Laboratório de Síntese Orgânica, Universidade Federal de São João Del Rei, Campus Centro Oeste Dona Lindu, 35.501-296 Divinópolis/MG, Brazil.
Molecules. 2012 Aug 29;17(9):10331-43. doi: 10.3390/molecules170910331.
A series of new chalcones substituted with azide/triazole groups were designed and synthesized, and their cytotoxic activity was evaluated in vitro against the HeLa cell line. O-Alkylation, Claisen-Schmidt condensation and Cu(I)-catalyzed cycloaddition of azides with terminal alkynes were applied in key steps. Fifteen compounds were tested against HeLa cells. Compound 8c was the most active molecule, with an IC₅₀ value of 13.03 μM, similar to the value of cisplatin (7.37 μM).
设计并合成了一系列带有叠氮基/三唑基的新型查尔酮，评估了它们对 HeLa 细胞系的体外细胞毒性。在关键步骤中应用了 O-烷基化、Claisen-Schmidt 缩合和 Cu(I)催化的叠氮化物与末端炔烃的环加成反应。对 15 种化合物进行了抗 HeLa 细胞测试。化合物 8c 是最活跃的分子，IC₅₀ 值为 13.03 μM，与顺铂（7.37 μM）相似。
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