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Title: Synthesis, structure and anticancer activity of copper(II) complexes of <i style="">N</i>-benzyl-2-(diethylamino)acetamide and 2-(diethylamino)-<i style="">N</i>-phenylethylacetamide
Authors: Singh, Amit P
Kaushik, Nagendra K
Verma, Akhilesh K
Gupta, Rajeev
Keywords: Bioinorganic chemistry
Amide-based ligands
Anti-cancer activity
Issue Date: Mar-2011
Publisher: NISCAIR-CSIR, India
Abstract: The ligands <i>N</i>-benzyl-2-(diethylamino)acetamide, (HL<sup>1</sup>) and 2-(diethylamino)-<i>N</i>-phenylethylacetamide (HL<sup>2</sup>), have been used to synthesize copper(II) complexes, [Cu(HL<sup>1</sup>)<sub>2</sub>](ClO<sub>4</sub>)<sub>2</sub> <b>(1)</b> and [Cu(HL<sup>2</sup>)<sub>2</sub>](ClO<sub>4</sub>)<sub>2</sub> <b>(2)</b>, respectively. Both complexes are well characterized by various spectral and physical methods. The crystal structure of complex <b style="">(1)</b> reveals that two bidentate ligands coordinate the Cu(II) ion via O<sub>amide</sub> and N<sub>amine</sub> atoms in the basal plane whereas one of the ClO<sub>4</sub><sup>-</sup> ions occupies the apical position maintaining a square–pyramidal geometry. Screening results for anti–proliferative studies against the U87 and HeLa cancerous cells indicate promising activity. The complexes enhanced growth inhibition and cell death in a concentration and time dependent manner for both U87 and HeLa cell lines. Of the two compounds, complex <b>(2)</b> exhibits better activity against both HeLa and U87 cells. Further, both complexes are specifically potent against U87 after 72 h of treatment. Micronucleus and apoptosis frequencies are 3 – 4 times higher in treated cells when compared with untreated control. Despite potent <i style="">in vitro</i> activity, both complexes exhibit diminished cytotoxicity against the normal human HEK cells at all effective concentrations.
Description: 474-483
ISSN: 0975-0975(Online); 0376-4710(Print)
Appears in Collections:IJC-A Vol.50A(03-04) [March-April 2011]

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