2. Academic Validation
  3. Excellent antitumor and antimetastatic activities based on novel coumarin/pyrazole oxime hybrids

Excellent antitumor and antimetastatic activities based on novel coumarin/pyrazole oxime hybrids

  • Eur J Med Chem. 2019 Mar 15;166:470-479. doi: 10.1016/j.ejmech.2019.01.070.
Hong Dai 1,  Meiling Huang 1,  Jianqiang Qian 2,  Ji Liu 2,  Chi Meng 2,  Yangyang Li 2,  Guxu Ming 2,  Ting Zhang 2,  Senling Wang 3,  Yujun Shi 3,  Yong Yao 4,  Shushan Ge 1,  Yanan Zhang 5,  Yong Ling 6
Affiliations

Affiliations

  • 1 College of Chemistry and Chemical Engineering, Nantong University, Nantong, 226019, People's Republic of China; School of Pharmacy, Nantong University, Nantong, 226001, People's Republic of China.
  • 2 School of Pharmacy, Nantong University, Nantong, 226001, People's Republic of China; Jiangsu Province Key Laboratory for Inflammation and Molecular Drug Target, Nantong University, Nantong, 226001, People's Republic of China.
  • 3 College of Chemistry and Chemical Engineering, Nantong University, Nantong, 226019, People's Republic of China.
  • 4 College of Chemistry and Chemical Engineering, Nantong University, Nantong, 226019, People's Republic of China. Electronic address: yaoyong1986@ntu.edu.cn.
  • 5 School of Pharmacy, Nantong University, Nantong, 226001, People's Republic of China; Jiangsu Province Key Laboratory for Inflammation and Molecular Drug Target, Nantong University, Nantong, 226001, People's Republic of China. Electronic address: zhangyanan@gmail.com.
  • 6 College of Chemistry and Chemical Engineering, Nantong University, Nantong, 226019, People's Republic of China; School of Pharmacy, Nantong University, Nantong, 226001, People's Republic of China; Jiangsu Province Key Laboratory for Inflammation and Molecular Drug Target, Nantong University, Nantong, 226001, People's Republic of China. Electronic address: Lyyy111@sina.com.
PMID: 30739827 DOI: 10.1016/j.ejmech.2019.01.070
Abstract

A series of hybrids 10a-v based on coumarin/pyrazole oxime have been synthesized, and exhibit good to excellent antitumor activities. Compound 10n has shown remarkable Anticancer effect on SMMC-7721 cells (IC50 = 2.08 μM), which is considerably lower than 5-FU (IC50 = 37.8 μM) and similar to ADM (IC50 = 2.67 μM), with little effect on normal hepatic cells LO2. Notably, the suppression experiments of metastatic activities reveal that 10n also displays significant anti-metastasis effects through inhibiting cell migration and invasion in highly metastatic SMMC-7721 cell line, and dose-dependently reverses TGF-β1-induced epithelial-mesenchymal transition (EMT) procedure better than ADM. Finally, 10n also possesses low acute toxicity and potent tumor growth inhibitory property against SMMC-7721 cell lines in vivo. Our findings suggest that novel coumarin/pyrazole oxime hybrids are promising therapeutic agent candidates for further research.

Keywords

Antimetastasis; Antitumor activity; Coumarin; Hybrids; Pyrazole oxime.

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