2. Academic Validation
  3. Synthesis, cytotoxicity and topoisomerase II inhibitory activity of lomefloxacin derivatives

Synthesis, cytotoxicity and topoisomerase II inhibitory activity of lomefloxacin derivatives

  • Bioorg Med Chem Lett. 2013 May 15;23(10):2974-8. doi: 10.1016/j.bmcl.2013.03.037.
You Zhou 1,  Xiaoli Xu,  Yuan Sun,  Huaping Wang,  Haopeng Sun,  Qidong You
Affiliations

Affiliation

  • 1 Jiangsu Key Laboratory of Drug Design and Optimization, China Pharmaceutical University, Nanjing 210009, China.
PMID: 23566520 DOI: 10.1016/j.bmcl.2013.03.037
Abstract

A novel series of amide derivatives of lomefloxacin were synthesized and evaluated for their Topoisomerase I and II inhibitory activity as well as cytotoxicity against a panel of five human Cancer cell lines. Of the compounds prepared compounds 9d and 9g exhibited strong inhibition against Topoisomerase II at 100μM. In addition, docking studies were performed to predict the inhibition mode.

Figures