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Title: Investigation of aromatase inhibitory activity of metal complexes of 8-hydroxyquinoline and uracil derivatives
Authors: Veda Prachayasittikul
Ratchanok Pingaew
Virapong Prachayasittikul
Chanin Nantasenamat
Somsak Ruchirawat
Supaluk Prachayasittikul
Mahidol University. Faculty of Medical Technology. Department of Clinical Microbiology and Applied Technology
Mahidol University. Faculty of Medical Technology. Center of Data Mining and Biomedical Informatics
Keywords: anticancer;metal-based compound;aromatase inhibitor
Issue Date: 14-Aug-2014
Citation: Drug Design, Development and Therapy. Vol.8, 2014, 1089-1096
Abstract: Purpose: Estrogens play important roles in the pathogenesis and progression of breast cancer as well as estrogen-related diseases. Aromatase is a key enzyme in the rate-limiting step of estrogen production, in which its inhibition is one strategy for controlling estrogen levels to improve prognosis of estrogen-related cancers and diseases. Herein, a series of metal (Mn, Cu, and Ni) complexes of 8-hydroxyquinoline (8HQ) and uracil derivatives (4–9) were investigated for their aromatase inhibitory and cytotoxic activities. Methods: The aromatase inhibition assay was performed according to a Gentest™ kit using CYP19 enzyme, wherein ketoconazole and letrozole were used as reference drugs. The cytotoxicity was tested on normal embryonic lung cells (MRC-5) using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay. Results: Only Cu complexes (6 and 9) exhibited aromatase inhibitory effect with IC50 0.30 and 1.7 µM, respectively. Cytotoxicity test against MRC-5 cells showed that Mn and Cu complexes (5 and 6), as well as free ligand 8HQ, exhibited activity with IC50 range 0.74–6.27 µM. Conclusion: Cu complexes (6 and 9) were found to act as a novel class of aromatase inhibitor. Our findings suggest that these 8HQ–Cu–uracil complexes are promising agents that could be potentially developed as a selective anticancer agent for breast cancer and other estrogen-related diseases.
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