Discovery of 3-(2-aminoethyl)-5-(3-phenyl-propylidene)-thiazolidine-2,4-dione as a dual inhibitor of the Raf/MEK/ERK and the PI3K/Akt signaling pathways |
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| Authors: | Qianbin Li Jingde Wu Hui Zheng Kai Liu Tai L Guo Yuying Liu Scott T Eblen Steven Grant Shijun Zhang |
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| Institution: | 1. Department of Medicinal Chemistry, School of Pharmacy, Virginia Commonwealth University, Richmond, VA 23298-0540, USA;2. Department of Cell and Molecular Pharmacology, Medical University of South Carolina, Charleston, SC, USA;3. Department of Pharmacology and Toxicology, Virginia Commonwealth University, Richmond, VA, USA;4. Departments of Internal Medicine and Biochemistry, Virginia Commonwealth University, Richmond, VA, USA |
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| Abstract: | A thiazolidine-2,4-dione derivative, 3-(2-aminoethyl)-5-(3-phenyl-propylidene)-thiazolidine-2,4-dione (2), was identified as a dual inhibitor of the Raf/MEK/ extracellular signal-regulated kinase (ERK) and the phosphatidylinositol 3-kinase (PI3K)/Akt signaling cascades. The discovered compound inhibited cell proliferation, induced early apoptosis, and arrested cells in G0/G1 phase in human leukemia U937 cells. These results indicate its potential as a new lead compound to develop novel dual signaling pathway inhibitors and anticancer agents. |
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