C-12-bit Pyxinol derivative, preparation method and application of C-12-bit Pyxinol derivative

The invention discloses a C-12-bit Pyxinol derivative as shown in a formula 5 or a formula 6, or a pharmaceutically acceptable salt thereof, and discloses a preparation method of the C-12-bit Pyxinol derivative. The C-12-site Pyxinol derivative provided by the invention is a novel compound obtained...

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Hauptverfasser: YANG GANGQIANG, MA YIQI, ZHAO YUJIN, LI SHUANG, YU LIPING, TAN SHUAI, ZHANG ZHEN, LV HANQI, LI XIANG, CHEN CHENG, QUAN MENGRAN
Format: Patent
Sprache:chi ; eng
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Zusammenfassung:The invention discloses a C-12-bit Pyxinol derivative as shown in a formula 5 or a formula 6, or a pharmaceutically acceptable salt thereof, and discloses a preparation method of the C-12-bit Pyxinol derivative. The C-12-site Pyxinol derivative provided by the invention is a novel compound obtained by carrying out modification design and synthesis on the C-12 site for the first time, and has remarkable anti-tumor drug resistance reversion ability. After the Pyxinol derivative is combined with a clinically common antitumor drug paclitaxel for use, the toxicity of the Pyxinol derivative to KBV is remarkably improved, so that the paclitaxel can still generate good antitumor activity to the Pyxinol derivative at an extremely low concentration. The Pyxinol derivative disclosed by the invention is used as a high-activity potential P-gp inhibitor and has a relatively high development value. # imgabs0 # 本发明公开了式5或式6所示的C-12位Pyxinol衍生物,或其药学上可接受的盐,并公开了其制备方法。本发明提供的C-12位Pyxinol衍生物是首次在C-12位进行修饰设计并合成得到的新化合物,具有显著的抗肿瘤耐药逆转能力。与临