1. Synthesis, in vitro and in vivo antitumor activity of scopoletin-cinnamic acid hybrids.
- Author
-
Li, Linhu, Zhao, Peng, Hu, Jinglin, Liu, Jinhong, Liu, Yan, Wang, Zhiqiang, Xia, Yufeng, Dai, Yue, and Chen, Li
- Subjects
- *
ANTINEOPLASTIC agents , *SCOPOLETIN , *CINNAMIC acid , *IN vitro studies , *DOXORUBICIN , *DRUG synthesis , *CANCER cells , *TUMOR growth - Abstract
A series of hybrids of scopoletin and substituted cinnamic acid were designed, synthesized and evaluated in vitro and in vivo against five human tumor cell lines [MCF-7, MDA-MB-231, A549, HCT-116, and HeLa] with doxorubicin as the positive control. Compounds 17a , 17b , 17c and 17g exhibited potent cytotoxic activity. Especially, compound 17b displayed broad spectrum activity with IC 50 values ranging from 0.249 μM to 0.684 μM. Moreover, in a preliminary pharmacological study, 17b not only remarkably induced cellular apoptosis, but also clearly induced A549 cells cycle arrest at S phase. In vivo study showed that 17b significantly suppressed tumor growth in a dose-dependent manner without causing the loss of the mean body weight of mice, which was superior to doxorubicin. These preliminary results indicate that 17b is an optimal anti-cancer leading compound and merit further structural modification. [ABSTRACT FROM AUTHOR]
- Published
- 2015
- Full Text
- View/download PDF