Discovery of Novel 3,4-Dihydro-2(1H)-Quinolinone Sulfonamide Derivatives as New Tubulin Polymerization Inhibitors with Anti-Cancer Activity
Copyright policy )Discovery of Novel 3,4-Dihydro-2(1H)-Quinolinone Sulfonamide Derivatives as New Tubulin Polymerization Inhibitors with Anti-Cancer Activity
In this paper, a small series of novel quinoline sulfonamide derivatives was synthesized, and their structure of the target compounds were confirmed by 1H NMR and MS. The screening of the news target compounds’ in vitro cytotoxic activities against tumor cell lines by the MTT method was performed. Among them, compound D13 (N-(4-methoxybenzyl)-2-oxo-N-(3,4,5-trimethoxyphenyl)-1,2,3,4-tetrahydroquinoline-6-sulfonamide exhibited the strongest inhibitory effect on the proliferation of HeLa (IC50: 1.34 μM), and this value correlated well with the inhibitory activities of the compound against tubulin polymerization (IC50: 6.74 μM). In summary, a new type of quinoline-sulfonamide derivative with tubulin polymerization inhibitory activity was discovered, and it can be used as a lead compound for further modification.
- Inner Mongolia University for Nationalities China (People's Republic of)
synthesis; quinoline-sulfonamide; anti-tumor; tubulin polymerization, Sulfonamides, synthesis, Dose-Response Relationship, Drug, Molecular Structure, Organic chemistry, Antineoplastic Agents, Quinolones, Article, Tubulin Modulators, Hydroquinones, Polymerization, tubulin polymerization, Structure-Activity Relationship, QD241-441, Tubulin, quinoline-sulfonamide, Drug Screening Assays, Antitumor, anti-tumor, Cell Proliferation
synthesis; quinoline-sulfonamide; anti-tumor; tubulin polymerization, Sulfonamides, synthesis, Dose-Response Relationship, Drug, Molecular Structure, Organic chemistry, Antineoplastic Agents, Quinolones, Article, Tubulin Modulators, Hydroquinones, Polymerization, tubulin polymerization, Structure-Activity Relationship, QD241-441, Tubulin, quinoline-sulfonamide, Drug Screening Assays, Antitumor, anti-tumor, Cell Proliferation
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