Copper Complexes of 8-Aminoquinoline and Uracils as Novel Aromatase Inhibitors

Title:Copper Complexes of 8-Aminoquinoline and Uracils as Novel Aromatase Inhibitors

Volume: 14 Issue: 8

Author(s): Nujarin Sinthupoom, Veda Prachayasittikul, Ratchanok Pingaew, Apilak Worachartcheewan, Supaluk Prachayasittikul*, Somsak Ruchirawat and Virapong Prachayasittikul*

Affiliation:

• Center of Data Mining and Biomedical Informatics, Faculty of Medical Technology, Mahidol University, Bangkok 10700,Thailand

• Department of Clinical Microbiology and Applied Technology, Faculty of Medical Technology, Mahidol University, Bangkok 10700,Thailand

Keywords: 8-Aminoquinoline, uracil, metal complex, aromatase inhibitor, cytotoxicity, cancer treatment.

Abstract: Background: Currently, aromatase inhibitors (AIs) have been developed for the treatment of breast cancers and other estrogen-related conditions. However, searching for more and new classes of AIs is being investigated. 8-Aminoquinoline (8AQ) is an interesting scaffold to be explored. In particular, 8AQ as its mixed ligands (5-nitrouracil, 5Nu and 5-iodouracil, 5Iu) metal complexes are potential compounds to be studied.

Objective: Metal complexes of 8AQ-5Nu/5Iu were investigated for aromatase inhibitory activity and cytotoxicity.

Methods: Metal complexes (1-6) and free ligands were evaluated for aromatase inhibitory and cytotoxic activities. Aromatase inhibitory activity of the metal complexes was performed according to a guideline of BD Gentest™ kit using CYP19 enzyme and O-benzyl fluorescein (DBF) as a substrate. Cytotoxic effect of the compounds was tested against normal embryonic lung cell line (MRC) using the MTT assay.

Results: Significantly, copper complexes 3 (IC50 = 0.7 μM) and 6 (IC50 = 1.7 μM) were shown to be active aromatase inhibitors with selectivity indices of 24.74 and16.40, respectively.

Conclusion: Copper complexes of 8AQ-5Nu (3) and of 8AQ-5Iu (6) were highlighted as novel aromatase inhibitors that could be further developed for therapeutic applications.

Cite this article as:

Sinthupoom Nujarin, Prachayasittikul Veda, Pingaew Ratchanok, Worachartcheewan Apilak, Prachayasittikul Supaluk*, Ruchirawat Somsak and Prachayasittikul Virapong*, Copper Complexes of 8-Aminoquinoline and Uracils as Novel Aromatase Inhibitors, Letters in Drug Design & Discovery 2017; 14 (8) . https://dx.doi.org/10.2174/1570180813666161103144822

DOI https://dx.doi.org/10.2174/1570180813666161103144822	Print ISSN 1570-1808
Publisher Name Bentham Science Publisher	Online ISSN 1875-628X