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 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 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 strands of DNA. In addition, the most potent derivat

SUBMITTER: Sankara Rao N 

PROVIDER: S-EPMC6350626 | biostudies-literature | 2019 Jan

REPOSITORIES: biostudies-literature