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New Synthetic Route of Two Active Isomeric Metabolites of Erlotinib and Their Bioactivity Studies against Several Tumor Cell Lines
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
2011-08-01
DOI10.1002/cjoc.201180305
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
WOS记录号WOS:000294779400025
项目编号2009ZX09301-010
资助机构National Integrity Innovational Technology Platform of New Drug and Development ; National Fund for Talent training in Basic Science
引用统计
被引频次:1[WOS]   [WOS记录]     [WOS相关记录]
文献类型期刊论文
条目标识符http://ir.bjmu.edu.cn/handle/400002259/62067
专题北京大学药学院_药剂学系
北京大学医学部管理机构_医学部
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
推荐引用方式
GB/T 7714
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.
APA Li Hanqing.,Li Mengyao.,Li Zaiquan.,Li Liang.,Bi Shanshan.,...&Lu Wei.(2011).New Synthetic Route of Two Active Isomeric Metabolites of Erlotinib and Their Bioactivity Studies against Several Tumor Cell Lines.CHINESE JOURNAL OF CHEMISTRY,29(8),1709-1714.
MLA Li Hanqing,et al."New Synthetic Route of Two Active Isomeric Metabolites of Erlotinib and Their Bioactivity Studies against Several Tumor Cell Lines".CHINESE JOURNAL OF CHEMISTRY 29.8(2011):1709-1714.
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