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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

Authors :
Li, Qianbin
Wu, Jingde
Zheng, Hui
Liu, Kai
Guo, Tai L.
Liu, Yuying
Eblen, Scott T.
Grant, Steven
Zhang, Shijun
Source :
Bioorganic & Medicinal Chemistry Letters. Aug2010, Vol. 20 Issue 15, p4526-4530. 5p.
Publication Year :
2010

Abstract

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. [Copyright &y& Elsevier]

Details

Language :
English
ISSN :
0960894X
Volume :
20
Issue :
15
Database :
Academic Search Index
Journal :
Bioorganic & Medicinal Chemistry Letters
Publication Type :
Academic Journal
Accession number :
52305264
Full Text :
https://doi.org/10.1016/j.bmcl.2010.06.030