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Bioorg Med Chem Lett. 2013 Jun 15;23(12):3523-30. doi: 10.1016/j.bmcl.2013.04.039. Epub 2013 Apr 25.

Design, synthesis, quantum chemical studies and biological activity evaluation of pyrazole-benzimidazole derivatives as potent Aurora A/B kinase inhibitors.

Author information

1
School of Pharmacy, Xuzhou Medical College, Xuzhou 221004, China.

Erratum in

  • Bioorg Med Chem Lett. 2013 Aug 1;23(15):4471. Jin, Min [corrected to Ji, Min].

Abstract

Novel pyrazole-benzimidazole derivatives have been designed and synthesized. The entire target compounds were determined against cancer cell lines U937, K562, A549, LoVo and HT29 and were screened for Aurora A/B kinase inhibitory activity in vitro. The compounds 7a, 7b, 7i, 7k and 7l demonstrated significant cancer cell lines and Aurora A/B kinase inhibitory activities. Molecular modeling studies suggested the derivatives have bound in the active site of Aurora A kinase through the formation of four hydrogen bonds. Quantum chemical studies were carried out on these compounds to understand the structural features essential for activity. The cellular activity of 7k was also tested by immunofluorescence.

PMID:
23664099
DOI:
10.1016/j.bmcl.2013.04.039
[Indexed for MEDLINE]

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