Literature DB >> 19762236

The discovery and optimisation of pyrido[2,3-d]pyrimidine-2,4-diamines as potent and selective inhibitors of mTOR kinase.

Karine Malagu1, Heather Duggan, Keith Menear, Marc Hummersone, Sylvie Gomez, Christine Bailey, Peter Edwards, Jan Drzewiecki, Frédéric Leroux, Mar Jimenez Quesada, Gesine Hermann, Stephanie Maine, Carrie-Anne Molyneaux, Armelle Le Gall, James Pullen, Ian Hickson, Lisa Smith, Sharon Maguire, Niall Martin, Graeme Smith, Martin Pass.   

Abstract

We describe a novel series of potent inhibitors of the kinase activity of mTOR. The compounds display good selectivity relative to other PI3K-related kinase family members and, in cellular assays, inhibit both mTORC1 and mTORC2 complexes and exhibit good antiproliferative activity.

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Year:  2009        PMID： 19762236     DOI： 10.1016/j.bmcl.2009.08.038

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


  12 in total

1.  Discovery and Biological Profiling of Potent and Selective mTOR Inhibitor GDC-0349.

Authors:  Zhonghua Pei; Elizabeth Blackwood; Lichuan Liu; Shiva Malek; Marcia Belvin; Michael F T Koehler; Daniel F Ortwine; Huifen Chen; Frederick Cohen; Jane R Kenny; Philippe Bergeron; Kevin Lau; Cuong Ly; Xianrui Zhao; Anthony A Estrada; Tom Truong; Jennifer A Epler; Jim Nonomiya; Lan Trinh; Steve Sideris; John Lesnick; Linda Bao; Ulka Vijapurkar; Sophie Mukadam; Suzanne Tay; Gauri Deshmukh; Yung-Hsiang Chen; Xiao Ding; Lori S Friedman; Joseph P Lyssikatos
Journal:  ACS Med Chem Lett       Date:  2012-11-29       Impact factor: 4.345

2.  Discovery and optimization of potent and selective benzonaphthyridinone analogs as small molecule mTOR inhibitors with improved mouse microsome stability.

Authors:  Qingsong Liu; Jinhua Wang; Seong A Kang; Carson C Thoreen; Wooyoung Hur; Hwan Geun Choi; David L Waller; Taebo Sim; David M Sabatini; Nathanael S Gray
Journal:  Bioorg Med Chem Lett       Date:  2011-05-07       Impact factor: 2.823

Review 3.  Targeting the mTOR kinase domain: the second generation of mTOR inhibitors.

Authors:  Yan-Jie Zhang; Yanwen Duan; X F Steven Zheng
Journal:  Drug Discov Today       Date:  2011-02-17       Impact factor: 7.851

4.  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

5.  mTOR Inhibitors at a Glance.

Authors:  Yin Zheng; Yu Jiang
Journal:  Mol Cell Pharmacol       Date:  2015

6.  The susceptibility of trypanosomatid pathogens to PI3/mTOR kinase inhibitors affords a new opportunity for drug repurposing.

Authors:  Rosario Diaz-Gonzalez; F Matthew Kuhlmann; Cristina Galan-Rodriguez; Luciana Madeira da Silva; Manuel Saldivia; Caitlin E Karver; Ana Rodriguez; Stephen M Beverley; Miguel Navarro; Michael P Pollastri
Journal:  PLoS Negl Trop Dis       Date:  2011-08-23

Review 7.  mTOR kinase: a possible pharmacological target in the management of chronic pain.

Authors:  Lucia Lisi; Paola Aceto; Pierluigi Navarra; Cinzia Dello Russo
Journal:  Biomed Res Int       Date:  2015-01-01       Impact factor: 3.411

Review 8.  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

Review 9.  mTOR inhibitors in cancer therapy.

Authors:  Jianling Xie; Xuemin Wang; Christopher G Proud
Journal:  F1000Res       Date:  2016-08-25

10.  Potent dual inhibitors of TORC1 and TORC2 complexes (KU-0063794 and KU-0068650) demonstrate in vitro and ex vivo anti-keloid scar activity.

Authors:  Farhatullah Syed; Hitesh J Sanganee; Subir Singh; Ashwani Bahl; Ardeshir Bayat
Journal:  J Invest Dermatol       Date:  2013-01-10       Impact factor: 8.551
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