Novel DNA intercalators without basic side chains as efficient antitumor agents: Design,synthesis and evaluation of benzo-[c,d]-indol-malononitrile derivatives |
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| Authors: | Xiaolian Li Qianqian Wang Yang Qing Yanjie Lin Yingli Zhang Xuhong Qian Jingnan Cui |
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| Affiliation: | 1. State Key Laboratory of Fine Chemicals, Dalian University of Technology, PO Box 89, 158 Zhongshan Road, Dalian 116012, China;2. Shanghai Key Laboratory of Chemical Biology, School of Pharmacy, East China University of Science and Technology, PO Box 544, 130 Meilong Road, Shanghai 200237, China;3. Department of Bioscience and Biotechnology, Dalian University of Technology, Dalian 116012, China |
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| 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 IC50 at 0.003 μM and against 7721 cells at 0.115 μM, respectively. |
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