Discovery of 4-methoxy-N-(1-naphthyl)benzenesulfonamide derivatives as small molecule dual-target inhibitors of tubulin and signal transducer and activator of transcription 3 (STAT3) based on ABT-751
| Autor: | Xuebao, Wang, Ying, Lu, Doudou, Sun, Jinheng, Qian, Sijun, Tu, Weixia, Yue, Humin, Lin, Haijie, Tang, Fanxi, Meng, Qin, He, Zixin, Xie, Yuan, Zhang, Huijun, Chen, Shumei, Ma, Zhigui, Zuo, Faqing, Ye |
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| Rok vydání: | 2022 |
| Předmět: |
STAT3 Transcription Factor
Sulfonamides Dose-Response Relationship Drug Molecular Structure Organic Chemistry Antineoplastic Agents Biochemistry Tubulin Modulators Structure-Activity Relationship Tubulin Cell Line Tumor Drug Discovery Humans Drug Screening Assays Antitumor Molecular Biology Cell Proliferation |
| Zdroj: | Bioorganic Chemistry. 125:105864 |
| ISSN: | 0045-2068 |
| Popis: | Overexpressed tubulin and continuously activated STAT3 play important roles in the development of many cancers and are potential therapeutic targets. A series of 4-methoxy-N -(1-naphthalene) benzenesulfonamide derivatives were designed and optimized based on β-tubulin inhibitor ABT-751 to verify whether STAT3 and tubulin dual target inhibitors have better antitumor effects. Compound DL14 showed strong inhibitory activity against A549, MDA-MB-231 and HCT-116 cells in vitro with IC |
| Databáze: | OpenAIRE |
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