Simple jQuery Dropdowns
Please use this identifier to cite or link to this item: http://repository.li.mahidol.ac.th/dspace/handle/123456789/41851
Title: Copper complexes of 8-aminoquinoline and uracils as novel aromatase inhibitors
Authors: Nujarin Sinthupoom
Virapong Prachayasittikul
Veda Prachayasittikul
Ratchanok Pingaew
Apilak Worachartcheewan
Supaluk Prachayasittikul
Somsak Ruchirawat
Mahidol University
Srinakharinwirot University
Chulabhorn Research Institute
Thailand Ministry of Education
Keywords: Biochemistry, Genetics and Molecular Biology
Issue Date: 1-Aug-2017
Citation: Letters in Drug Design and Discovery. Vol.14, No.8 (2017), 880-884
Abstract: © 2017 Bentham Science Publishers. 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.
URI: https://www.scopus.com/inward/record.uri?partnerID=HzOxMe3b&scp=85027875828&origin=inward
http://repository.li.mahidol.ac.th/dspace/handle/123456789/41851
ISSN: 1875628X
15701808
Appears in Collections:Scopus 2016-2017

Files in This Item:
There are no files associated with this item.


Items in DSpace are protected by copyright, with all rights reserved, unless otherwise indicated.