Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 24, Issue 2, Pages 586-590Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2013.12.014
Keywords
Naphthalimides; Pyrazole; Anticancer; DNA-binding
Categories
Funding
- National Basic Research 973 Program [2010CB534913]
- Hebei Provincial Natural Science Foundation of China-Shijiazhuang Pharmaceutical Group (CSPC) Foundation [B2011201174, B2012201044]
- Hebei Province Nature Science Fund for Distinguished Young Scholars [B2011201164]
- Nature Science Fund of Hebei Province [B2011201135]
- Key Basic Research Special Foundation of Science Technology Ministry of Hebei Province [11966412D, 12966418D]
- Open Fund of Key Laboratory of Chemical Biology of Hebei Province [09265631D-7]
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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 mu M and 0.79 mu M, 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. (C) 2013 Elsevier Ltd. All rights reserved.
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