Literature DB >> 22310227

5-Aryl-4-carboxamide-1,3-oxazoles: potent and selective GSK-3 inhibitors.

Gabriella Gentile1, Giancarlo Merlo, Alfonso Pozzan, Giovanni Bernasconi, Benjamin Bax, Paul Bamborough, Angela Bridges, Paul Carter, Margarete Neu, Gang Yao, Caroline Brough, Geoffrey Cutler, Aaron Coffin, Svetlana Belyanskaya.   

Abstract

5-Aryl-4-carboxamide-1,3-oxazoles are a novel, potent and selective series of GSK-3 inhibitors. The optimization of the series to yield compounds with cell activity and brain permeability is described. Crown
Copyright © 2012. Published by Elsevier Ltd. All rights reserved.

Entities:  

Mesh：

Substances：

Year:  2012        PMID： 22310227     DOI： 10.1016/j.bmcl.2012.01.034

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


  10 in total

1.  Discovery, SAR, and X-ray Binding Mode Study of BCATm Inhibitors from a Novel DNA-Encoded Library.

Authors:  Hongfeng Deng; Jingye Zhou; Flora S Sundersingh; Jennifer Summerfield; Don Somers; Jeffrey A Messer; Alexander L Satz; Nicolas Ancellin; Christopher C Arico-Muendel; Katie L Sargent Bedard; Arthur Beljean; Svetlana L Belyanskaya; Ryan Bingham; Sarah E Smith; Eric Boursier; Paul Carter; Paolo A Centrella; Matthew A Clark; Chun-Wa Chung; Christopher P Davie; Jennifer L Delorey; Yun Ding; G Joseph Franklin; LaShadric C Grady; Kenny Herry; Clare Hobbs; Christopher S Kollmann; Barry A Morgan; Laura J Pothier Kaushansky; Quan Zhou
Journal:  ACS Med Chem Lett       Date:  2015-07-21       Impact factor: 4.345

2.  Novel neuroprotective GSK-3β inhibitor restricts Tat-mediated HIV-1 replication.

Authors:  Irene Guendel; Sergey Iordanskiy; Rachel Van Duyne; Kylene Kehn-Hall; Mohammed Saifuddin; Ravi Das; Elizabeth Jaworski; Gavin C Sampey; Svetlana Senina; Leonard Shultz; Aarthi Narayanan; Hao Chen; Benjamin Lepene; Chen Zeng; Fatah Kashanchi
Journal:  J Virol       Date:  2013-11-13       Impact factor: 5.103

3.  Discovery of a Highly Selective Glycogen Synthase Kinase-3 Inhibitor (PF-04802367) That Modulates Tau Phosphorylation in the Brain: Translation for PET Neuroimaging.

Authors:  Steven H Liang; Jinshan Michael Chen; Marc D Normandin; Jeanne S Chang; George C Chang; Christine K Taylor; Patrick Trapa; Mark S Plummer; Kimberly S Para; Edward L Conn; Lori Lopresti-Morrow; Lorraine F Lanyon; James M Cook; Karl E G Richter; Charlie E Nolan; Joel B Schachter; Fouad Janat; Ye Che; Veerabahu Shanmugasundaram; Bruce A Lefker; Bradley E Enerson; Elijahu Livni; Lu Wang; Nicolas J Guehl; Debasis Patnaik; Florence F Wagner; Roy Perlis; Edward B Holson; Stephen J Haggarty; Georges El Fakhri; Ravi G Kurumbail; Neil Vasdev
Journal:  Angew Chem Int Ed Engl       Date:  2016-06-29       Impact factor: 15.336

4.  DNA-Compatible Suzuki-Miyaura Cross-Coupling Reaction of Aryl Iodides With (Hetero)Aryl Boronic Acids for DNA-Encoded Libraries.

Authors:  Vijay Kumar Siripuram; Yashoda Krishna Sunkari; Thu-Lan Nguyen; Marc Flajolet
Journal:  Front Chem       Date:  2022-06-14       Impact factor: 5.545

5.  Novel inhibitors of severe acute respiratory syndrome coronavirus entry that act by three distinct mechanisms.

Authors:  Adeyemi O Adedeji; William Severson; Colleen Jonsson; Kamalendra Singh; Susan R Weiss; Stefan G Sarafianos
Journal:  J Virol       Date:  2013-05-15       Impact factor: 5.103

6.  Discovery of a Potent Class of PI3Kα Inhibitors with Unique Binding Mode via Encoded Library Technology (ELT).

Authors:  Hongfang Yang; Patricia F Medeiros; Kaushik Raha; Patricia Elkins; Kenneth E Lind; Ruth Lehr; Nicholas D Adams; Joelle L Burgess; Stanley J Schmidt; Steven D Knight; Kurt R Auger; Michael D Schaber; G Joseph Franklin; Yun Ding; Jennifer L DeLorey; Paolo A Centrella; Sibongile Mataruse; Steven R Skinner; Matthew A Clark; John W Cuozzo; Ghotas Evindar
Journal:  ACS Med Chem Lett       Date:  2015-03-20       Impact factor: 4.345

7.  Encoded Library Synthesis Using Chemical Ligation and the Discovery of sEH Inhibitors from a 334-Million Member Library.

Authors:  Alexander Litovchick; Christoph E Dumelin; Sevan Habeshian; Diana Gikunju; Marie-Aude Guié; Paolo Centrella; Ying Zhang; Eric A Sigel; John W Cuozzo; Anthony D Keefe; Matthew A Clark
Journal:  Sci Rep       Date:  2015-06-10       Impact factor: 4.379

8.  Prioritizing multiple therapeutic targets in parallel using automated DNA-encoded library screening.

Authors:  Carl A Machutta; Christopher S Kollmann; Kenneth E Lind; Xiaopeng Bai; Pan F Chan; Jianzhong Huang; Lluis Ballell; Svetlana Belyanskaya; Gurdyal S Besra; David Barros-Aguirre; Robert H Bates; Paolo A Centrella; Sandy S Chang; Jing Chai; Anthony E Choudhry; Aaron Coffin; Christopher P Davie; Hongfeng Deng; Jianghe Deng; Yun Ding; Jason W Dodson; David T Fosbenner; Enoch N Gao; Taylor L Graham; Todd L Graybill; Karen Ingraham; Walter P Johnson; Bryan W King; Christopher R Kwiatkowski; Joël Lelièvre; Yue Li; Xiaorong Liu; Quinn Lu; Ruth Lehr; Alfonso Mendoza-Losana; John Martin; Lynn McCloskey; Patti McCormick; Heather P O'Keefe; Thomas O'Keeffe; Christina Pao; Christopher B Phelps; Hongwei Qi; Keith Rafferty; Genaro S Scavello; Matt S Steiginga; Flora S Sundersingh; Sharon M Sweitzer; Lawrence M Szewczuk; Amy Taylor; May Fern Toh; Juan Wang; Minghui Wang; Devan J Wilkins; Bing Xia; Gang Yao; Jean Zhang; Jingye Zhou; Christine P Donahue; Jeffrey A Messer; David Holmes; Christopher C Arico-Muendel; Andrew J Pope; Jeffrey W Gross; Ghotas Evindar
Journal:  Nat Commun       Date:  2017-07-17       Impact factor: 14.919

9.  N-terminal phosphorylation regulates the activity of glycogen synthase kinase 3 from Plasmodium falciparum.

Authors:  Samuel Pazicky; Arne Alder; Haydyn Mertens; Dmitri Svergun; Tim Gilberger; Christian Löw
Journal:  Biochem J       Date:  2022-02-11       Impact factor: 3.857

10.  Universal strategies for the DNA-encoding of libraries of small molecules using the chemical ligation of oligonucleotide tags.

Authors:  Alexander Litovchick; Matthew A Clark; Anthony D Keefe
Journal:  Artif DNA PNA XNA       Date:  2014
  10 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.