Centro de Química Medicinal da Universidade do Porto-CEQUIMED-UP, Rua Aníbal Cunha 164, PT-4050-047 Porto.
Chem Biodivers. 2012 Jun;9(6):1133-43. doi: 10.1002/cbdv.201100190.
Six prenyl (=3-methylbut-2-en-1-yl) chalcones (=1,3-diphenylprop-2-en-1-ones), 2-7, and one natural non-prenylated chalcone, 1, have been synthesized and evaluated for their in vitro growth-inhibitory activity against three human tumor cell lines. A pronounced dose-dependent growth-inhibitory effect was observed for all prenylated derivatives, except for 7. The chalcone possessing one prenyloxy group at C(2'), i.e., 2, was the most active derivative against the three human tumor cell lines (5.9<GI₅₀<7.7 μM). The majority of compounds caused an increase in percentage of apoptotic cells and/or they interfered with cell cycle distribution in the MCF-7 cell line.
六种prenyl（= 3-methylbut-2-en-1-yl）查耳酮（= 1,3-diphenylprop-2-en-1-ones），2-7，和一种天然的非 prenylated 查耳酮，1，已被合成并评估其对三种人类肿瘤细胞系的体外生长抑制活性。所有 prenylated 衍生物都表现出明显的剂量依赖性生长抑制作用，除了 7。在 C（2'）处具有一个 prenyloxy 基团的查耳酮，即 2，是对三种人类肿瘤细胞系（5.9<GI₅₀<7.7 μM）最有效的衍生物。大多数化合物导致凋亡细胞的百分比增加，或者它们干扰 MCF-7 细胞系中的细胞周期分布。
