| Summary: | 碩士 === 中國醫藥大學 === 藥物化學研究所碩士班 === 95 === Abstract
Microtubules are a valid target for anticancer drugs, and it is necessary to continue developing those antimitotic drugs as chemotherapeutic agents. We put the target on researching and synthesizing novel agents for inhibiting cancer cells in our laboratory. At the same time, we found that 2-phenyl-4-quinolone (2-PQ) derivatives were novel antimitotic agents, and most of them were displayed great anticancer activity at large cell lines and some animal experiment. These years, we synthesized a series of 2-PQ derivatives, and chose one of them with excellent anticancer activity for cancer cells as leading compound, 2''-fluoro-6,7-(methylenedioxy)-2-phenyl-4-quinolone (2FMPQ). Therefore, we synthesized 4-substituted derivatives of 2FMPQ to improve the unsatisfying pharmacokinetic characters of 2FMPQ, and expected they could be prodrugs convert to the active form when they are taken into the body in the future.
We also put the 6,7-methylenedioxy-2-(2,3,4-substituted phenyl)-4-quinolone analogous to dock into the colchicine binding site of tubulin to discuss and conclude the correlation between pharmacological parameter and interactions with protein active domain of the series of substituted 2-PQ.
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