Discovery of 2-amino-3-amido-5-aryl-pyridines as highly potent, orally bioavailable, and efficacious PERK kinase inhibitors

Calvo, Veronica; Surguladze, David; Li, An-Hu; Surman, Matthew D.; Malibhatla, Srikanth; Bandaru, Madhavarao; Jonnalagadda, Suresh Krishna; Adarasandi, Ravi; Velmala, Madhusudhan; Singireddi, Durga Rama Prasad; Velpuri, Mahendar; Nareddy, Bhaskar Reddy; Sastry, Visweswara; Mandati, Chiranjeevi; Guguloth, Rambabu; Siddiqui, Shapi; Patil, Basanagoud S.; Chad, Elena; Wolfley, Jennifer; Gasparek, Jennifer; Feldman, Kirsten; Betzenhauser, Matthew; Wiens, Brent; Koszelak-Rosenblum, Mary; Zhu, Guangyu; Du, Hongwen; Rigby, Alan C.; Mulvihill, Mark J.

doi:10.1016/j.bmcl.2021.128058

Discovery of 2-amino-3-amido-5-aryl-pyridines as highly potent, orally bioavailable, and efficacious PERK kinase inhibitors

Journal Article · Thu Jul 01 00:00:00 EDT 2021 · Bioorganic and Medicinal Chemistry Letters

DOI:https://doi.org/10.1016/j.bmcl.2021.128058· OSTI ID:1786393

Calvo, Veronica; Surguladze, David; ; Surman, Matthew D.; Malibhatla, Srikanth; Bandaru, Madhavarao; Jonnalagadda, Suresh Krishna; Adarasandi, Ravi; Velmala, Madhusudhan; Singireddi, Durga Rama Prasad; Velpuri, Mahendar; Nareddy, Bhaskar Reddy; Sastry, Visweswara; Mandati, Chiranjeevi; Guguloth, Rambabu; Siddiqui, Shapi; Patil, Basanagoud S.; Chad, Elena; Wolfley, Jennifer; Gasparek, Jennifer more »

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Sponsoring Organization:: USDOE

Grant/Contract Number:: AC02-06CH11357

OSTI ID:: 1786393

Alternate ID(s):: OSTI ID: 1832564
OSTI ID: 1836760

Journal Information:: Bioorganic and Medicinal Chemistry Letters, Journal Name: Bioorganic and Medicinal Chemistry Letters Journal Issue: C Vol. 43; ISSN 0960-894X

Publisher:: ElsevierCopyright Statement

Country of Publication:: United Kingdom

Language:: English

References (15)

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When PERK inhibitors turn out to be new potent RIPK1 inhibitors: critical issues on the specificity and use of GSK2606414 and GSK2656157 Rojas-Rivera, Diego; Delvaeye, Tinneke; Roelandt, Ria Cell Death & Differentiation, Vol. 24, Issue 6 https://doi.org/10.1038/cdd.2017.58	journal	April 2017
Signal integration in the endoplasmic reticulum unfolded protein response Ron, David; Walter, Peter Nature Reviews Molecular Cell Biology, Vol. 8, Issue 7 https://doi.org/10.1038/nrm2199	journal	July 2007
Protein kinase R(PKR)–like endoplasmic reticulum kinase (PERK) inhibitors: a patent review (2010-2015) Axten, Jeffrey M. Expert Opinion on Therapeutic Patents, Vol. 27, Issue 1 https://doi.org/10.1080/13543776.2017.1238072	journal	September 2016
Activation-dependent substrate recruitment by the eukaryotic translation initiation factor 2 kinase PERK Marciniak, Stefan J.; Garcia-Bonilla, Lidia; Hu, Junjie Journal of Cell Biology, Vol. 172, Issue 2 https://doi.org/10.1083/jcb.200508099	journal	January 2006
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Identification and Characterization of Pancreatic Eukaryotic Initiation Factor 2 α-Subunit Kinase, PEK, Involved in Translational Control Shi, Yuguang; Vattem, Krishna M.; Sood, Ruchira Molecular and Cellular Biology, Vol. 18, Issue 12 https://doi.org/10.1128/MCB.18.12.7499	journal	December 1998
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