Novel DNA intercalators without basic side chains as efficient antitumor agents: design, synthesis and evaluation of
Xiaolian Li1, Qianqian Wang, Yang Qing
1State Key Laboratory of Fine Chemicals, Dalian University of Technology, PO Box 89, 158 Zhongshan Road, Dalian 116012, China.
Abstract:
Several 2-(substituted benzo[c,d]indol-2(1H)-ylidene)malononitriles have been designed and synthesized. Their DNA binding, antitumor and DNA damaging properties were evaluated. All the compounds exhibited efficient antitumor activities with preference to be against the tumor cell line 7721 rather than the tumor cell line MCF-7. Compound 1f could intercalate into DNA entirely presumably by the good conjugation of carbonyl group with benzo[c,d]indol moiety. What's more, 1f exhibited potent toxicity against MCF-7 cells with IC(50) at 0.003 microM and against 7721 cells at 0.115 microM, respectively.
Related Concept Videos
Inhibitors of Bacterial DNA Synthesis
Antiviral Nucleoside Inhibitors
DNA Topoisomerases
Types and Mechanism of action
Topoisomerases are divided into two main types. Type I...
Drugs that Destabilize Microtubules


