| Summary: | 碩士 === 國防醫學院 === 藥學研究所 === 93 === ABSTRACT 1
Solid tumour causes cells with deficiency oxygen to form hypoxic cell because the blood is insufficient in supply. Cancer patients who resist to chemotherapy and radiotherapy to cause, while causing and treating solid tumour, curative effect is not good. The bioreductive anticancer agents is one kind of novel anticancer drugs, which the selectivity acts on hypoxic cell.Dual actions of bioreductive anticancer agents directly destroy DNA and act as auxiliary treatment for chemotherapy / radiotherapy. At present, the bioreductive anticancer agents can be divided into four main classes in accordance with the structure. Among them it is the highest with the cytotoxic selectivity (HCR=300) of cell to hypoxic cell of tirapazamine (TPZ) of aromatic N-oxides,which the side effect is minimum.The bioreductive agents lead development potentiality of novel anticancer agents
Regard TPZ as the lead compound of anticancer agents in this laboratory synthesis and modification based on TPZ. We aimed at synthesis a series of di-N-oxide chemicals to develop higher selectivity effects and lower toxicity targeting hypoxic cells. The target compounds assess were examined the cytotoxic activity by SRB assay.
Those target compounds have no significant anticancer effect, but compound 13a, 15, 24b, 24c, showed slightly better cytotoxic effect than lead compound TPZ (compound 3 ).
ABSTRACT 2
Mitotic is cellular process of differentiation. It can produce with the daughter cell of the same self-characteristics of master cell. So the growth of the life and growth in nature cancer cells can make use of those characteristics. One of that antimitotic agents the pharmaceutical and acted on the cell had antimitotic effect and reach the anticancer result. The mechanism are : 1. Inhibiting the assembly of tubulin; 2. Stabilising microtubule and to prevent it to depolymerization. (example: Taxol)
At present, clinical use antimitotic agents amost originate from active constituents of natural plants. Regarding podophyllotoxin as the lead compound of antimitotic anticancer agents were in progress in our laboratory. A rapid one-pot microwave synthetic approach, target compounds 4a-l were synthesized for examining antineoplastic activity. The target compounds assess were examined the cytotoxic activity by SRB assay.
Those target compounds have no significant anticancer effect.
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