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Page 1
Synthesis, structure-activity relationships, and in vivo efficacy of the novel potent and selective anaplastic lymphoma kinase (ALK) inhibitor 5-chloro-N2-(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)-N4-(2-(isopropylsulfonyl)phenyl)pyrimidine-2,4-diamine (LDK378) currently in phase 1 and phase 2 clinical trials.
Marsilje TH, Pei W, Chen B, Lu W, Uno T, Jin Y, Jiang T, Kim S, Li N, Warmuth M, Sarkisova Y, Sun F, Steffy A, Pferdekamper AC, Li AG, Joseph SB, Kim Y, Liu B, Tuntland T, Cui X, Gray NS, Steensma R, Wan Y, Jiang J, Chopiuk G, Li J, Gordon WP, Richmond W, Johnson K, Chang J, Groessl T, He YQ, Phimister A, Aycinena A, Lee CC, Bursulaya B, Karanewsky DS, Seidel HM, Harris JL, Michellys PY. Marsilje TH, et al. Among authors: tuntland t. J Med Chem. 2013 Jul 25;56(14):5675-90. doi: 10.1021/jm400402q. Epub 2013 Jun 26. J Med Chem. 2013. PMID: 23742252
Arylaminoethyl carbamates as a novel series of potent and selective cathepsin S inhibitors.
Tully DC, Liu H, Chatterjee AK, Alper PB, Williams JA, Roberts MJ, Mutnick D, Woodmansee DH, Hollenbeck T, Gordon P, Chang J, Tuntland T, Tumanut C, Li J, Harris JL, Karanewsky DS. Tully DC, et al. Among authors: tuntland t. Bioorg Med Chem Lett. 2006 Oct 1;16(19):5107-11. doi: 10.1016/j.bmcl.2006.07.032. Epub 2006 Jul 28. Bioorg Med Chem Lett. 2006. PMID: 16876407
Novel tricyclic pyrazolopyrimidines as potent and selective GPR119 agonists.
Azimioara M, Alper P, Cow C, Mutnick D, Nikulin V, Lelais G, Mecom J, McNeill M, Michellys PY, Wang Z, Reding E, Paliotti M, Li J, Bao D, Zoll J, Kim Y, Zimmerman M, Groessl T, Tuntland T, Joseph SB, McNamara P, Seidel HM, Epple R. Azimioara M, et al. Among authors: tuntland t. Bioorg Med Chem Lett. 2014 Dec 1;24(23):5478-83. doi: 10.1016/j.bmcl.2014.10.010. Epub 2014 Oct 13. Bioorg Med Chem Lett. 2014. PMID: 25455488
Design and synthesis of novel selective anaplastic lymphoma kinase inhibitors.
Michellys PY, Chen B, Jiang T, Jin Y, Lu W, Marsilje TH, Pei W, Uno T, Zhu X, Wu B, Nguyen TN, Bursulaya B, Lee C, Li N, Kim S, Tuntland T, Liu B, Sun F, Steffy A, Hood T. Michellys PY, et al. Among authors: tuntland t. Bioorg Med Chem Lett. 2016 Feb 1;26(3):1090-1096. doi: 10.1016/j.bmcl.2015.11.049. Epub 2015 Nov 17. Bioorg Med Chem Lett. 2016. PMID: 26750252
Discovery of structurally novel, potent and orally efficacious GPR119 agonists.
Alper P, Azimioara M, Cow C, Mutnick D, Nikulin V, Michellys PY, Wang Z, Reding E, Paliotti M, Li J, Bao D, Zoll J, Kim Y, Zimmerman M, Groessel T, Tuntland T, Joseph SB, McNamara P, Seidel HM, Epple R. Alper P, et al. Among authors: tuntland t. Bioorg Med Chem Lett. 2014 May 15;24(10):2383-7. doi: 10.1016/j.bmcl.2014.03.023. Epub 2014 Mar 27. Bioorg Med Chem Lett. 2014. PMID: 24751443
Synthesis and SAR of arylaminoethyl amides as noncovalent inhibitors of cathepsin S: P3 cyclic ethers.
Tully DC, Liu H, Chatterjee AK, Alper PB, Epple R, Williams JA, Roberts MJ, Woodmansee DH, Masick BT, Tumanut C, Li J, Spraggon G, Hornsby M, Chang J, Tuntland T, Hollenbeck T, Gordon P, Harris JL, Karanewsky DS. Tully DC, et al. Among authors: tuntland t. Bioorg Med Chem Lett. 2006 Oct 1;16(19):5112-7. doi: 10.1016/j.bmcl.2006.07.033. Epub 2006 Jul 28. Bioorg Med Chem Lett. 2006. PMID: 16876402
Synthesis and SAR of succinamide peptidomimetic inhibitors of cathepsin S.
Chatterjee AK, Liu H, Tully DC, Guo J, Epple R, Russo R, Williams J, Roberts M, Tuntland T, Chang J, Gordon P, Hollenbeck T, Tumanut C, Li J, Harris JL. Chatterjee AK, et al. Among authors: tuntland t. Bioorg Med Chem Lett. 2007 May 15;17(10):2899-903. doi: 10.1016/j.bmcl.2007.02.049. Epub 2007 Feb 27. Bioorg Med Chem Lett. 2007. PMID: 17382545
Discovery and biological evaluation of benzo[a]carbazole-based small molecule agonists of the thrombopoietin (Tpo) receptor.
Alper PB, Marsilje TH, Mutnick D, Lu W, Chatterjee A, Roberts MJ, He Y, Karanewsky DS, Chow D, Lao J, Gerken A, Tuntland T, Liu B, Chang J, Gordon P, Seidel HM, Tian SS. Alper PB, et al. Among authors: tuntland t. Bioorg Med Chem Lett. 2008 Oct 1;18(19):5255-8. doi: 10.1016/j.bmcl.2008.08.068. Epub 2008 Aug 22. Bioorg Med Chem Lett. 2008. PMID: 18778936
55 results