Trifluoromethylated carboline compounds targeting DNA: Synthesis, binding and anti-proliferative effects on human cancer cell lines.

Bioorganic Chemistry(2019)

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摘要
•3 sets of trifluoromethylated carboline compounds prepared by Pictet-Spengler cyclization.•Interaction of the molecules with CT DNA was emphasized by fluorescence, ITC, FTIR and viscosity.•Binding follows: comp3 > comp 4 > comp1 > comp2 > comp5 > comp6 > comp7.•Cytotoxicity follows: comp3 > comp4 > comp7 > comp6 > comp5 > comp2 and > comp1.•Comp3 showed maximum cytotoxicity with minimum GI50 of 6.2 µM, against HCT-116 causing apoptosis.
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关键词
Trifluoromethylated carboline compounds,Nucleic acid-small molecular binding,FTIR,ITC,Cell cytotoxicity,Apoptosis
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