1-脱氧巴卡丁 VI 衍生的 C-13、C-14 修饰紫杉烷类似物的合成及生物评价。
Synthesis and biological evaluation of C-13, C-14 modified taxane analogues from 1-deoxybaccatin VI.
机构信息
Department of Chemistry, Innovative Drug Research Center, College of Sciences, Shanghai University , Shanghai , China.
出版信息
Nat Prod Res. 2019 Dec;33(24):3478-3484. doi: 10.1080/14786419.2018.1484459. Epub 2018 Jun 13.
Abstract
Four C-13, C-14 side chain modified 9()-hydroxy-1-deoxy-taxane analogues , , and were semi-synthesized from 1-deoxybaccatin VI. The antitumor activity of these compounds was evaluated against A549 and A2780 cell lines. The preliminary SAR analysis showed that introduction of oxygen-containing group on C-14 could improve the cytotoxic activities.
摘要
四种 C-13、C-14 侧链修饰的 9()-羟基-1-去氧紫杉烷类似物 、 、 和 由 1-去氧巴卡丁 VI 半合成得到。这些化合物对 A549 和 A2780 细胞系的抗肿瘤活性进行了评价。初步的 SAR 分析表明，在 C-14 上引入含氧基团可以提高细胞毒性。
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