| Summary: | 碩士 === 嘉南藥理大學 === 藥學系 === 106 === Camptothecin has good anti-cancer activity but have poor water solubility. For improving water solubility, our laboratory designed and synthesized two glucuronide prodrugs of Camptothecin (9-ACG and 10-HCG) which will mainly be activated at tumor site expressing large number of β-glucuronidase. According to previous studies, 10-HCG have good affinity for β-glucuronidase but water solubility is not better than 9-ACG. Therefore, we design and synthesize the target compound 10-HCPG by creating N-methyl piperazine on the spacer of 10-HCG, expect for good water solubility, stable in blood, low cytotoxicity, good affinity with β-glucuronidase and specific to tumor cells. Synthesis of 10-HCPG have a problem which spacer conjugating with 10-hydroxycamptothecin have steric effect. For solving this problem, spacer conjugate with 2-amino-5-hydroxybenzaldehyde which have less steric effect and conjugate with tricyclic ketone with condensation reaction
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