1. N-Sulfonyl-aminobiaryls asAntitubulin Agents and Inhibitors of Signal Transducers and Activatorsof Transcription 3 (STAT3) Signaling.
- Author
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Mei-Jung Lai, Hsueh-Yun Lee, Hsun-Yueh Chuang, Li-Hsun Chang, An-Chi Tsai, Mei-Chuan Chen, Han-Lin Huang, Yi-Wen Wu, Che-Ming Teng, Shiow-Lin Pan, Yi-Min Liu, Samir Mehndiratta, and Jing-Ping Liou
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TUBULINS , *CELLULAR signal transduction , *INHIBITION of cellular proliferation , *CHEMICAL derivatives , *PHOSPHORYLATION , *GENETIC transcription , *CELL communication - Abstract
A seriesof N-sulfonyl-aminobiaryl derivativeshave been examined as novel antitubulin agents. Compound 21[N-(4′-cyano-3′-fluoro-biphenyl-2-yl)-4-methoxy-benzenesulfonamide]exhibits remarkable antiproliferative activity against four cancercell lines (pancreatic AsPC-1, lung A549, liver Hep3B, and prostatePC-3) with a mean GI50value of 57.5 nM. Additional assaysreveal that 21inhibits not only tubulin polymerizationbut also the phosphorylation of STAT3 inhibition with an IC50value of 0.2 μM. Four additional compounds (8, 10, 19, and 35) are alsoable to inhibit this phosphorylation. This study describes novel N-sulfonyl-aminobiaryl (biaryl-benzenesulfonamides) as potentanticancer agents targeting both STAT3 and tubulin. [ABSTRACT FROM AUTHOR]
- Published
- 2015
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