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

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

The mTOR protein is a master regulator of cell growth and proliferation, and inhibitors of its kinase activity have the potential to become new class of anticancer drugs. Starting from quinoline 1, which was identified in a biochemical mTOR assay, we developed a tricyclic benzonaphthyridinone inhibi...

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Main Authors: Liu, Qingsong (Author), Chang, Jae Won (Author), Wang, Jinhua (Author), Kang, Seong A. (Author), Thoreen, Carson C. (Author), Markhard, Andrew L. (Author), Hur, Wooyoung (Author), Zhang, Jianming (Author), Sim, Taebo (Author), Gray, Nathanael S. (Author), Sabatini, David (Author)
Other Authors: Massachusetts Institute of Technology. Department of Biology (Contributor), Whitehead Institute for Biomedical Research (Contributor), Koch Institute for Integrative Cancer Research at MIT (Contributor), Sabatini, David M. (Contributor)
Format: Article
Language:English
Published: American Chemical Society (ACS), 2014-02-28T20:07:15Z.
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