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[摘要]：Polyfunctional tetrahydro-2H-pyranol3,2-clpyridazin-3(6H)-one derivatives were synthesized and biologically evaluated as novel anticancer agents. These motifs were produced by a five-step reaction sequence in which the Achmatowicz oxidative cyclization, is the basic core for such synthesis. Compounds 15f, 16c, and 16d showed antiproliferative activity against the SK-BR-3 breast cancer cell line. Importantly, 16c and 16d showed the highest efficacy, being approximately 30-fold more potent against SK-BR-3 (IC50 0.21 and 0.15 mu M, respectively) compared to other cancer cell lines tested. In addition, 16c and 16d displayed about 295 fold less toxicity against normal breast cell line MCF10A compared to SKBR-3 breast cancer cells. These compounds form the foundation for further investigation in our continuing efforts to develop potent anticancer agents. (C) 2010 Elsevier Masson SAS. All rights reserved. |
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