1. Synthesis and cytotoxicity studies of novel [1,2,4]triazolo[1,5-a]pyrimidine-7-amines.
- Author
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Zhai X, Zhao YF, Liu YJ, Zhang Y, Xun FQ, Liu J, and Gong P
- Subjects
- Amines pharmacology, Antineoplastic Agents pharmacology, Cell Line, Tumor, Humans, Pyrimidines pharmacology, Structure-Activity Relationship, Triazoles pharmacology, Amines chemical synthesis, Antineoplastic Agents chemical synthesis, Pyrimidines chemical synthesis, Triazoles chemical synthesis
- Abstract
A series of novel N-anilino-5-methyl-2-(3-(5-(alkylaminomethyl)furan-2-yl-methylthio)propyl)-[1,2,4]triazolo-[1,5-a]pyrimidine-7-amine derivatives were synthesized and evaluated for their in vitro cytotoxicity against two cancer cell lines, Bel-7402 and HT-1080. Compounds 9, 14, 19 and 23 possessed marked cytotoxicity, especially 23 (with IC(50) values of 15.0 microM and 7.8 microM against Bel-7402 and HT-1080 cell lines, respectively), which had emerged as lead compound. The activity was found to depend strongly on substitution pattern of the side chains at C-2 position, and 4-triflouromethylanilino substituent at C-7 position was an option for anticancer potency.
- Published
- 2008
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