Publication:
Investigation of aromatase inhibitory activity of metal complexes of 8-hydroxyquinolineand uracil derivatives

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0

Issued Date

2014

Resource Type

Article

File Type

application/pdf

ISSN

11778881

DOI

10.2147/DDDT.S67300

Other identifier(s)

2-s2.0-84906242390

Rights Holder(s)

มหาวิทยาลัยศรีนครินทรวิโรฒ

Bibliographic Citation

Drug Design, Development and Therapy. Vol 8, (2014), p.1089-1096

Suggested Citation

Prachayasittikul V., Pingaew R., Nantasenamat C., Prachayasittikul S., Ruchirawat S., Prachayasittikul V. Investigation of aromatase inhibitory activity of metal complexes of 8-hydroxyquinolineand uracil derivatives. Drug Design, Development and Therapy. Vol 8, (2014), p.1089-1096. doi:10.2147/DDDT.S67300 Retrieved from: https://hdl.handle.net/20.500.14740/6465

Title

Investigation of aromatase inhibitory activity of metal complexes of 8-hydroxyquinolineand uracil derivatives

Author(s)

Prachayasittikul V.
 Pingaew R.
 Nantasenamat C.
 Prachayasittikul S.
 Ruchirawat S.
 Prachayasittikul V.

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.

Subject(s)

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

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URI

https://hdl.handle.net/20.500.14740/6465

Collections

Scopus: Year 1983-2021

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