267654-13-7Relevant academic research and scientific papers
Identification of KPNB1 as a Cellular Target of Aminothiazole Derivatives with Anticancer Activity
Kim, Yong-Hak,Ha, Siyoung,Kim, Jungwon,Ham, Seung Wook
supporting information, p. 1406 - 1409 (2016/07/16)
We found that aminothiazole derivative (E)-N-(5-benzylthiazol-2-yl)-3-(furan-2-yl)acrylamide (1) has strong anticancer activity, and undertook proteomics approaches to identify the target protein of compound 1, importin β1 (KPNB1). A competitive binding assay using fluorescein-labeled 1 showed that 1 has strong binding affinity for KPNB1 (Kd: ～20 nm). Furthermore, through western blotting assays for KPNB1, KPNA2, EGFR, ErbB2, and STAT3, we confirmed that 1 has inhibitory effects on the importin pathway. KPBN1 appears to be overexpressed in several cancer cells, and siRNA-induced inhibition of KPNB1 shows significant inhibition of cancer cell proliferation, while leaving non-cancerous cells unaffected. Therefore, compound 1 is a promising new lead for the development of KPNB1-targeted anticancer agents. Fluorescein-labeled 1 could be a useful quantitative probe for the development of novel KPNB1 inhibitors.
Novel 2-Aminothiazole Derivatives and Composition for Treating Cancer Comprising the Same
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Paragraph 0057; 0058; 0059; 0070, (2017/06/06)
PURPOSE: A novel 2-aminothiazole derivative and an anticancer composition containing the same are provided to suppress growth and proliferation of various cancer cells and to induce cancer cell apoptosis. CONSTITUTION: A 2-aminothiazole derivative is denoted by chemical formula 1. In chemical formula 1, R1 is phenyl, halogen-substituted phenyl, alkyl of 1-4 carbon atoms, or phenyl-substituted alkyl of C1-4; and R2 is alkyl of C1-9, furyl-substituted alkyl of C1-4, furyl-substituted alkenyl of C1-4. An anticancer composition contains the 2-aminothiazole derivative of chemical formula 1 or pharmaceutically acceptable salt thereof as an active ingredient. The anticancer composition is a pharmaceutical composition for preventing or treating cancer.
