2. Academic Validation
  3. Synthesis and biological evaluation of novel N-substituted benzamides as anti-migration agents for treatment of osteosarcoma

Synthesis and biological evaluation of novel N-substituted benzamides as anti-migration agents for treatment of osteosarcoma

  • Eur J Med Chem. 2021 Mar 15:214:113203. doi: 10.1016/j.ejmech.2021.113203.
Xiaojing Chen 1,  Guangbao Wang 1,  Ali Mohammed Mohammed Alsayed 1,  Zongxuan Du 1,  Lu Liu 1,  Yue Ma 1,  Peng Liu 1,  Qianwen Zhang 1,  Xianxin Chen 1,  Wenbin Chen 1,  Faqing Ye 2,  Xiaohui Zheng 3,  Zhiguo Liu 4
Affiliations

Affiliations

  • 1 Chemical Biology Research Center at School of Pharmaceutical Sciences, Wenzhou Medical University, 1210 University Town, Wenzhou, Zhejiang, 325035, China.
  • 2 School of Pharmaceutical Sciences, Wenzhou Medical University, 1210 University Town, Wenzhou, Zhejiang, 325035, China. Electronic address: yfq664340@163.com.
  • 3 Chemical Biology Research Center at School of Pharmaceutical Sciences, Wenzhou Medical University, 1210 University Town, Wenzhou, Zhejiang, 325035, China. Electronic address: zhengxh@wmu.edu.cn.
  • 4 Chemical Biology Research Center at School of Pharmaceutical Sciences, Wenzhou Medical University, 1210 University Town, Wenzhou, Zhejiang, 325035, China. Electronic address: lzgcnu@163.com.
PMID: 33530028 DOI: 10.1016/j.ejmech.2021.113203
Abstract

A novel series of novel N-substituted (indole or indazole) benzamides were synthesized, and their anti-tumor properties were evaluated. The majority of tested compounds possessed moderate cytotoxicity, but inspiringly, we verified that active compound 5d presents an astonishing advantage by inhibiting the adhesion, migration, and invasion of osteosarcoma (OS) cells in vitro. Mechanistically, we confirmed 5d inhibited the migration ability of OS cells via the expression of genes related to adhesion, migration, and invasion. This effects of 5d suggest that it can be used as a potential chemotherapeutic drug to some aggressive and/or metastatic cancers, as well as in combination with Other clinical anti-cancer drugs. In turn, this could enhance the therapeutic effect or reduce the risk of cell migration.

Keywords

Activity; Anti-migration; N-substituted benzamides; Osteosarcoma.

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