Literature DB >> 19733066

Identification and optimisation of novel and selective small molecular weight kinase inhibitors of mTOR.

Keith A Menear1, Sylvie Gomez, Karine Malagu, Christine Bailey, Kristel Blackburn, Xiao-Ling Cockcroft, Sally Ewen, Alexandra Fundo, Armelle Le Gall, Gesine Hermann, Luisa Sebastian, Mihiro Sunose, Thomas Presnot, Eleanor Torode, Ian Hickson, Niall M B Martin, Graeme C M Smith, Kurt G Pike.   

Abstract

A pharmacophore mapping approach, derived from previous experience of PIKK family enzymes, was used to identify a hit series of selective inhibitors of the mammalian target of rapamycin (mTOR). Subsequent refinement of the SAR around this hit series based on a tri-substituted triazine scaffold has led to the discovery of potent and selective inhibitors of mTOR.

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Year:  2009        PMID： 19733066     DOI： 10.1016/j.bmcl.2009.08.069

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


  12 in total

1.  An in silico protocol for identifying mTOR inhibitors from natural products.

Authors:  Lei Chen; Ling Wang; Qiong Gu; Jun Xu
Journal:  Mol Divers       Date:  2014-08-26       Impact factor: 2.943

2.  Ligand-based 3-D pharmacophore generation and molecular docking of mTOR kinase inhibitors.

Authors:  Karunakar Tanneeru; Lalitha Guruprasad
Journal:  J Mol Model       Date:  2011-07-30       Impact factor: 1.810

3.  mTOR Mediated Anti-Cancer Drug Discovery.

Authors:  Qingsong Liu; Carson Thoreen; Jinhua Wang; David Sabatini; Nathanael S Gray
Journal:  Drug Discov Today Ther Strateg       Date:  2009

4.  Identification of novel N-(morpholine-4-carbonyloxy) amidine compounds as potent inhibitors against hepatitis C virus replication.

Authors:  Akiko Kusano-Kitazume; Naoya Sakamoto; Yukiko Okuno; Yuko Sekine-Osajima; Mina Nakagawa; Sei Kakinuma; Kei Kiyohashi; Sayuri Nitta; Miyako Murakawa; Seishin Azuma; Yuki Nishimura-Sakurai; Masatoshi Hagiwara; Mamoru Watanabe
Journal:  Antimicrob Agents Chemother       Date:  2011-12-27       Impact factor: 5.191

5.  Discovery of 1-(4-(4-propionylpiperazin-1-yl)-3-(trifluoromethyl)phenyl)-9-(quinolin-3-yl)benzo[h][1,6]naphthyridin-2(1H)-one as a highly potent, selective mammalian target of rapamycin (mTOR) inhibitor for the treatment of cancer.

Authors:  Qingsong Liu; Jae Won Chang; Jinhua Wang; Seong A Kang; Carson C Thoreen; Andrew Markhard; Wooyoung Hur; Jianming Zhang; Taebo Sim; David M Sabatini; Nathanael S Gray
Journal:  J Med Chem       Date:  2010-10-14       Impact factor: 7.446

6.  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

7.  Discovery of 9-(6-aminopyridin-3-yl)-1-(3-(trifluoromethyl)phenyl)benzo[h][1,6]naphthyridin-2(1H)-one (Torin2) as a potent, selective, and orally available mammalian target of rapamycin (mTOR) inhibitor for treatment of cancer.

Authors:  Qingsong Liu; Jinhua Wang; Seong A Kang; Carson C Thoreen; Wooyoung Hur; Tausif Ahmed; David M Sabatini; Nathanael S Gray
Journal:  J Med Chem       Date:  2011-02-15       Impact factor: 7.446

8.  Design, synthesis, cytotoxicity evaluation and docking studies of 1,2,4-triazine derivatives bearing different arylidene-hydrazinyl moieties as potential mTOR inhibitors.

Authors:  Sara Ranjbar; Najmeh Edraki; Mahsima Khoshneviszadeh; Alireza Foroumadi; Ramin Miri; Mehdi Khoshneviszadeh
Journal:  Res Pharm Sci       Date:  2018-02

9.  Synthesis and Characterization of New Series of 1,3-5-Triazine Hydrazone Derivatives with Promising Antiproliferative Activity.

Authors:  Hessa H Al H Al Rasheed; Azizah M M Malebari; Kholood A A Dahlous; Ayman El-Faham
Journal:  Molecules       Date:  2020-06-11       Impact factor: 4.411

10.  Synthesis, Anti-proliferative Activity, and Molecular Docking Study of New Series of 1,3-5-Triazine Schiff Base Derivatives.

Authors:  Hessa H Al Rasheed; Azizah M Malebari; Kholood A Dahlous; Darren Fayne; Ayman El-Faham
Journal:  Molecules       Date:  2020-09-05       Impact factor: 4.411
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