Literature DB >> 18625552

4-(1,3-Thiazol-2-yl)morpholine derivatives as inhibitors of phosphoinositide 3-kinase.

Rikki Alexander1, Ahrani Balasundaram, Mark Batchelor, Daniel Brookings, Karen Crépy, Tom Crabbe, Marie-France Deltent, Frank Driessens, Andrew Gill, Sue Harris, Gillian Hutchinson, Claire Kulisa, Mark Merriman, Prakash Mistry, Ted Parton, James Turner, Ian Whitcombe, Sara Wright.   

Abstract

4-(1,3-Thiazol-2-yl)morpholine derivatives have been identified as potent and selective inhibitors of phosphoinositide 3-kinase. The SAR data of selected examples are presented and the in vivo profiling of compound 18 is shown to demonstrate the utility of this class of compounds in xenograft models of tumor growth.

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Year:  2008        PMID： 18625552     DOI： 10.1016/j.bmcl.2008.06.076

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


  5 in total

1.  Direct Conversion of Primary Alcohols to 1,2-Amino Alcohols: Enantioselective Iridium-Catalyzed Carbonyl Reductive Coupling of Phthalimido-Allene via Hydrogen Auto-Transfer.

Authors:  Kim Spielmann; Ming Xiang; Leyah A Schwartz; Michael J Krische
Journal:  J Am Chem Soc       Date:  2019-08-29       Impact factor: 15.419

2.  Molecular dynamics and integrated pharmacophore-based identification of dual [Formula: see text] inhibitors.

Authors:  Maninder Kaur; Pankaj Kumar Singh; Manjinder Singh; Renu Bahadur; Om Silakari
Journal:  Mol Divers       Date:  2017-11-14       Impact factor: 2.943

Review 3.  Progress in the preclinical discovery and clinical development of class I and dual class I/IV phosphoinositide 3-kinase (PI3K) inhibitors.

Authors:  S J Shuttleworth; F A Silva; A R L Cecil; C D Tomassi; T J Hill; F I Raynaud; P A Clarke; P Workman
Journal:  Curr Med Chem       Date:  2011       Impact factor: 4.530

Review 4.  Recent development of ATP-competitive small molecule phosphatidylinostitol-3-kinase inhibitors as anticancer agents.

Authors:  Yu Liu; Wen-Zhu Wan; Yan Li; Guan-Lian Zhou; Xin-Guang Liu
Journal:  Oncotarget       Date:  2017-01-24

5.  Efficient Routes to a Diverse Array of Amino Alcohol-Derived Chiral Fragments.

Authors:  Sina Haftchenary; Shawn D Nelson; Laura Furst; Sivaraman Dandapani; Steven J Ferrara; Žarko V Bošković; Samuel Figueroa Lazú; Adrian M Guerrero; Juan C Serrano; DeMarcus K Crews; Cristina Brackeen; Jeffrey Mowat; Thomas Brumby; Marcus Bauser; Stuart L Schreiber; Andrew J Phillips
Journal:  ACS Comb Sci       Date:  2016-08-12       Impact factor: 3.784
  5 in total

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