THE TUMOR-SELECTIVE ANTI-CANCER PRODRUG BQC-G
- 1、下载文档前请自行甄别文档内容的完整性，平台不提供额外的编辑、内容补充、找答案等附加服务。
- 2、"仅部分预览"的文档,不可在线预览部分如存在完整性等问题,可反馈申请退款(可完整预览的文档不适用该条件!)。
- 3、如文档侵犯您的权益，请联系客服反馈,我们会尽快为您处理(人工客服工作时间：9:00-18:30)。
专利名称：THE TUMOR-SELECTIVE ANTI-CANCER PRODRUG BQC-G
发明人：PRIJOVIC, Zeljko, M.,LEU, Yu-Lin,ROFFLER, Steve, R.
申请号：US2010/058045
申请日：20101124
公开号：WO2011/066418A1
公开日：
20110603
专利内容由知识产权出版社提供专利附图：
摘要：The invention relates to the synthesis of a second-generation camptothecin glucuronide prodrug (BQC-G) of a potent anticancer camptothecin derivative 5,6-
dihydro-4H-benzo[de]quinoline-camptothecin (BQC). BQC-G was over 4000 times more water soluble than BQC, displayed good stability in human plasma and was an excellent substrate for enzymatic hydrolysis by bacterial and human β-glucuronidases. BQC-G was about 30 times less toxic than BQC, but was as toxic as BQC after hydrolysis of the glucuronide moiety by β-glucuronidase. In the presence of human serum albumin, BQC-G displayed lower cytotoxicity (IC = 1080 nM) but could be activated by β-glucuronidase to display potent activity (IC = 13.3 nM).
申请人：ACADEMIA SINICA,PRIJOVIC, Zeljko, M.,LEU, Yu-Lin,ROFFLER, Steve, R.
地址：128 Academia Road Section 2 Nankang Taipei 115 Taiwan TW,Institute Of Biomedicial Sciences Academia Sinica Taipei, 11529 TW,Chia Nan University Of Pharmacy And Science Erh-jen Road Section 1, No. 60 Tainan, 71710 TW,Institute Of Biomedicial Sciences Academia Sinica Academia Road Section 2, No. 128 Taipei, 11529 TW 国籍：TW,TW,TW,TW
代理人：JAESCHKE, Wayne, C.
更多信息请下载全文后查看。