2. Academic Validation
  3. Synthesis, in vitro and in vivo antitumor activity of scopoletin-cinnamic acid hybrids

Synthesis, in vitro and in vivo antitumor activity of scopoletin-cinnamic acid hybrids

  • Eur J Med Chem. 2015 Mar 26;93:300-7. doi: 10.1016/j.ejmech.2015.01.040.
Linhu Li 1,  Peng Zhao 2,  Jinglin Hu 1,  Jinhong Liu 1,  Yan Liu 1,  Zhiqiang Wang 1,  Yufeng Xia 3,  Yue Dai 2,  Li Chen 4
Affiliations

Affiliations

  • 1 Department of Natural Medicinal Chemistry, China Pharmaceutical University, 24 Tong Jia Xiang, Nanjing 210009, People's Republic of China.
  • 2 Department of Pharmacology of Chinese Materia Medica, China Pharmaceutical University, 24 Tong Jia Xiang, Nanjing 210009, People's Republic of China.
  • 3 Department of Chinese Materia Medica Analysis, China Pharmaceutical University, 24 Tong Jia Xiang, Nanjing 210009, People's Republic of China. Electronic address: yfxiacpu@126.com.
  • 4 Department of Natural Medicinal Chemistry, China Pharmaceutical University, 24 Tong Jia Xiang, Nanjing 210009, People's Republic of China. Electronic address: chenliduo12@gmail.com.
PMID: 25703298 DOI: 10.1016/j.ejmech.2015.01.040
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 IC50 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.

Keywords

Antitumor activity; Cinnamic acid; Scopoletin.

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