Journal
MEDCHEMCOMM
Volume 10, Issue 1, Pages 72-79Publisher
ROYAL SOC CHEMISTRY
DOI: 10.1039/c8md00395e
Keywords
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Funding
- CSIR-New Delhi
- project entitled Affordable Cancer Therapeutics under the XIIth five year plan [CSC0301]
- SERB, DST, Govt. of India [YSS-2015-001709]
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A new series of different naphthalimide-benzothiazole/cinnamide derivatives were designed, synthesized and tested for their in vitro cytotoxicity on selected human cancer cell lines. Among them, derivatives 4a and 4b with the 6-aminobenzothiazole ring and 5g with the cinnamide ring displayed potent cytotoxic activity against colon (IC50: 3.715 and 3.467 mu M) and lung cancer (IC50: 4.074 and 3.890 mu M) cell lines when compared to amonafide (IC50: 5.459 and 7.762 mu M). Later, the DNA binding studies for these selected derivatives (by CD, UV/vis, fluorescence spectroscopy, DNA viscosity, and molecular docking) suggested that these new derivatives significantly intercalate between two strands of DNA. In addition, the most potent derivatives 4a and 4b were also found to inhibit DNA topoisomerase-II.
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