Literature DB >> 20580230

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.

Qianbin Li1, Jingde Wu, Hui Zheng, Kai Liu, Tai L Guo, Yuying Liu, Scott T Eblen, Steven Grant, Shijun Zhang.   

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 G(0)/G(1) 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. Published by Elsevier Ltd.

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Year:  2010        PMID: 20580230     DOI: 10.1016/j.bmcl.2010.06.030

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


  7 in total

1.  Ocular Toxicity Profile of ST-162 and ST-168 as Novel Bifunctional MEK/PI3K Inhibitors.

Authors:  Andrew Smith; Mercy Pawar; Marcian E Van Dort; Stefanie Galbán; Amanda R Welton; Greg M Thurber; Brian D Ross; Cagri G Besirli
Journal:  J Ocul Pharmacol Ther       Date:  2018-04-30       Impact factor: 2.671

2.  Dihydroartemisinin inhibits the Raf/ERK/MEK and PI3K/AKT pathways in glioma cells.

Authors:  Wei DU; Changhe Pang; Yake Xue; Qingjun Zhang; Xinting Wei
Journal:  Oncol Lett       Date:  2015-09-15       Impact factor: 2.967

3.  Structure-Guided Design and Initial Studies of a Bifunctional MEK/PI3K Inhibitor (ST-168).

Authors:  Marcian E Van Dort; Stefanie Galbán; Charles A Nino; Hao Hong; April A Apfelbaum; Gary D Luker; Greg M Thurber; Lydia Atangcho; Cagri G Besirli; Brian D Ross
Journal:  ACS Med Chem Lett       Date:  2017-07-24       Impact factor: 4.345

4.  Structural modifications of (Z)-3-(2-aminoethyl)-5-(4-ethoxybenzylidene)thiazolidine-2,4-dione that improve selectivity for inhibiting the proliferation of melanoma cells containing active ERK signaling.

Authors:  Kwan-Young Jung; Ramin Samadani; Jay Chauhan; Kerrick Nevels; Jeremy L Yap; Jun Zhang; Shilpa Worlikar; Maryanna E Lanning; Lijia Chen; Mary Ensey; Sagar Shukla; Rosene Salmo; Geoffrey Heinzl; Caryn Gordon; Troy Dukes; Alexander D MacKerell; Paul Shapiro; Steven Fletcher
Journal:  Org Biomol Chem       Date:  2013-06-14       Impact factor: 3.876

5.  A novel dual MEK/PDK1 inhibitor 9za retards the cell cycle at G0/G1 phase and induces mitochondrial apoptosis in non-small cell lung cancer cells.

Authors:  Rangru Liu; Zutao Yu; Zhuo Chen; Danqi Liu; Fengying Huang; Qianbin Li; Gaoyun Hu; Xinan Yi; Xi Li; Honghao Zhou; Zhaoqian Liu
Journal:  PeerJ       Date:  2020-10-02       Impact factor: 2.984

6.  Synthesis, α-glucosidase inhibition and molecular docking studies of novel thiazolidine-2,4-dione or rhodanine derivatives.

Authors:  Guang-Cheng Wang; Ya-Ping Peng; Zhen-Zhen Xie; Jing Wang; Ming Chen
Journal:  Medchemcomm       Date:  2017-05-31       Impact factor: 3.597

Review 7.  5-Ene-4-thiazolidinones - An efficient tool in medicinal chemistry.

Authors:  Danylo Kaminskyy; Anna Kryshchyshyn; Roman Lesyk
Journal:  Eur J Med Chem       Date:  2017-09-20       Impact factor: 6.514

  7 in total

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