Literature DB >> 22119469

Novel and selective spiroindoline-based inhibitors of Sky kinase.

Noel A Powell1, Jeffrey T Kohrt, Kevin J Filipski, Michael Kaufman, Derek Sheehan, Jeremy E Edmunds, Amy Delaney, Yuli Wang, Francis Bourbonais, Doh-Yeel Lee, Frank Schwende, Fang Sun, Pat McConnell, Cornel Catana, Huifen Chen, Jeff Ohren, Lisa A Perrin.   

Abstract

We report the discovery of a novel series of spiroindoline-based inhibitors of Sky kinase that bind in the ATP-binding site and exhibit high levels of kinome selectivity through filling the Ala571-subpocket. These inhibitors exhibit moderate oral bioavailability in the rat due to low absorption across the gut wall.
Copyright © 2011 Elsevier Ltd. All rights reserved.

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Year:  2011        PMID: 22119469     DOI: 10.1016/j.bmcl.2011.11.036

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


  10 in total

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Review 3.  The TAM family: phosphatidylserine sensing receptor tyrosine kinases gone awry in cancer.

Authors:  Douglas K Graham; Deborah DeRyckere; Kurtis D Davies; H Shelton Earp
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4.  The Axl kinase domain in complex with a macrocyclic inhibitor offers first structural insights into an active TAM receptor kinase.

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Journal:  J Biol Chem       Date:  2017-07-19       Impact factor: 5.157

5.  Synthesis of spirocyclic indolines by interruption of the Bischler-Napieralski reaction.

Authors:  Jonathan William Medley; Mohammad Movassaghi
Journal:  Org Lett       Date:  2013-07-05       Impact factor: 6.005

Review 6.  The Role of TAM Family Receptors in Immune Cell Function: Implications for Cancer Therapy.

Authors:  Magdalena Paolino; Josef M Penninger
Journal:  Cancers (Basel)       Date:  2016-10-21       Impact factor: 6.639

Review 7.  Targeting the TAM Receptors in Leukemia.

Authors:  Madeline G Huey; Katherine A Minson; H Shelton Earp; Deborah DeRyckere; Douglas K Graham
Journal:  Cancers (Basel)       Date:  2016-11-08       Impact factor: 6.639

Review 8.  Targeting Tyro3, Axl and MerTK (TAM receptors): implications for macrophages in the tumor microenvironment.

Authors:  Kayla V Myers; Sarah R Amend; Kenneth J Pienta
Journal:  Mol Cancer       Date:  2019-05-14       Impact factor: 27.401

Review 9.  The Emerging Role of TYRO3 as a Therapeutic Target in Cancer.

Authors:  Sherri K Smart; Eleana Vasileiadi; Xiaodong Wang; Deborah DeRyckere; Douglas K Graham
Journal:  Cancers (Basel)       Date:  2018-11-29       Impact factor: 6.639

10.  Spiro[pyrrolidine-3,3'-oxindoles] and Their Indoline Analogues as New 5-HT6 Receptor Chemotypes.

Authors:  Ádám A Kelemen; Grzegorz Satala; Andrzej J Bojarski; György M Keserű
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  10 in total

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