Literature DB >> 18248814

Imidazo[4,5-c]quinolines as inhibitors of the PI3K/PKB-pathway.

Frédéric Stauffer1, Sauveur-Michel Maira, Pascal Furet, Carlos García-Echeverría.   

Abstract

Imidazo[4,5-c]quinoline derivatives have been discovered and developed as potent and effective modulators of the phosphatidylinositol 3-kinase (PI3K)/protein kinase B (PKB) pathway to lead to clinical development candidates. The SAR data of representative examples of this compound class and their biological profiling in cellular and in vivo settings are presented and discussed.

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Year:  2007        PMID： 18248814     DOI： 10.1016/j.bmcl.2007.12.018

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


  29 in total

Review 1.  Phosphatidylinositol 3-kinase-AKT-mammalian target of rapamycin (PI3K-Akt-mTOR) signaling pathway in non-small cell lung cancer.

Authors:  Po Yee Yip
Journal:  Transl Lung Cancer Res       Date:  2015-04

2.  A highly potent and selective Vps34 inhibitor alters vesicle trafficking and autophagy.

Authors:  Baptiste Ronan; Odile Flamand; Lionel Vescovi; Christine Dureuil; Laurence Durand; Florence Fassy; Marie-France Bachelot; Annabelle Lamberton; Magali Mathieu; Thomas Bertrand; Jean-Pierre Marquette; Youssef El-Ahmad; Bruno Filoche-Romme; Laurent Schio; Carlos Garcia-Echeverria; Hélène Goulaouic; Benoit Pasquier
Journal:  Nat Chem Biol       Date:  2014-10-19       Impact factor: 15.040

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

Review 4.  PI3K and Akt as molecular targets for cancer therapy: current clinical outcomes.

Authors:  Ipsita Pal; Mahitosh Mandal
Journal:  Acta Pharmacol Sin       Date:  2012-09-17       Impact factor: 6.150

5.  New quinoline/chalcone hybrids as anti-cancer agents: Design, synthesis, and evaluations of cytotoxicity and PI3K inhibitory activity.

Authors:  Samar H Abbas; Amer Ali Abd El-Hafeez; Mai E Shoman; Monica M Montano; Heba A Hassan
Journal:  Bioorg Chem       Date:  2018-11-02       Impact factor: 5.275

6.  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

Review 7.  PDK1 inhibitors.

Authors:  Elisa Barile; Surya K De; Maurizio Pellecchia
Journal:  Pharm Pat Anal       Date:  2012-05

8.  Increased AKT S473 phosphorylation after mTORC1 inhibition is rictor dependent and does not predict tumor cell response to PI3K/mTOR inhibition.

Authors:  Madlaina Breuleux; Matthieu Klopfenstein; Christine Stephan; Cheryl A Doughty; Louise Barys; Saveur-Michel Maira; David Kwiatkowski; Heidi A Lane
Journal:  Mol Cancer Ther       Date:  2009-04       Impact factor: 6.261

9.  Active-site inhibitors of mTOR target rapamycin-resistant outputs of mTORC1 and mTORC2.

Authors:  Morris E Feldman; Beth Apsel; Aino Uotila; Robbie Loewith; Zachary A Knight; Davide Ruggero; Kevan M Shokat
Journal:  PLoS Biol       Date:  2009-02-10       Impact factor: 8.029

10.  Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases.

Authors:  Beth Apsel; Jimmy A Blair; Beatriz Gonzalez; Tamim M Nazif; Morri E Feldman; Brian Aizenstein; Randy Hoffman; Roger L Williams; Kevan M Shokat; Zachary A Knight
Journal:  Nat Chem Biol       Date:  2008-10-12       Impact factor: 15.040
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