Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10592948 | Bioorganic & Medicinal Chemistry Letters | 2014 | 5 Pages |
Abstract
A novel series of 4-pyrazolyl-1,8-naphthalimide derivatives have been designed and facilely synthesized. For anticancer activity in vitro, most of the compounds were found to be more toxic against human mammary cancer cells (MCF-7) than human cervical carcinoma cells (Hela) and human lung cancer cells (A549). Compounds 4i, 4h, 4b and 4a showed improved cytotoxic activity against MCF-7 cells over amonafide, in particular compounds 4i and 4h, the IC50 values of which against cell lines of MCF-7 were 0.51 μM and 0.79 μM, respectively. The DNA-binding properties of 4i were investigated by UV-vis, fluorescence, and Circular Dichroism (CD) spectroscopies and thermal denaturation. The results indicated that compound 4i as the DNA-intercalating agent exhibited middle binding affinity with CT-DNA.
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Authors
Shenghui Li, Shengjie Xu, Yonghe Tang, Shan Ding, Jinchao Zhang, Shuxiang Wang, Guoqiang Zhou, Chuanqi Zhou, Xiaoliu Li,