, Booker SK, Caenepeel S, Chen K, D'Amico D, Freeman D, Jiang J, Liu L, McCarter JD, San Miguel T, Mullady EL, Schrag M, Subramanian R, Tang J, Wahl RC, Wang L, Whittington DA, Wu T, Xi N, Xu Y, Yakowec P, Yang K, Zalameda LP, Zhang N, Hughes P, Norman MH. D'Angelo ND, et al. Among authors: caenepeel s. J Med Chem. 2011 Mar 24;54(6):1789-811. doi: 10.1021/jm1014605. Epub 2011 Feb 18. J Med Chem. 2011. PMID: 21332118
Phospshoinositide 3-kinase (PI3K)/mammalian target of rapamycin (mTOR) dual inhibitors: discovery and structure-activity relationships of a series of quinoline and quinoxaline derivatives.
Nishimura N, Siegmund A, Liu L, Yang K, Bryan MC, Andrews KL, Bo Y, Booker SK, Caenepeel S, Freeman D, Liao H, McCarter J, Mullady EL, San Miguel T, Subramanian R, Tamayo N, Wang L, Whittington DA, Zalameda L, Zhang N, Hughes PE, Norman MH. Nishimura N, et al. Among authors: caenepeel s. J Med Chem. 2011 Jul 14;54(13):4735-51. doi: 10.1021/jm200386s. Epub 2011 Jun 20. J Med Chem. 2011. PMID: 21612232
32 results