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Page 1
A new series of estrogen receptor modulators that display selectivity for estrogen receptor beta.
Henke BR, Consler TG, Go N, Hale RL, Hohman DR, Jones SA, Lu AT, Moore LB, Moore JT, Orband-Miller LA, Robinett RG, Shearin J, Spearing PK, Stewart EL, Turnbull PS, Weaver SL, Williams SP, Wisely GB, Lambert MH. Henke BR, et al. Among authors: spearing pk. J Med Chem. 2002 Dec 5;45(25):5492-505. doi: 10.1021/jm020291h. J Med Chem. 2002. PMID: 12459017
Conformationally constrained farnesoid X receptor (FXR) agonists: Naphthoic acid-based analogs of GW 4064.
Akwabi-Ameyaw A, Bass JY, Caldwell RD, Caravella JA, Chen L, Creech KL, Deaton DN, Jones SA, Kaldor I, Liu Y, Madauss KP, Marr HB, McFadyen RB, Miller AB, Navas F III, Parks DJ, Spearing PK, Todd D, Williams SP, Wisely GB. Akwabi-Ameyaw A, et al. Among authors: spearing pk. Bioorg Med Chem Lett. 2008 Aug 1;18(15):4339-43. doi: 10.1016/j.bmcl.2008.06.073. Epub 2008 Jun 28. Bioorg Med Chem Lett. 2008. PMID: 18621523
FXR agonist activity of conformationally constrained analogs of GW 4064.
Akwabi-Ameyaw A, Bass JY, Caldwell RD, Caravella JA, Chen L, Creech KL, Deaton DN, Madauss KP, Marr HB, McFadyen RB, Miller AB, Navas F 3rd, Parks DJ, Spearing PK, Todd D, Williams SP, Bruce Wisely G. Akwabi-Ameyaw A, et al. Among authors: spearing pk. Bioorg Med Chem Lett. 2009 Aug 15;19(16):4733-9. doi: 10.1016/j.bmcl.2009.06.062. Epub 2009 Jun 21. Bioorg Med Chem Lett. 2009. PMID: 19586769
Discovery of tertiary sulfonamides as potent liver X receptor antagonists.
Zuercher WJ, Buckholz RG, Campobasso N, Collins JL, Galardi CM, Gampe RT, Hyatt SM, Merrihew SL, Moore JT, Oplinger JA, Reid PR, Spearing PK, Stanley TB, Stewart EL, Willson TM. Zuercher WJ, et al. Among authors: spearing pk. J Med Chem. 2010 Apr 22;53(8):3412-6. doi: 10.1021/jm901797p. J Med Chem. 2010. PMID: 20345102
Conformationally constrained farnesoid X receptor (FXR) agonists: heteroaryl replacements of the naphthalene.
Bass JY, Caravella JA, Chen L, Creech KL, Deaton DN, Madauss KP, Marr HB, McFadyen RB, Miller AB, Mills WY, Navas F 3rd, Parks DJ, Smalley TL Jr, Spearing PK, Todd D, Williams SP, Wisely GB. Bass JY, et al. Among authors: spearing pk. Bioorg Med Chem Lett. 2011 Feb 15;21(4):1206-13. doi: 10.1016/j.bmcl.2010.12.089. Epub 2010 Dec 23. Bioorg Med Chem Lett. 2011. PMID: 21256005
Conformationally constrained farnesoid X receptor (FXR) agonists: alternative replacements of the stilbene.
Akwabi-Ameyaw A, Caravella JA, Chen L, Creech KL, Deaton DN, Madauss KP, Marr HB, Miller AB, Navas F 3rd, Parks DJ, Spearing PK, Todd D, Williams SP, Wisely GB. Akwabi-Ameyaw A, et al. Among authors: spearing pk. Bioorg Med Chem Lett. 2011 Oct 15;21(20):6154-60. doi: 10.1016/j.bmcl.2011.08.034. Epub 2011 Aug 11. Bioorg Med Chem Lett. 2011. PMID: 21890356
Discovery of a novel, CNS penetrant M4 PAM chemotype based on a 6-fluoro-4-(piperidin-1-yl)quinoline-3-carbonitrile core.
Bewley BR, Spearing PK, Weiner RL, Luscombe VB, Zhan X, Chang S, Cho HP, Rodriguez AL, Niswender CM, Conn PJ, Bridges TM, Engers DW, Lindsley CW. Bewley BR, et al. Among authors: spearing pk. Bioorg Med Chem Lett. 2017 Sep 15;27(18):4274-4279. doi: 10.1016/j.bmcl.2017.08.043. Epub 2017 Aug 20. Bioorg Med Chem Lett. 2017. PMID: 28866269 Free PMC article.
Synthesis and SAR of a series of mGlu7 NAMs based on an ethyl-8-methoxy-4-(4-phenylpiperazin-1-yl)quinoline carboxylate core.
Kalbfleisch JJ, Reed CW, Park C, Spearing PK, Quitalig MC, Jenkins MT, Rodriguez AL, Blobaum AL, Conn PJ, Niswender CM, Lindsley CW. Kalbfleisch JJ, et al. Among authors: spearing pk. Bioorg Med Chem Lett. 2020 Nov 15;30(22):127529. doi: 10.1016/j.bmcl.2020.127529. Epub 2020 Sep 2. Bioorg Med Chem Lett. 2020. PMID: 32890686 Free PMC article.
13 results