23-羟基白桦酸 C-28 酯衍生物的合成及抗肿瘤活性研究。
Synthesis and biological activity of 23-hydroxybetulinic acid C-28 ester derivatives as antitumor agent candidates.
机构信息
School of Pharmacy, Yantai University, Yantai 264005, Shandong, China.
出版信息
Molecules. 2012 Jul 25;17(8):8832-41. doi: 10.3390/molecules17088832.
23-Hydroxybetulinic acid (1) served as the precursor for the synthesis of C-28 ester derivatives. The target compounds were evaluated in vitro for their antitumor activities against five cell lines (A549, BEL-7402, SF-763, B16 and HL-60). Among the obtained compounds, 6i had the most potent antitumor activity, with the IC(50 values of 8.35 µM in HL-60 cells and showed similar antitumor activity as cyclophosphamide in H22 liver tumor and as 5-fluorouracil in B16 melanoma in vivo.
23-羟基白桦酸（1）可用作合成 C-28 酯衍生物的前体。目标化合物在体外对五种细胞系（A549、BEL-7402、SF-763、B16 和 HL-60）的抗肿瘤活性进行了评价。在所得到的化合物中，6i 具有最强的抗肿瘤活性，在 HL-60 细胞中的 IC（50 值为 8.35µM，并在体内显示出与环磷酰胺在 H22 肝癌和 5-氟尿嘧啶在 B16 黑色素瘤中相似的抗肿瘤活性。
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