N-Sulfonyl-aminobiaryls as Antitubulin Agents and Inhibitors of Signal Transducers and Activators of Transcription 3 (STAT3) Signaling

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, Jing Ping Liou

研究成果: 雜誌貢獻文章

15 引文 (Scopus)

摘要

A series of N-sulfonyl-aminobiaryl derivatives have 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 cancer cell lines (pancreatic AsPC-1, lung A549, liver Hep3B, and prostate PC-3) with a mean GI50 value of 57.5 nM. Additional assays reveal that 21 inhibits not only tubulin polymerization but also the phosphorylation of STAT3 inhibition with an IC50 value of 0.2 μM. Four additional compounds (8, 10, 19, and 35) are also able to inhibit this phosphorylation. This study describes novel N-sulfonyl-aminobiaryl (biaryl-benzenesulfonamides) as potent anticancer agents targeting both STAT3 and tubulin. (Chemical Equation Presented).
原文英語
頁(從 - 到)6549-6558
頁數10
期刊Journal of Medicinal Chemistry
58
發行號16
DOIs
出版狀態已發佈 - 八月 27 2015

指紋

STAT3 Transcription Factor
Tubulin
Phosphorylation
Polymerization
Antineoplastic Agents
Inhibitory Concentration 50
Prostate
Cell Line
Lung
Liver
Neoplasms
benzenesulfonamide
diphenyl

ASJC Scopus subject areas

  • Molecular Medicine
  • Drug Discovery
  • Medicine(all)

引用此文

N-Sulfonyl-aminobiaryls as Antitubulin Agents and Inhibitors of Signal Transducers and Activators of Transcription 3 (STAT3) Signaling. / Lai, Mei-Jung; Lee, Hsueh Yun; Chuang, Hsun-Yueh; Chang, Li-Hsun; Tsai, An-Chi; Chen, Mei Chuan; Huang, Han-Lin; Wu, Yi-Wen; Teng, Che-Ming; Pan, Shiow Lin; Liu, Yi-Min; Mehndiratta, Samir; Liou, Jing Ping.

於: Journal of Medicinal Chemistry, 卷 58, 編號 16, 27.08.2015, p. 6549-6558.

研究成果: 雜誌貢獻文章

Lai, Mei-Jung ; Lee, Hsueh Yun ; Chuang, Hsun-Yueh ; Chang, Li-Hsun ; Tsai, An-Chi ; Chen, Mei Chuan ; Huang, Han-Lin ; Wu, Yi-Wen ; Teng, Che-Ming ; Pan, Shiow Lin ; Liu, Yi-Min ; Mehndiratta, Samir ; Liou, Jing Ping. / N-Sulfonyl-aminobiaryls as Antitubulin Agents and Inhibitors of Signal Transducers and Activators of Transcription 3 (STAT3) Signaling. 於: Journal of Medicinal Chemistry. 2015 ; 卷 58, 編號 16. 頁 6549-6558.
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abstract = "A series of N-sulfonyl-aminobiaryl derivatives have 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 cancer cell lines (pancreatic AsPC-1, lung A549, liver Hep3B, and prostate PC-3) with a mean GI50 value of 57.5 nM. Additional assays reveal that 21 inhibits not only tubulin polymerization but also the phosphorylation of STAT3 inhibition with an IC50 value of 0.2 μM. Four additional compounds (8, 10, 19, and 35) are also able to inhibit this phosphorylation. This study describes novel N-sulfonyl-aminobiaryl (biaryl-benzenesulfonamides) as potent anticancer agents targeting both STAT3 and tubulin. (Chemical Equation Presented).",
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AU - Chuang, Hsun-Yueh

AU - Chang, Li-Hsun

AU - Tsai, An-Chi

AU - Chen, Mei Chuan

AU - Huang, Han-Lin

AU - Wu, Yi-Wen

AU - Teng, Che-Ming

AU - Pan, Shiow Lin

AU - Liu, Yi-Min

AU - Mehndiratta, Samir

AU - Liou, Jing Ping

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N2 - A series of N-sulfonyl-aminobiaryl derivatives have 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 cancer cell lines (pancreatic AsPC-1, lung A549, liver Hep3B, and prostate PC-3) with a mean GI50 value of 57.5 nM. Additional assays reveal that 21 inhibits not only tubulin polymerization but also the phosphorylation of STAT3 inhibition with an IC50 value of 0.2 μM. Four additional compounds (8, 10, 19, and 35) are also able to inhibit this phosphorylation. This study describes novel N-sulfonyl-aminobiaryl (biaryl-benzenesulfonamides) as potent anticancer agents targeting both STAT3 and tubulin. (Chemical Equation Presented).

AB - A series of N-sulfonyl-aminobiaryl derivatives have 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 cancer cell lines (pancreatic AsPC-1, lung A549, liver Hep3B, and prostate PC-3) with a mean GI50 value of 57.5 nM. Additional assays reveal that 21 inhibits not only tubulin polymerization but also the phosphorylation of STAT3 inhibition with an IC50 value of 0.2 μM. Four additional compounds (8, 10, 19, and 35) are also able to inhibit this phosphorylation. This study describes novel N-sulfonyl-aminobiaryl (biaryl-benzenesulfonamides) as potent anticancer agents targeting both STAT3 and tubulin. (Chemical Equation Presented).

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