Please use this identifier to cite or link to this item: http://ir.swu.ac.th/jspui/handle/123456789/13933
Title: Investigation of aromatase inhibitory activity of metal complexes of 8-hydroxyquinolineand uracil derivatives
Authors: Prachayasittikul V.
Pingaew R.
Nantasenamat C.
Prachayasittikul S.
Ruchirawat S.
Prachayasittikul V.
Keywords: 3 (4,5 dimethyl 2 thiazolyl) 2,5 diphenyltetrazolium bromide
5 nitrouracil
8 quinolinol
aromatase
aromatase inhibitor
copper complex
doxorubicin
iodouracil
ketoconazole
letrozole
manganese derivative
metal complex
nickel complex
unclassified drug
uracil derivative
8 quinolinol
aromatase inhibitor
coordination compound
copper
letrozole
manganese
nickel
nitrile
triazole derivative
uracil
analytical equipment
antineoplastic activity
article
breast cancer
drug cytotoxicity
drug structure
embryo
enzyme assay
enzyme inhibition
human
human cell
IC 50
lung alveolus cell
structure analysis
cell line
chemistry
comparative study
cytology
drug effects
IC50
lung
Aromatase Inhibitors
Cell Line
Coordination Complexes
Copper
Humans
Inhibitory Concentration 50
Ketoconazole
Lung
Manganese
Nickel
Nitriles
Oxyquinoline
Triazoles
Uracil
Issue Date: 2014
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. © 2014 Prachayasittikul et al.
URI: https://www.scopus.com/inward/record.uri?eid=2-s2.0-84906242390&doi=10.2147%2fDDDT.S67300&partnerID=40&md5=d64004a46e7e454a5c2b0953427933b9
http://ir.swu.ac.th/jspui/handle/123456789/13933
ISSN: 11778881
Appears in Collections:SCOPUS 1983-2021

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