摘要
The synthesis and differential antiproliferative activity of two active isomeric metabolites of erlotinib were in- vestigated. This synthetic process had demonstrated to avoid the unstable 4-chloroquinazoline intermediates and long procedures. New intermediates and final compounds were identified by IH NMR, 13C NMR and ESI-TOF MS, and their purities were determined by high performance liquid chromatography. In vitro proliferative assay indi- cated 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.
The synthesis and differential antiproliferative activity of two active isomeric metabolites of erlotinib were in- vestigated. This synthetic process had demonstrated to avoid the unstable 4-chloroquinazoline intermediates and long procedures. New intermediates and final compounds were identified by IH NMR, 13C NMR and ESI-TOF MS, and their purities were determined by high performance liquid chromatography. In vitro proliferative assay indi- cated 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.
