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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 id orcid.org/0000-0003-2503-4699 ; Institute of Pharmaceutical Chemistry, Faculty of Pharmacy, University “Ss. Cyril and Methodius”, 1000 Skopje, Republic of Macedonia


Puni tekst: engleski pdf 1.211 Kb

str. 53-63

preuzimanja: 803

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Sažetak

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.

Ključne riječi

chromandiones; breast cancer; metastatic cells; antiproliferative effect

Hrčak ID:

128389

URI

https://hrcak.srce.hr/128389

Datum izdavanja:

31.3.2015.

Posjeta: 2.536 *