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 language | English |
|---|---|
| Pages (from-to) | 6549-6558 |
| Number of pages | 10 |
| Journal | Journal of Medicinal Chemistry |
| Volume | 58 |
| Issue number | 16 |
| DOIs | |
| Publication status | Published - Aug 27 2015 |
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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 journal › Article
}
TY - JOUR
T1 - N-Sulfonyl-aminobiaryls as Antitubulin Agents and Inhibitors of Signal Transducers and Activators of Transcription 3 (STAT3) Signaling
AU - Lai, Mei-Jung
AU - Lee, Hsueh Yun
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
PY - 2015/8/27
Y1 - 2015/8/27
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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UR - http://www.scopus.com/inward/citedby.url?scp=84940480723&partnerID=8YFLogxK
U2 - 10.1021/acs.jmedchem.5b00659
DO - 10.1021/acs.jmedchem.5b00659
M3 - Article
VL - 58
SP - 6549
EP - 6558
JO - Journal of Medicinal Chemistry
JF - Journal of Medicinal Chemistry
SN - 0022-2623
IS - 16
ER -