Abstract
The synthesis of several new pyrazole and indazole derivatives from acetophenone and tetralone substrates is reported. The bioactivities of the new compounds were evaluated through in vitro assays for endothelial cell proliferation and tube formation. Results herein indicate that the easily prepared compounds containing the indazole structural framework exhibit potent cytostatic properties against all cell lines tested, with compounds 13 and 14 being the most active displaying IC(50) values of 1.5 ± 0.4 µM and 5.6 ± 2.5 µM, respectively, against MCF-7 cells. In addition, the indazole derivative 16 was assessed as a competent inhibitor of endothelial tube formation at 30 µM.
Copyright © 2012 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.
MeSH terms
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Acetophenones / chemical synthesis
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Acetophenones / chemistry
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Acetophenones / pharmacology
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Angiogenesis Inhibitors / chemical synthesis
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Angiogenesis Inhibitors / chemistry
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Angiogenesis Inhibitors / pharmacology*
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Animals
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Breast Neoplasms / drug therapy
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Breast Neoplasms / pathology
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Cell Line, Tumor
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Cell Proliferation / drug effects*
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Endothelial Cells / drug effects
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Endothelial Cells / metabolism
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Female
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HeLa Cells
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Humans
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Indazoles / chemical synthesis
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Indazoles / chemistry
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Indazoles / pharmacology*
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Inhibitory Concentration 50
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Mice
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Pyrazoles / chemical synthesis
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Pyrazoles / chemistry
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Pyrazoles / pharmacology*
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Tetralones / chemical synthesis
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Tetralones / chemistry
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Tetralones / pharmacology
Substances
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Acetophenones
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Angiogenesis Inhibitors
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Indazoles
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Pyrazoles
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Tetralones