Literature DB >> 18579373

Discovery of novel hydroxy-thiazoles as HIF-alpha prolyl hydroxylase inhibitors: SAR, synthesis, and modeling evaluation.

Christopher M Tegley1, Vellarkad N Viswanadhan, Kaustav Biswas, Michael J Frohn, Tanya A N Peterkin, Catherine Chang, Roland W Bürli, Jennifer H Dao, Henrike Veith, Norma Rogers, Sean C Yoder, Gloria Biddlecome, Philip Tagari, Jennifer R Allen, Randall W Hungate.   

Abstract

Inhibition of the PHD2 enzyme has been associated with increased red blood cell levels. From a screening hit, a series of novel hydroxyl-thiazoles were developed as potent PHD2 inhibitors.

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Year:  2008        PMID： 18579373     DOI： 10.1016/j.bmcl.2008.06.031

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


  11 in total

1.  Benzimidazole-2-pyrazole HIF Prolyl 4-Hydroxylase Inhibitors as Oral Erythropoietin Secretagogues.

Authors:  Mark D Rosen; Hariharan Venkatesan; Hillary M Peltier; Scott D Bembenek; Kimon C Kanelakis; Lucy X Zhao; Barry E Leonard; Frances M Hocutt; Xiaodong Wu; Heather L Palomino; Theresa I Brondstetter; Peter V Haugh; Laurence Cagnon; Wen Yan; Lisa A Liotta; Andrew Young; Tara Mirzadegan; Nigel P Shankley; Terrance D Barrett; Michael H Rabinowitz
Journal:  ACS Med Chem Lett       Date:  2010-10-05       Impact factor: 4.345

Review 2.  Hypoxia-inducible factor prolyl hydroxylase inhibition: robust new target or another big bust for stroke therapeutics?

Authors:  Saravanan S Karuppagounder; Rajiv R Ratan
Journal:  J Cereb Blood Flow Metab       Date:  2012-03-14       Impact factor: 6.200

3.  Utilization of an in vivo reporter for high throughput identification of branched small molecule regulators of hypoxic adaptation.

Authors:  Natalya A Smirnova; Ilay Rakhman; Natalia Moroz; Manuela Basso; Jimmy Payappilly; Sergey Kazakov; Francisco Hernandez-Guzman; Irina N Gaisina; Alan P Kozikowski; Rajiv R Ratan; Irina G Gazaryan
Journal:  Chem Biol       Date:  2010-04-23

4.  Synthesis, antiproliferative activity and possible mechanism of action of novel 2-acetamidobenzamides bearing the 2-phenoxy functionality.

Authors:  Demetrio Raffa; Benedetta Maggio; Fabiana Plescia; Stella Cascioferro; Maria Valeria Raimondi; Gabriella Cancemi; Antonella D'Anneo; Marianna Lauricella; Maria Grazia Cusimano; Ruoli Bai; Ernest Hamel; Giuseppe Daidone
Journal:  Bioorg Med Chem       Date:  2015-08-28       Impact factor: 3.641

5.  Selective EGLN Inhibition Enables Ablative Radiotherapy and Improves Survival in Unresectable Pancreatic Cancer.

Authors:  Tara N Fujimoto; Lauren E Colbert; Yanqing Huang; Jessica M Molkentine; Amit Deorukhkar; Laura Baseler; Meifang Yu; Daniel Lin; Sonal Gupta; Peter K Cabeceiras; Charles V Kingsley; Ramesh C Tailor; Gabriel O Sawakuchi; Eugene J Koay; Helen Piwnica-Worms; Anirban Maitra; Cullen M Taniguchi
Journal:  Cancer Res       Date:  2019-05-01       Impact factor: 12.701

6.  Reporter ligand NMR screening method for 2-oxoglutarate oxygenase inhibitors.

Authors:  Ivanhoe K H Leung; Marina Demetriades; Adam P Hardy; Clarisse Lejeune; Tristan J Smart; Andrea Szöllössi; Akane Kawamura; Christopher J Schofield; Timothy D W Claridge
Journal:  J Med Chem       Date:  2013-01-04       Impact factor: 7.446

7.  Effect of proline analogues on activity of human prolyl hydroxylase and the regulation of HIF signal transduction pathway.

Authors:  Xiaoyan Ma; Xiaoxin Wang; Jing Cao; Zhirong Geng; Zhilin Wang
Journal:  PLoS One       Date:  2014-04-22       Impact factor: 3.240

8.  Dual-action inhibitors of HIF prolyl hydroxylases that induce binding of a second iron ion.

Authors:  Kar Kheng Yeoh; Mun Chiang Chan; Armin Thalhammer; Marina Demetriades; Rasheduzzaman Chowdhury; Ya-Min Tian; Ineke Stolze; Luke A McNeill; Myung Kyu Lee; Esther C Y Woon; Mukram M Mackeen; Akane Kawamura; Peter J Ratcliffe; Jasmin Mecinović; Christopher J Schofield
Journal:  Org Biomol Chem       Date:  2012-11-15       Impact factor: 3.876

9.  Competitive HIF Prolyl Hydroxylase Inhibitors Show Protection against Oxidative Stress by a Mechanism Partially Dependent on Glycolysis.

Authors:  Ann-Louise Bergström; Karina Fog; Thomas Nikolaj Sager; Anne Techau Bruun; Kenneth Thirstrup
Journal:  ISRN Neurosci       Date:  2013-12-05

10.  Tuning the Transcriptional Response to Hypoxia by Inhibiting Hypoxia-inducible Factor (HIF) Prolyl and Asparaginyl Hydroxylases.

Authors:  Mun Chiang Chan; Nicholas E Ilott; Johannes Schödel; David Sims; Anthony Tumber; Kerstin Lippl; David R Mole; Christopher W Pugh; Peter J Ratcliffe; Chris P Ponting; Christopher J Schofield
Journal:  J Biol Chem       Date:  2016-08-08       Impact factor: 5.157
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