Literature DB >> 19954970

Novel imidazolopyrimidines as dual PI3-Kinase/mTOR inhibitors.

Aranapakam M Venkatesan1, Christoph M Dehnhardt, Zecheng Chen, Efren Delos Santos, Osvaldo Dos Santos, Matthew Bursavich, Adam M Gilbert, John W Ellingboe, Semiramis Ayral-Kaloustian, Gulnaz Khafizova, Natasja Brooijmans, Robert Mallon, Irwin Hollander, Larry Feldberg, Judy Lucas, Ker Yu, Jay Gibbons, Robert Abraham, Tarek S Mansour.   

Abstract

This article describes the syntheses and SAR of a series of imidazolopyrimidine derivatives, which are evaluated as inhibitors of PI3-Kinase (PI3K) and mTOR. These compounds were found to be ATP competitive with good tumor cell growth inhibition, and suppression of pathway specific biomakers such as phosphorylation of Akt at T308. Copyright 2009 Elsevier Ltd. All rights reserved.

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Year:  2009        PMID: 19954970     DOI: 10.1016/j.bmcl.2009.11.057

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


  4 in total

1.  Predictive Model for Site-Selective Aryl and Heteroaryl C-H Functionalization via Organic Photoredox Catalysis.

Authors:  Kaila A Margrey; Joshua B McManus; Simone Bonazzi; Frederic Zecri; David A Nicewicz
Journal:  J Am Chem Soc       Date:  2017-08-07       Impact factor: 15.419

2.  A selectivity study on mTOR/PI3Kα inhibitors by homology modeling and 3D-QSAR.

Authors:  Ting Ran; Tao Lu; Haoliang Yuan; Haichun Liu; Jian Wang; Weiwei Zhang; Ying Leng; Guowu Lin; Shulin Zhuang; Yadong Chen
Journal:  J Mol Model       Date:  2011-04-27       Impact factor: 1.810

3.  Thiazolidinedione-based PI3Kα inhibitors: an analysis of biochemical and virtual screening methods.

Authors:  Jo-Anne Pinson; Oleg Schmidt-Kittler; Jiuxiang Zhu; Ian G Jennings; Kenneth W Kinzler; Bert Vogelstein; David K Chalmers; Philip E Thompson
Journal:  ChemMedChem       Date:  2011-01-04       Impact factor: 3.466

Review 4.  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

  4 in total

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