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Synthesis and antitumor activities of novel 2-substituted pyrimidinone-5-carboxylic acid benzylamides |
| CHEN Weimin1, FENG Jin2, TU Hongyi3 |
| 1.Department of Medicinal Chemistry, College of Pharmacy, Jinan University, Guangzhou 510632, China; Institute of Pharmaceutical Sciences, The First Military Medical University, Guangzhou 510515, China; 2.Department of Medicinal Chemistry, College of Pharmacy, Jinan University, Guangzhou 510632, China; 3.Institute of Pharmaceutical Sciences, The First Military Medical University, Guangzhou 510515, China |
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Abstract The title compounds were synthesized via N-benzylmalonamic acid methyl ester (3). As the key intermediate, 3 was prepared from methyl malonyl chloride and benzylamine. Then, compound 3 was reacted with dimethylformamide dimethyl acetal yielding vinylogue amides 4 and 5. Isomers 4 and 5 were respectively treated with amidine and guanidine to afford the title compounds 2-substituted pyrimidinone-5-carboxylic acid benzylamides 6 and 7. All of the new compounds were characterized by 1H-NMR (nuclear magnetic resonance), 13C-NMR, MS and High Resolution Mass Spectrometer (HRMS). The antitumor activities of the compounds were tested in vitro against LoVo cells and Hep3B cells. Both compounds 6 and 7 show activity against these two cell lines.
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Issue Date: 05 June 2007
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