N-Sulfonyl-aminobiaryls as Antitubulin Agents and Inhibitors of Signal Transducers and Activators of Transcription 3 (STAT3) Signaling
| Autor: | Jing Ping Liou, Yi-Min Liu, Hsun-Yueh Chuang, Mei Chuan Chen, Mei-Jung Lai, An-Chi Tsai, Samir Mehndiratta, Yi-Wen Wu, Li-Hsun Chang, Han-Lin Huang, Shiow Lin Pan, Che-Ming Teng, Hsueh Yun Lee |
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| Rok vydání: | 2015 |
| Předmět: |
STAT3 Transcription Factor
Antineoplastic Agents Apoptosis Binding Competitive Structure-Activity Relationship Transcription (biology) Cell Line Tumor Drug Discovery Humans Structure–activity relationship Phosphorylation STAT3 IC50 Sulfonyl chemistry.chemical_classification Sulfonamides biology Chemistry Tubulin Modulators Tubulin Biochemistry Cell culture biology.protein Molecular Medicine Colchicine |
| Zdroj: | Journal of Medicinal Chemistry. 58:6549-6558 |
| ISSN: | 1520-4804 0022-2623 |
| DOI: | 10.1021/acs.jmedchem.5b00659 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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