The novel anti-tumor agents of 4-triazol-1,8-naphthalimides: synthesis, cytotoxicity, DNA intercalation and photocleavage

  • Eur J Med Chem. 2011 Apr;46(4):1274-9. doi: 10.1016/j.ejmech.2011.01.050.
Xiaolian Li  1 ,  Yanjie Lin ,  Qianqian Wang ,  Yukun Yuan ,  Hua Zhang ,  Xuhong Qian
Affiliations
  • 1. State Key Laboratory of Fine Chemicals, Dalian University of Technology, PO Box 89, 158 Zhongshan Road, Dalian 116012, China. [email protected]
PMID: 21345546 DOI: 10.1016/j.ejmech.2011.01.050
Abstract

A novel series of 4-(4-phenyl-[1,2,3]-triazol-1-yl)-1,8-naphthalimide derivatives had been synthesized easily by employing "click reaction". For anti-tumor activity in vitro, all the compounds were found to be more toxic against MCF-7 than Hela and 7721 cells. 4a, 4b and 4e Showed improved cytotoxic activity against MCF-7 cells over Amonafide, in particular compound 4a, with an IC(50) could amount to 10(-7) M. The UV-vis spectra and Circular Dichroism titration indicated that the compounds behaved as effective DNA-intercalating agents. The investigation of their photo-damaging ability illuminated that these compounds could damage DNA effectively into form II and even form III.