Zobrazeno 1 - 10
of 20
pro vyhledávání: '"Marlena Grynfarb"'
Autor:
Peer B. Jacobson, Lars Öhman, Birgitta Gelius, Marlena Grynfarb, Annika Goos-Nilsson, Richards Steven J, Masha Kalmanovich, Steven Fung, Thomas W. von Geldern, Denise Wilcox, Marie K. Österlund, Phong Nguyen, Jiahong Wang
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 16:6086-6090
A series of potent steroidal glucocorticoid receptor antagonists has been discovered. After conjugation to cholic acid, the compounds retained an affinity for GR in vitro and had modest in vivo efficacy.
Autor:
Todd J. Friends, Arthur M. Doweyko, Johnny Sandberg, Jon J. Hangeland, Denis E. Ryono, Karin Mellstroem, Marlena Grynfarb
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 15:4579-4584
High affinity thyromimetics containing a novel phenyl-naphthylene core are reported. The functionalized core is readily accessible via a Suzuki coupling protocol. Examples of this new class of TR ligands have sub-nanomolar binding affinities for the
Autor:
Phong Nguyen, Sue J. Swanson, Jyoti R. Patel, Jiahong Wang, Annika Goos-Nilsson, J.T. Link, Peer B. Jacobson, Zhenping Tian, Marlena Grynfarb, Jia Du, James M. Schmidt, Brad Zinker, Thomas W von Geldern, Steven Fung, Thomas J Reisch, Denise Wilcox, Gary Rotert, Benjamin C. Lane, Bach Hickman, Bryan Sorensen
Publikováno v:
Journal of Medicinal Chemistry. 48:5295-5304
Much has been learned about the consequences of glucocorticoid receptor antagonism by studying steroidal active antagonists such as RU-38486 (1). In the liver glucocorticoid receptor antagonism suppresses hepatic glucose production decreasing plasma
Autor:
Bo Carlsson, Lars-Göran Bladh, Marlena Grynfarb, Theresa Appelqvist, Konrad F. Koehler, Asa Hedfors, Chris Litten, Johan Malm, Peter Agback
Publikováno v:
Journal of Medicinal Chemistry. 48:3114-3117
Based on the recently described concept of "indirect antagonism" of nuclear receptors, a series of thyroid hormone receptor (TR) antagonists were prepared, in which the outer ring of a thyromimetic was replaced with alkyl chains of variable length an
Autor:
Marlena Grynfarb, Maurice Emery, Jyoti R. Patel, Annika Goos-Nilsson, Bryan K. Sorensen, Susan Swanson, David Arendsen, Gaoquan Li, James T. Link, Bach Nguyen
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 14:4169-4172
The optimization of a series of nonsteroidal glucocorticoid modulators is reported. Potent selective GR ligands that have improved metabolic stability were discovered typified by the subnanomolar acid 12 (GR binding IC 50 = 0.6 nM).
Autor:
Marlena Grynfarb, Maurice Emery, J.T. Link, Noah Tu, Bryan K. Sorensen, Bach Nguyen, Annika Goos-Nilsson
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 14:4179-4183
Bile acid conjugates of a selective nonsteroidal glucocorticoid receptor modulator were prepared and evaluated. Potent GR binding conjugates that showed improved metabolic stability were discovered. However, cellular potency and pharmacokinetics were
Autor:
Anna Bäcksbro-Saeidi, Sandra Gordon, Peter Agback, Bo Carlsson, Konrad F. Koehler, Peter Brandt, Stefan Rehnmark, Theresa Apelqvist, Johan Malm, Mathias Färnegårdh, Gary J. Grover, William Nelson, Marlena Grynfarb
Publikováno v:
Journal of Medicinal Chemistry. 49:6635-6637
A new high-affinity thyroid hormone antagonist 6 with druglike properties was designed and synthesized. The compound behaved as an antagonist in a cell transactivation assay, and in a first in vivo experiment in rats.
Autor:
Johnny Sandberg, Karin Mellström, Mahmoud Rahimi-Ghadim, Denis E. Ryono, Gary J. Grover, Zhang Minsheng, Peter Agback, Neeraj Garg, William N. Washburn, Marlena Grynfarb, Ana Maria Garcia Collazo, Yolanda Caringal, Wei Meng, Robert Paul Brigance, Yi-Lin Li, Stefan Rehnmark, Chris Litten, Johan Malm, Thomas Anders Norin
Publikováno v:
Bioorganicmedicinal chemistry letters. 17(15)
Based on the scaffold of the pharmacologically selective thyromimetic 2b, structurally a close analog to KB-141 (2a), a number of novel N-acylated-α-amino acid derivatives were synthesized and tested in a TR radioligand binding assay as well as in a
Autor:
Bradley J. Backes, Peer B. Jacobson, Phong Nguyen, Thomas W. von Geldern, Gregory Hamilton, Annika Goos-Nilsson, Steven Fung, Denise Wilcox, Marlena Grynfarb, Jiahong Wang
Publikováno v:
Bioorganicmedicinal chemistry letters. 17(1)
Libraries of mifepristone analogs, MP-Acids, were designed and synthesized to increase the chances of identifying GR antagonists that possess liver-selective pharmacological profiles. MP-Acids were uniformly potent GR antagonists in binding and in ce
Autor:
Liu Ye, Ana-Maria Garcia Collazo, Mathias Färnegårdh, Konrad F. Koehler, Karin Mellström, Johnny Sandberg, Harri Ahola, Bolette Husman, Johan Malm, Jan Ljunggren, Marlena Grynfarb, Neeraj Garg
Publikováno v:
Bioorganicmedicinal chemistry letters. 16(5)
Based on the examination of the crystal structure of rat TRbeta complexed with 3,5,3'-triiodo-l-thyronine (2) a novel TRbeta-selective indole derivative 6b was prepared and tested in vitro. This compound was found to be 14 times selective for TRbeta