Abstract

N-substituted (E)-4-arylidene isoquinoline-1,3-dione derivatives as potent anticancer agents � Synthesis and molecular evaluations

Author(s): Manikandan A. and Sivakumar A

This article describes a two-step synthesis of (E)-4-arylidene isoquinoline-1,3-dione derivatives and their anticancer effects. First, an intermediate N-aryl homophthalimide was synthesized using ZnO as the catalyst. Second, a new modified synthesis of (E)-4-arylidene isoquinoline-1,3-dione derivatives in the presence of oxalic acid in ethanol (EtOH). The obtained products were characterized by FT- IR, GC/MS, 1H NMR, and 13C NMR. Synthesized isoquinoline derivatives 5a-h possesses significant cytotoxic activity against MCF-7 cell lines. Molecular docking study results are disclosing the structure-activity similarity of the synthesized compounds with anticancer evaluations. IC50 ± SD values for the compounds 5g (3.57±0.54 μg/ml), 5h (3.89±0.82 μg/ml) and 5d (4.42±0.98μg/ml) were very close to the standard doxorubicin (3.36±0.38 μg/ml). The mean percentage of inhibition for doxorubicin was 70.39±7.18, for our compounds, it was 33.14±6.61 (5b) to 61.75±8.22 (5g). At the end of study, the necessity of in vivo animal model evaluations was understood and the same studies are progressing currently.

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