設計與合成2-取代-3-苯基喹?衍生物作為抗癌製劑

Design and Synthesis of 2-Substituted-3-Arylquinoline Derivatives as Anticancer Agents

高毓澤(Yu-Tse Kau)

指導教授 ： 陳義龍

高雄醫學大學/生命科學院/醫藥暨應用化學系碩士在職專班/碩士(2015年)

https://doi.org/10.6832/KMU.2015.00111

摘要

由實驗室所合成一系列2-取代-3-苯基喹?化合物中發現其誘導GNMT啟動子之活性。從此系列化合物中發現(Z)-form結構之化合物具有較佳的誘導活性。因此本實驗希望將先前所合成出一系列化合物將其轉換成(Z)-form結構，希望可以得到更具誘導活性之化合物。另一部分則是希望置入不同的縮氨硫脲基團及在縮氨硫脲基團的硫原子做修飾，並也探討其(E)-form及(Z)-form結構之誘導活性之差異。
結果顯示將化合物轉換為(Z)-form結構對其誘導活性的提升效果並不明顯，只有少數化合物KYT-5353及KYT-5356之誘導活性是提升的。

關鍵字

2-取代-3-苯基喹?

並列摘要

A number of 2-substituted-3-phenylquinoline derivatives were synthesized by our laboratory for the past few years. Some of them exhibited promising activity to induce GNMT promoter, especially the derivatives of (Z)-form isomer of semicarbazone derivatives.
This thesis describes the preparation and antiproliferative evaluations of 3-phenylquinoline derivatives in which C-2 position was substituted with various thiosemicarbazone and semicarbazone. These new thiosemicarbazone derivatives were further substituted with different kind of alkyl groups. In addition, we have also converted (E)-form isomers into (Z)-form isomers, and evaluated their activities of inducing GNMT promoter.

並列關鍵字

2-substituted-3-phenylquinoline

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