於本篇論文中，本人提出一個新的概念將光引導去氧核醣核酸切割試劑與奈米粒子相結合，形成一新型具有切割去氧核醣核酸能力之奈米材料。除此之外，本人也至被一系列木酚素衍生物並檢測該類化合物對於愛滋病毒之抑制活性。
在本論文第一部分，本人將光引導去氧核醣核酸切割試劑藉由聚乙二醇支鏈與金奈米粒子相結合，形成一新型具有切割去氧核醣核酸能力之奈米材料。
在第二部分中，本人成功製造出一種新型具鐵磁性之光引導去氧核醣核酸切割奈米粒子其平均直徑為6.1奈米。此新型奈米粒子去氧核醣核酸切割能力可低至10 □M並可由核磁共振造影技術追蹤此奈米粒子。
在第三部分中，本人設計並合成出七個新型之木酚素衍生物。在這些新型衍生物中還有氮原子的化合物可以轉換成對應的水溶性鹽類，並具有良好的水溶性。此類新型之木酚素衍生物不但水溶性佳同時也相當穩定。這些新型化合物並發現具又抑制愛滋病毒之能力。其中活性最好化合物18b其抑制半數生長濃度為0.88 □M。

In this thesis, I developed a new concept to combine photo-induced DNA cleaving agents and nanoparticles together to produce the novel nanomaterials with DNA cleaving ability. Furthermore, a new series of nordihydroguaiaretic acid (NDGA) derivatives were prepared and screened their inhibitions against HIV.
In the part 1 of this thesis, Arylhyrazones were linked onto gold nanoparticles through the poly(ethylene glycol) spacer to produce a new type of photo-induced DNA-cleaving nanomaterials.
In the part 2, a new type of magnetite phenylhydrazone–Fe3O4 conjugated nanoparticles 8 were synthesized with a diameter of 6.1 nm in average. They possessed DNA cleaving ability with concentration as low as 10 □M and can be traced by MRI.
In the part 3, totally 7 new nordihydroguaiaretic acid derivatives successfully synthesized. Among these derivatives, the nitrogen-containing compounds were converted to the corresponding hydrochloride salts. Having good solubility, these NDGA derivatives were found stable in aqueous solution. These new compounds exerted appealing activity against HIV Tat-regulated transactivation in human epithelial cells. The most potent compounds meso-2,3-dimethyl-1,4-bis(3,4-[2-(piperdino)ethoxyphenyl])butane tetrakishydrochloride salt (18b) showed IC50 values of □□□□□□M.

Part 1

Novel Arylhydrazone-conjugated gold nanoparticles with DNA-cleaving Ability: the first DNA-nicking nanomaterial

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Part 2

Magnetite Nanoparticles of Ferrosoferric Oxide Conjugated with Phenylhydrazone for DNA Cleavage

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Part 3

Development of New Nordihydroguaiaretic Acid Derivatives as Anti-HIV Agents

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