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Page 1
Structure guided design of a series of selective pyrrolopyrimidinone MARK inhibitors.
Katz JD, Haidle A, Childers KK, Zabierek AA, Jewell JP, Hou Y, Altman MD, Szewczak A, Chen D, Harsch A, Hayashi M, Warren L, Hutton M, Nuthall H, Su HP, Munshi S, Stanton MG, Davies IW, Munoz B, Northrup A. Katz JD, et al. Among authors: nuthall h. Bioorg Med Chem Lett. 2017 Jan 1;27(1):114-120. doi: 10.1016/j.bmcl.2016.08.068. Epub 2016 Oct 22. Bioorg Med Chem Lett. 2017. PMID: 27816515
Optimization of microtubule affinity regulating kinase (MARK) inhibitors with improved physical properties.
Sloman DL, Noucti N, Altman MD, Chen D, Mislak AC, Szewczak A, Hayashi M, Warren L, Dellovade T, Wu Z, Marcus J, Walker D, Su HP, Edavettal SC, Munshi S, Hutton M, Nuthall H, Stanton MG. Sloman DL, et al. Among authors: nuthall h. Bioorg Med Chem Lett. 2016 Sep 1;26(17):4362-6. doi: 10.1016/j.bmcl.2016.02.003. Epub 2016 Feb 6. Bioorg Med Chem Lett. 2016. PMID: 27491711
MARK inhibitors: Declaring a No-Go decision on a chemical series based on extensive DMPK experimentation.
Haidle AM, Childers KK, Zabierek AA, Katz JD, Jewell JP, Hou Y, Altman MD, Szewczak A, Chen D, Harsch A, Hayashi M, Warren L, Hutton M, Nuthall H, Stanton MG, Davies IW, Munoz B, Northrup A. Haidle AM, et al. Among authors: nuthall h. Bioorg Med Chem Lett. 2017 Jan 1;27(1):109-113. doi: 10.1016/j.bmcl.2016.08.066. Epub 2016 Aug 25. Bioorg Med Chem Lett. 2017. PMID: 27894874
Triazoloamides as potent γ-secretase modulators with reduced hERG liability.
Fischer C, Zultanski SL, Zhou H, Methot JL, Shah S, Nuthall H, Hughes BL, Smotrov N, Hill A, Szewczak AA, Moxham CM, Bays N, Middleton RE, Munoz B, Shearman MS. Fischer C, et al. Among authors: nuthall h. Bioorg Med Chem Lett. 2012 May 1;22(9):3140-6. doi: 10.1016/j.bmcl.2012.03.054. Epub 2012 Mar 21. Bioorg Med Chem Lett. 2012. PMID: 22497762
Triazoles as γ-secretase modulators.
Fischer C, Zultanski SL, Zhou H, Methot JL, Brown WC, Mampreian DM, Schell AJ, Shah S, Nuthall H, Hughes BL, Smotrov N, Kenific CM, Cruz JC, Walker D, Bouthillette M, Nikov GN, Savage DF, Jeliazkova-Mecheva VV, Diaz D, Szewczak AA, Bays N, Middleton RE, Munoz B, Shearman MS. Fischer C, et al. Among authors: nuthall h. Bioorg Med Chem Lett. 2011 Jul 1;21(13):4083-7. doi: 10.1016/j.bmcl.2011.04.089. Epub 2011 May 4. Bioorg Med Chem Lett. 2011. PMID: 21616665
Potent benzoazepinone γ-secretase modulators with improved bioavailability.
Methot JL, Fischer C, Li C, Rivkin A, Ahearn SP, Brown WC, Kattar S, Kelley E, Mampreian DM, Schell A, Rosenau A, Zhou H, Ball R, Deshmukh SV, Jeliazkova-Mecheva VV, Diaz D, Moy LY, Kenific CM, Moxham C, Shah S, Nuthall H, Szewczak AA, Hill A, Hughes B, Smotrov N, Munoz B, Miller TA, Shearman MS. Methot JL, et al. Among authors: nuthall h. Bioorg Med Chem Lett. 2015 Sep 1;25(17):3495-500. doi: 10.1016/j.bmcl.2015.06.032. Epub 2015 Jun 15. Bioorg Med Chem Lett. 2015. PMID: 26142947
Protease-activated receptor 2 activation induces behavioural changes associated with depression-like behaviour through microglial-independent modulation of inflammatory cytokines.
Moudio S, Willis A, Pytka K, Abulkassim R, Brett RR, Webster JF, Wozny C, Barbour M, Jiang HR, Watson DG, van Kralingen JC, MacKenzie SM, Daniels M, McColl BW, Sossick S, Nuthall HN, Bushell TJ. Moudio S, et al. Among authors: nuthall hn. Psychopharmacology (Berl). 2022 Jan;239(1):229-242. doi: 10.1007/s00213-021-06040-1. Epub 2021 Dec 9. Psychopharmacology (Berl). 2022. PMID: 34888704 Free PMC article.
28 results