Chinese Journal of Organic Chemistry >
Synthesis and Cytotoxic Activity of Imatinib Derivatives
Received date: 2015-06-25
Revised date: 2015-07-27
Online published: 2015-08-26
Supported by
Project supported by the Foundation of Heilongjiang Educational Committee (No. 12521417).
Fourteen derivatives of imatinib have been prepared by condensation of (L)-N-acylation amino acid with N-(5-amino-2-methylphenyl)-4-(3-pyridyl)-2-pyrimidine amine (6), which was prepared from 3-acetyl-pyrimidin and 2-methyl-5-nitroaniline through the reactions of addition, condensation, cyclization and reduction, respectively. The structures of all target compounds were characterized by IR, 1H NMR, 13C NMR and HRMS techniques. They were evaluated for cytotoxic activity against human Leukemia cells (K562), human non-small-cell-lung cancer cells lines (A549) and human hepatoma cell lines (HepG-2) by methyl thiazolyl tetrazolium (MTT) method. The results showed the cytotoxic activities of compounds 7d,7i,7j,7k,7l, 7n against human Leukemia cells (K562) and human non-small-cell-lung cancer cell lines (A549), compounds 7a, 7d,7e against human hepatoma cell lines (HepG-2) were comparable to those of imatinib.
Chen Shijie , He Long , Wang Xuewei , Gong Xianfeng , Zhang Hua . Synthesis and Cytotoxic Activity of Imatinib Derivatives[J]. Chinese Journal of Organic Chemistry, 2015 , 35(11) : 2377 -2382 . DOI: 10.6023/cjoc201506030
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