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Synthesis and Biological Activity of Some New Pyrazole Copper(II) Complexes

As a part of systematic investigation of synthesis and biologically active compounds of pyrazole derivatives containing transition metal, several new pyrazole copper(II) complexes 3a−f were synthesized from pyrazole sodium salts 2a−f, which were produced from spiro‐pyrazoles 1a−f and sodium hydride...

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Published in:Journal of heterocyclic chemistry 2012-09, Vol.49 (5), p.1218-1223
Main Authors: Maruoka, Hiroshi, Nishida, Sho, Kashige, Nobuhiro, Yoshimura, Yuki, Omori, Masahiko, Tomita, Ryoko, Masumoto, Eiichi, Okabe, Fumi, Miake, Fumio, Yamagata, Kenji, Fujioka, Toshihiro
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Language:English
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Summary:As a part of systematic investigation of synthesis and biologically active compounds of pyrazole derivatives containing transition metal, several new pyrazole copper(II) complexes 3a−f were synthesized from pyrazole sodium salts 2a−f, which were produced from spiro‐pyrazoles 1a−f and sodium hydride by a ring‐opening reaction. All the synthesized compounds were characterized by spectroscopic analysis. Pyrazole copper(II) complexes 3a−d and 3f exhibited high DNA cleavage activity in vitro. Furthermore, compounds 3a−f were tested for their growth inhibitory activity in A549 lung cancer, B16F10 murine melanoma, and HeLa human uterine carcinoma cells. Compounds 3c,d displayed moderate B16F10 and HeLa inhibitory activity levels (3c: IC50 = 45 μM in B16F10 cells and 34 μM in HeLa cells, 3d: IC50 = 50 μM in B16F10 cells and 32 μM in HeLa cells).
ISSN:0022-152X
1943-5193
DOI:10.1002/jhet.919