Design and synthesis a water-soluble group for ether-linkage of 10-hydroxycamptothecin prodrug

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標題:	Design and synthesis a water-soluble group for ether-linkage of 10-hydroxycamptothecin prodrug
作者:	邱沛芳林偉琪陳國輝呂玉玲
貢獻者:	藥學系
日期:	2017
上傳時間:	2022-01-25 14:44:35 (UTC+8)
摘要:	For selective cancer chemotherapy, we previously designed and synthesized two β-glucuronidase-activated prodrugs of camptothecin (9-ACG and 10-HCG), which increased water solubility for camptothecins. In normal tissues, β-glucuronidase is localized primarily in lysosomes and thereby not available for activation of glucuronide prodrugs because these prodrugs are generally hydrophilic, thus rendering them impermeable to cell membranes. Therefore, glucuronide-based prodrugs can be used in prodrug monotherapy.9-ACG was more soluble than 10-HCG via oxycarbamate linkage, so 9-ACG was more low toxicity than 10-HCG. However, 10-HCG was a good substrate for β-glucuronidase, which has ether linkage. In order to increase the solubility of 10-HCG, we designed 10-HCPG, which creates a hydrophilic group in link of prodrug. We predict that 10-HCPG is soluble, low cytotoxicity and good a substrate for β-glucuronidase. We expect 10-HCPG, which is a good candidate for selective cancer chemotherapy.
關聯:	2017 第十一屆嘉南藥理大學藥理學院師生研究成果發表會，起迄日：2017/05/02-2017/05/04
显示于类别:	[藥理學院] 2017 第十一屆嘉南藥理大學藥理學院師生研究成果發表會 [藥學系(所)] 會議論文

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