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).

Original languageEnglish
Pages (from-to)6549-6558
Number of pages10
JournalJournal of Medicinal Chemistry
Volume58
Issue number16
DOIs
Publication statusPublished - Aug 27 2015

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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)

Cite this

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.

In: Journal of Medicinal Chemistry, Vol. 58, No. 16, 27.08.2015, p. 6549-6558.

Research output: Contribution to journalArticle

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. In: Journal of Medicinal Chemistry. 2015 ; Vol. 58, No. 16. pp. 6549-6558.
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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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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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