Literature DB >> 16931007

Structure-based design, synthesis, and SAR evaluation of a new series of 8-hydroxyquinolines as HIF-1alpha prolyl hydroxylase inhibitors.

Namal C Warshakoon1, Shengde Wu, Angelique Boyer, Richard Kawamoto, Justin Sheville, Sean Renock, Kevin Xu, Matthew Pokross, Songtao Zhou, Carol Winter, Richard Walter, Marlene Mekel, Artem G Evdokimov.   

Abstract

A new series of potent 8-hydroxyquinolines was designed based on the newly resolved X-ray crystal structure of EGLN-1. Both alkyl and aryl 8-hydroxyquinoline-7-carboxyamides were good HIF-1alpha prolyl hydroxylase (EGLN) inhibitors. In subsequent VEGF induction assays, these exhibited potent VEGF activity. In addition, this class of compounds did show the ability to stabilize HIF-1alpha.

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Year:  2006        PMID： 16931007     DOI： 10.1016/j.bmcl.2006.08.040

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


  19 in total

Review 1.  Cellular oxygen sensing in health and disease.

Authors:  David R Mole; Peter J Ratcliffe
Journal:  Pediatr Nephrol       Date:  2007-10-23       Impact factor: 3.714

2.  High-throughput screening for inhibitors of Mycobacterium tuberculosis H37Rv.

Authors:  Subramaniam Ananthan; Ellen R Faaleolea; Robert C Goldman; Judith V Hobrath; Cecil D Kwong; Barbara E Laughon; Joseph A Maddry; Alka Mehta; Lynn Rasmussen; Robert C Reynolds; John A Secrist; Nice Shindo; Dustin N Showe; Melinda I Sosa; William J Suling; E Lucile White
Journal:  Tuberculosis (Edinb)       Date:  2009-09-15       Impact factor: 3.131

3.  Synthesis of a FTO inhibitor with anticonvulsant activity.

Authors:  Guanqun Zheng; Thomas Cox; Leah Tribbey; Gloria Z Wang; Paulina Iacoban; Matthew E Booher; Gregory J Gabriel; Lu Zhou; Nancy Bae; Joie Rowles; Chuan He; Mark J Olsen
Journal:  ACS Chem Neurosci       Date:  2014-06-05       Impact factor: 4.418

4.  Affinity-Based Fluorescence Polarization Assay for High-Throughput Screening of Prolyl Hydroxylase 2 Inhibitors.

Authors:  Yonghua Lei; Tianhan Hu; Xingsen Wu; Yue Wu; Qichao Bao; Lianshan Zhang; Hua Xia; Haopeng Sun; Qidong You; Xiaojin Zhang
Journal:  ACS Med Chem Lett       Date:  2015-11-09       Impact factor: 4.345

5.  Ab initio structural modeling of and experimental validation for Chlamydia trachomatis protein CT296 reveal structural similarity to Fe(II) 2-oxoglutarate-dependent enzymes.

Authors:  Kyle E Kemege; John M Hickey; Scott Lovell; Kevin P Battaile; Yang Zhang; P Scott Hefty
Journal:  J Bacteriol       Date:  2011-09-30       Impact factor: 3.490

6.  Screening chelating inhibitors of HIF-prolyl hydroxylase domain 2 (PHD2) and factor inhibiting HIF (FIH).

Authors:  Shannon C Flagg; Cristina B Martin; Cornelius Y Taabazuing; Breanne E Holmes; Michael J Knapp
Journal:  J Inorg Biochem       Date:  2012-03-17       Impact factor: 4.155

7.  Discovery of a new molecular probe ML228: an activator of the hypoxia inducible factor (HIF) pathway.

Authors:  Jimmy R Theriault; Andrew S Felts; Brittney S Bates; Jose R Perez; Michelle Palmer; Shawn R Gilbert; Eric S Dawson; Julie L Engers; Craig W Lindsley; Kyle A Emmitte
Journal:  Bioorg Med Chem Lett       Date:  2011-11-28       Impact factor: 2.823

8.  Gas phase reaction of substituted isoquinolines to carboxylic acids in ion trap and triple quadrupole mass spectrometers after electrospray ionization and collision-induced dissociation.

Authors:  Mario Thevis; Maxie Kohler; Nils Schlörer; Wilhelm Schänzer
Journal:  J Am Soc Mass Spectrom       Date:  2007-11-09       Impact factor: 3.109

9.  Unusual mass spectrometric dissociation pathway of protonated isoquinoline-3-carboxamides due to multiple reversible water adduct formation in the gas phase.

Authors:  Simon Beuck; Tobias Schwabe; Stefan Grimme; Nils Schlörer; Matthias Kamber; Wilhelm Schänzer; Mario Thevis
Journal:  J Am Soc Mass Spectrom       Date:  2009-08-07       Impact factor: 3.109

Review 10.  Inhibition of oxygen sensors as a therapeutic strategy for ischaemic and inflammatory disease.

Authors:  Peter Fraisl; Julián Aragonés; Peter Carmeliet
Journal:  Nat Rev Drug Discov       Date:  2009-01-23       Impact factor: 84.694
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