Design, synthesis and antitumor activities of fluoroquinolone C-3 heterocycles (IV): s-triazole Schiff–Mannich bases derived from ofloxacin

Guoqiang Hu, Guoqiang Wang, Nannan Duan, Xiaoyi Wen, Tieyao Cao, Songqiang Xie, Wenlong Huang
2012 Acta Pharmaceutica Sinica B  
The aim of this research was to produce novel antitumor fluoroquinolones from antibacterial analogs by introduction of a heterocyclic ring as a bioisostere of the C-3 carboxylic acid group. To this end, two series of eleven s-triazole derivatives bearing functionalized side chains of Schiff bases and Schiff-Mannich bases were designed and synthesized. Structures were characterized by elemental analysis and spectral data after which in vitro antitumor activity against L1210, CHO and HL60 cell
more » ... es was evaluated in the MTT assay. Compounds possessing a free phenol group were particularly active and warrant further development.
doi:10.1016/j.apsb.2011.11.003 fatcat:szspavb6rvb6lhux33zvvfpqmm