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学科主题: 药学
题名:
New Synthetic Route of Two Active Isomeric Metabolites of Erlotinib and Their Bioactivity Studies against Several Tumor Cell Lines
作者: Li Hanqing1; Li Mengyao1; Li Zaiquan2; Li Liang1; Bi Shanshan1; Deng Chenhui1; Chen Rui1; Zhou Tianyan1,3; Lu Wei1,3
关键词: erlotinib hydrochloride ; epidermal growth factor receptor ; active metabolites ; biological activity ; antiproliferation
刊名: CHINESE JOURNAL OF CHEMISTRY
发表日期: 2011-08-01
DOI: 10.1002/cjoc.201180305
卷: 29, 期:8, 页:1709-1714
收录类别: SCI ; IC ; CCR
文章类型: Article
WOS标题词: Science & Technology
类目[WOS]: Chemistry, Multidisciplinary
研究领域[WOS]: Chemistry
关键词[WOS]: GROWTH-FACTOR RECEPTOR ; TYROSINE KINASE INHIBITORS ; ACUTE MYELOGENOUS LEUKEMIA ; SMALL-MOLECULE INHIBITOR ; FLT3 ANTAGONIST ; EGFR ; GEFITINIB ; DISCOVERY ; PHARMACOKINETICS ; ACTIVATION
英文摘要:

The synthesis and differential antiproliferative activity of two active isomeric metabolites of erlotinib were investigated. This synthetic process had demonstrated to avoid the unstable 4-chloroquinazoline intermediates and long procedures. New intermediates and final compounds were identified by H-1 NMR, C-13 NMR and ESI-TOF MS, and their purities were determined by high performance liquid chromatography. In vitro proliferative assay indicated that these two metabolites possessed antiproliferative activity against some conventional tumor cell lines and EGFR tyrosine kinase over-expression tumor cell lines as compared to erlotinib control, and their antitumor activity in cellular level was first reported here.

语种: 英语
所属项目编号: 2009ZX09301-010
项目资助者: National Integrity Innovational Technology Platform of New Drug and Development ; National Fund for Talent training in Basic Science
WOS记录号: WOS:000294779400025
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.bjmu.edu.cn/handle/400002259/62067
Appears in Collections:北京大学药学院_药剂学系_期刊论文

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作者单位: 1.Peking Univ, Hlth Sci Ctr, Sch Pharmaceut Sci, Dept Pharmaceut, Beijing 100191, Peoples R China
2.Peking Univ, Hlth Sci Ctr, Sch Basic Med Sci, Dept Radiat Med, Beijing 100191, Peoples R China
3.Peking Univ, State Key Lab Nat & Biomimet Drugs, Beijing 100191, Peoples R China

Recommended Citation:
Li Hanqing,Li Mengyao,Li Zaiquan,et al. New Synthetic Route of Two Active Isomeric Metabolites of Erlotinib and Their Bioactivity Studies against Several Tumor Cell Lines[J]. CHINESE JOURNAL OF CHEMISTRY,2011,29(8):1709-1714.
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