Literature DB >> 18374567

Synthesis of small molecule inhibitors of the orphan nuclear receptor steroidogenic factor-1 (NR5A1) based on isoquinolinone scaffolds.

Joshua Roth1, Franck Madoux, Peter Hodder, William R Roush.   

Abstract

Three synthetic routes were developed for structure-activity relationship (SAR) studies of HTS-derived isoquinolinone inhibitor probes for the orphan nuclear receptor steroidogenic factor-1 (NR5A1). Among the new analogs reported herein, 31 and 32 have improved potency, lower cellular toxicity, and improved selectivity compared to the initial HTS-derived leads 1 and 2.

Entities:  

Mesh：

Substances：

Year:  2008        PMID： 18374567      PMCID： PMC2592603          DOI： 10.1016/j.bmcl.2008.03.027

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  19 in total

Review 1.  The nuclear receptor superfamily and drug discovery.

Authors:  John T Moore; Jon L Collins; Kenneth H Pearce
Journal:  ChemMedChem       Date:  2006-05       Impact factor: 3.466

2.  GAL4-VP16 is an unusually potent transcriptional activator.

Authors:  I Sadowski; J Ma; S Triezenberg; M Ptashne
Journal:  Nature       Date:  1988-10-06       Impact factor: 49.962

3.  Knockout mice lacking steroidogenic factor 1 are a novel genetic model of hypothalamic obesity.

Authors:  Gregor Majdic; Morag Young; Elise Gomez-Sanchez; Paul Anderson; Lidia S Szczepaniak; Robert L Dobbins; J Denis McGarry; Keith L Parker
Journal:  Endocrinology       Date:  2002-02       Impact factor: 4.736

Review 4.  Steroidogenic factor 1: an essential mediator of endocrine development.

Authors:  Keith L Parker; Douglas A Rice; Deepak S Lala; Yayoi Ikeda; Xunrong Luo; Margaret Wong; Marit Bakke; Liping Zhao; Claudia Frigeri; Neil A Hanley; Nancy Stallings; Bernard P Schimmer
Journal:  Recent Prog Horm Res       Date:  2002

5.  Increased steroidogenic factor-1 dosage triggers adrenocortical cell proliferation and cancer.

Authors:  Mabrouka Doghman; Tatiana Karpova; Giovanna Assis Rodrigues; Malika Arhatte; Juliana De Moura; Luciane R Cavalli; Virginie Virolle; Pascal Barbry; Gerard P Zambetti; Bonald C Figueiredo; Leslie L Heckert; Enzo Lalli
Journal:  Mol Endocrinol       Date:  2007-08-30

6.  The use of ATP bioluminescence as a measure of cell proliferation and cytotoxicity.

Authors:  S P Crouch; R Kozlowski; K J Slater; J Fletcher
Journal:  J Immunol Methods       Date:  1993-03-15       Impact factor: 2.303

7.  Potent, selective and cell penetrant inhibitors of SF-1 by functional ultra-high-throughput screening.

Authors:  Franck Madoux; Xiaolin Li; Peter Chase; Gina Zastrow; Michael D Cameron; Juliana J Conkright; Patrick R Griffin; Scott Thacher; Peter Hodder
Journal:  Mol Pharmacol       Date:  2008-03-11       Impact factor: 4.436

Review 8.  Tissue-specific knockouts of steroidogenic factor 1.

Authors:  Liping Zhao; Marit Bakke; Neil A Hanley; Gregor Majdic; Nancy R Stallings; Pancharatnam Jeyasuria; Keith L Parker
Journal:  Mol Cell Endocrinol       Date:  2004-02-27       Impact factor: 4.102

9.  Identification of the first synthetic steroidogenic factor 1 inverse agonists: pharmacological modulation of steroidogenic enzymes.

Authors:  Andria L Del Tredici; Carsten B Andersen; Erika A Currier; Steven R Ohrmund; Luke C Fairbain; Birgitte W Lund; Norman Nash; Roger Olsson; Fabrice Piu
Journal:  Mol Pharmacol       Date:  2007-11-30       Impact factor: 4.436

10.  SF-1 a key player in the development and differentiation of steroidogenic tissues.

Authors:  Pierre Val; Anne-Marie Lefrançois-Martinez; Georges Veyssière; Antoine Martinez
Journal:  Nucl Recept       Date:  2003-09-18
View more
  8 in total

Review 1.  The dynamics of nuclear receptors and nuclear receptor coregulators in the pathogenesis of endometriosis.

Authors:  Sang Jun Han; Bert W O'Malley
Journal:  Hum Reprod Update       Date:  2014-03-14       Impact factor: 15.610

2.  Identification of a novel non-retinoid pan inverse agonist of the retinoic acid receptors.

Authors:  Scott A Busby; Naresh Kumar; Dana S Kuruvilla; Monica A Istrate; Juliana J Conkright; Yongjun Wang; Theodore M Kamenecka; Michael D Cameron; William R Roush; Thomas P Burris; Patrick R Griffin
Journal:  ACS Chem Biol       Date:  2011-03-17       Impact factor: 5.100

3.  Small molecule agonists of the orphan nuclear receptors steroidogenic factor-1 (SF-1, NR5A1) and liver receptor homologue-1 (LRH-1, NR5A2).

Authors:  Richard J Whitby; Jozef Stec; Raymond D Blind; Sally Dixon; Lisa M Leesnitzer; Lisa A Orband-Miller; Shawn P Williams; Timothy M Willson; Robert Xu; William J Zuercher; Fang Cai; Holly A Ingraham
Journal:  J Med Chem       Date:  2011-03-10       Impact factor: 7.446

Review 4.  Phospholipid--driven gene regulation.

Authors:  Paul M Musille; Jeffrey A Kohn; Eric A Ortlund
Journal:  FEBS Lett       Date:  2013-01-16       Impact factor: 4.124

5.  Solution-phase synthesis of a diverse isocoumarin library.

Authors:  Sujata Roy; Sudipta Roy; Benjamin Neuenswander; David Hill; Richard C Larock
Journal:  J Comb Chem       Date:  2009 Nov-Dec

6.  Inhibition of adrenocortical carcinoma cell proliferation by steroidogenic factor-1 inverse agonists.

Authors:  Mabrouka Doghman; Julie Cazareth; Dominique Douguet; Franck Madoux; Peter Hodder; Enzo Lalli
Journal:  J Clin Endocrinol Metab       Date:  2009-03-24       Impact factor: 5.958

7.  Zinc oxide nanoparticles catalyzed condensation reaction of isocoumarins and 1,7-heptadiamine in the formation of bis-isoquinolinones.

Authors:  Varadhan Krishnakumar; Kesarla Mohan Kumar; Badal Kumar Mandal; Fazlur-Rahman Nawaz Khan
Journal:  ScientificWorldJournal       Date:  2012-03-12

8.  Molecular markers of prognosis in canine cortisol-secreting adrenocortical tumours.

Authors:  Karin Sanders; Gerjanne J van Staalduinen; Maarten C M Uijens; Jan A Mol; Erik Teske; Adri Slob; Jan Willem Hesselink; Hans S Kooistra; Sara Galac
Journal:  Vet Comp Oncol       Date:  2019-08-04       Impact factor: 2.613
  8 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.