Abstract
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.