Original scientific paper

https://doi.org/10.1515/acph-2015-0002

Potential antiproliferative effect of isoxazolo- and thiazolo coumarin derivatives on breast cancer mediated bone and lung metastases

LULZIME BALLAZHI ; Institute of Pharmaceutical Chemistry, Faculty of Pharmacy, University “Ss. Cyril and Methodius”, 1000 Skopje, Republic of Macedonia
EMIL POPOVSKI ; Institute of Chemistry, Faculty of Natural Sciences & Mathematics, University “Ss. Cyril & Methodius”, PO Box 162, 1000 Skopje, Republic of Macedonia
AHMED JASHARI ; Faculty of Natural Sciences & Mathematics, State University of Tetovo, 1200 Tetovo, Republic of Macedonia
FAIK IMERI ; Institute of Pharmacology, University of Bern, CH-3010 Bern, Switzerland
IBRAHIM IBRAHIMI ; Faculty of Medical Sciences, State University of Tetovo, 1200 Tetovo, Republic of Macedonia
BOZHANA MIKHOVA ; Institute of Organic Chemistry with Centre of Phytochemistry Bulgarian Academy of Sciences, 1113 Sofia, Bulgaria
KRISTINA MLADENOVSKA orcid.org/0000-0003-2503-4699 ; Institute of Pharmaceutical Chemistry, Faculty of Pharmacy, University “Ss. Cyril and Methodius”, 1000 Skopje, Republic of Macedonia

Abstract

The study highlights the current progress in the development of coumarin scaffolds for drug discovery as novel anti-cancer agents in metastatic breast cancer. Eight compounds, combining the coumarin core and five membered heterocycles (isoxazoles and thiazoles) in hydrazinyldiene-chroman-2,4-diones, were characterized in terms of a potential antiproliferative effect on bone (SCP1833) and lung (SCP4175) metastatic breast cancer cell lines using the 3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyltetrazolium bromide assay. Cell viability was evaluated after 48 and 72 h of treatment and the 50 % inhibitory concentrations were determined. The results demonstrated dose- and time-dependent activity, with the most potent molecules having a thiazole moiety, without or with additional methyl group(s) attached to the carbon(s) at position(s) 5 and/or 4 in the thiazole ring. These molecules possessed significantly higher potency against both test cell lines compared to 4-hydroxycoumarin.

Keywords

chromandiones; breast cancer; metastatic cells; antiproliferative effect

Hrčak ID:

128389

URI

https://hrcak.srce.hr/128389

Publication date:

31.3.2015.

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