Zobrazeno 1 - 4
of 4
pro vyhledávání: '"Adwoa Akwabi-Ameyaw"'
Autor:
Harry B. Marr, Kevin P. Madauss, Jonathan Y. Bass, Shawn P. Williams, Dan Todd, Paul Kenneth Spearing, Adwoa Akwabi-Ameyaw, Lihong Chen, Robert B. McFadyen, Justin A. Caravella, Derek J. Parks, Frank Navas, David N. Deaton, Katrina L. Creech, G. Bruce Wisely, Richard Dana Caldwell, Aaron B. Miller
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:4733-4739
Two series of conformationally constrained analogs of the FXR agonist GW 4064 1 were prepared. Replacement of the metabolically labile stilbene with either benzothiophene or naphthalene rings led to the identification of potent full agonists 2a and 2
Autor:
Lihong Chen, Jonathan Y. Bass, David N. Deaton, Aaron B. Miller, Justin A. Caravella, Istvan Kaldor, Robert B. McFadyen, Stacey A. Jones, Dan Todd, Paul Kenneth Spearing, Kevin P. Madauss, Adwoa Akwabi-Ameyaw, Derek J. Parks, Richard Dana Caldwell, Frank Navas, Yaping Liu, Katrina L. Creech, G. Bruce Wisely, Harry B. Marr, Shawn P. Williams
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:4339-4343
Starting from the known FXR agonist GW 4064 1a, a series of stilbene replacements were prepared. The 6-substituted 1-naphthoic acid 1b was an equipotent FXR agonist with improved developability parameters relative to 1a. Analog 1b also reduced the se
Autor:
Dennis Heyer, Lisa A. Orband-Miller, Frank Navas, David W. Gray, Shawn P. Williams, Adwoa Akwabi-Ameyaw, Jean Shearin, Jing Fang, Subba Reddy Katamreddy, Aaron B. Miller, Jonathan E. Britton
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:5075-5077
A series of estrogen receptor ligands based on a 3-alkyl naphthalene scaffold was synthesized using an intramolecular enolate-alkyne cycloaromatization as the key step. Several of these compounds bearing a C6-OH group were shown to be high affinity l
Autor:
Aaron B. Miller, Harry B. Marr, Katrina L. Creech, G. Bruce Wisely, Shawn P. Williams, Adwoa Akwabi-Ameyaw, Lihong Chen, David N. Deaton, Justin A. Caravella, Paul Kenneth Spearing, Kevin P. Madauss, Derek J. Parks, Frank Navas, Dan Todd
Publikováno v:
Bioorganicmedicinal chemistry letters. 21(20)
To further explore the optimum placement of the acid moiety in conformationally constrained analogs of GW 4064 1a, a series of stilbene replacements were prepared. The benzothiophene 1f and the indole 1g display the optimal orientation of the carboxy