Literature DB >> 20735001

Nonsteroidal dissociated glucocorticoid agonists containing azaindoles as steroid A-ring mimetics.

Doris Riether1, Christian Harcken, Hossein Razavi, Daniel Kuzmich, Thomas Gilmore, Jörg Bentzien, Edward J Pack, Donald Souza, Richard M Nelson, Alison Kukulka, Tazmeen N Fadra, Ljiljana Zuvela-Jelaska, Josephine Pelletier, Roger Dinallo, Mark Panzenbeck, Carol Torcellini, Gerald H Nabozny, David S Thomson.   

Abstract

Syntheses and structure-activity relationships (SAR) of nonsteroidal glucocorticoid receptor (GR) agonists are described. These compounds contain azaindole moieties as A-ring mimetics and display various degrees of in vitro dissociation between gene transrepression and transactivation. Collagen induced arthritis studies in mouse have demonstrated that in vitro dissociated compounds (R)-16 and (R)-37 have steroid-like anti-inflammatory properties with improved metabolic side effect profiles, such as a reduced increase in body fat and serum insulin levels, compared to steroids.

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Year:  2010        PMID： 20735001     DOI： 10.1021/jm100751q

Source DB:  PubMed          Journal:  J Med Chem        ISSN： 0022-2623            Impact factor:   7.446


  5 in total

1.  Optimization of drug-like properties of nonsteroidal glucocorticoid mimetics and identification of a clinical candidate.

Authors:  Christian Harcken; Doris Riether; Pingrong Liu; Hossein Razavi; Usha Patel; Thomas Lee; Todd Bosanac; Yancey Ward; Mark Ralph; Zhidong Chen; Donald Souza; Richard M Nelson; Alison Kukulka; Tazmeen N Fadra-Khan; Ljiljana Zuvela-Jelaska; Mita Patel; David S Thomson; Gerald H Nabozny
Journal:  ACS Med Chem Lett       Date:  2014-11-20       Impact factor: 4.345

2.  Discovery and structure-activity relationship of novel 2,3-dihydrobenzofuran-7-carboxamide and 2,3-dihydrobenzofuran-3(2H)-one-7-carboxamide derivatives as poly(ADP-ribose)polymerase-1 inhibitors.

Authors:  Maulik R Patel; Aaditya Bhatt; Jamin D Steffen; Adel Chergui; Junko Murai; Yves Pommier; John M Pascal; Louis D Trombetta; Frank R Fronczek; Tanaji T Talele
Journal:  J Med Chem       Date:  2014-06-25       Impact factor: 7.446

3.  Exploring 6-Azaindole and 7-Azaindole Rings for Developing Cannabinoid Receptor 1 Allosteric Modulators.

Authors:  Sri Sujana Immadi; Rachel Dopart; Zhixing Wu; Boqiao Fu; Debra A Kendall; Dai Lu
Journal:  Cannabis Cannabinoid Res       Date:  2018-12-10

4.  Org 214007-0: a novel non-steroidal selective glucocorticoid receptor modulator with full anti-inflammatory properties and improved therapeutic index.

Authors:  Marie-José C van Lierop; Wynand Alkema; Anke J Laskewitz; Rein Dijkema; Hans M van der Maaden; Martin J Smit; Ralf Plate; Paolo G M Conti; Christan G J M Jans; C Marco Timmers; Constant A A van Boeckel; Scott J Lusher; Ross McGuire; Rene C van Schaik; Jacob de Vlieg; Ruben L Smeets; Claudia L Hofstra; Annemieke M H Boots; Marcel van Duin; Benno A Ingelse; Willem G E J Schoonen; Aldo Grefhorst; Theo H van Dijk; Folkert Kuipers; Wim H A Dokter
Journal:  PLoS One       Date:  2012-11-12       Impact factor: 3.240

Review 5.  Efficacy and safety of selective glucocorticoid receptor modulators in comparison to glucocorticoids in arthritis, a systematic review.

Authors:  M Safy; M J H de Hair; J W G Jacobs; F Buttgereit; M C Kraan; J M van Laar
Journal:  PLoS One       Date:  2017-12-21       Impact factor: 3.240
  5 in total

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