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Design and synthesis of DNA-intercalative naphthalimide- benzothiazole/cinnamide derivatives: Cytotoxicity evaluation and topoisomerase-IIα inhibition

Abstract

A new series of different naphthalimide-benzothiazole/cinnamide derivatives was designed, synthesized and tested for their in vitro cytotoxicity on selected human cancer cell lines. Among them, derivatives 4a and 4b possess with 6-aminobenzothiazole ring and 5g having cinnamide ring displayed potent cytotoxic activity against colon (IC50: 3.715 and 3.467 µM) and lung cancer (IC50: 4.074 and 3.890 µM) cell lines when compared to amonafide (IC50: 5.459 and 7.762 µM). 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 stacks of DNA. In addition, the most potent derivatives 4a and 4b were also found to inhibit DNA topoisomerase-II.

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Publication details

The article was received on 13 Aug 2018, accepted on 01 Nov 2018 and first published on 08 Nov 2018


Article type: Research Article
DOI: 10.1039/C8MD00395E
Citation: Med. Chem. Commun., 2018, Accepted Manuscript
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    Design and synthesis of DNA-intercalative naphthalimide- benzothiazole/cinnamide derivatives: Cytotoxicity evaluation and topoisomerase-IIα inhibition

    A. Kamal, N. S. Rao, N. Nagesh, L. V. Nayak, S. Sunkari, R. Tokala, K. gaddam, P. Regur and N. Shankaraiah, Med. Chem. Commun., 2018, Accepted Manuscript , DOI: 10.1039/C8MD00395E

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