Discovery of polymethoxyphenyl-pyridines bearing amino side chains as tubulin colchicine-binding site inhibitors
| Autor: | XiaoYang Li, HuanXian Wu, Kai-Wen Feng, JiaHuan Xu, Shaoyu Wu, zhong-zhen zhou, Xiao-Fang Li |
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| Rok vydání: | 2022 |
| Předmět: |
History
Aniline Compounds Binding Sites Polymers and Plastics Molecular Structure Pyridines Organic Chemistry Clinical Biochemistry Pharmaceutical Science Antineoplastic Agents Biochemistry Industrial and Manufacturing Engineering Tubulin Modulators Structure-Activity Relationship Tubulin Cell Line Tumor Drug Discovery Molecular Medicine Business and International Management Drug Screening Assays Antitumor Colchicine Molecular Biology Cell Proliferation |
| Zdroj: | Bioorganic & Medicinal Chemistry. 73:117007 |
| ISSN: | 0968-0896 |
| DOI: | 10.1016/j.bmc.2022.117007 |
| Popis: | Nineteen TH03 analogues were designed and synthesized as tubulin colchicine-binding site inhibitors with potent antiproliferative activities. Among these compounds, 3,5-dimethoxyphenylpyridines 8j bearing a 4-methoxybenzyl aniline side-chain displayed the best antiproliferative activities against glioma (U87MG and U251). In addition, the trimethoxyphenylpyridine 8o bearing a 4-methyl-N-methyl aniline side-chain showed the best antiproliferative activities against colon carcinoma and lung cancer with the lowest IC |
| Databáze: | OpenAIRE |
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