<abstract xmlns="http://www.w3.org/1999/xhtml"><p> The study highlights the current progress in the development of coumarin scaffolds for drug discovery as novel anticancer 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</p></abstract>

The study highlights the current progress in the development of coumarin scaffolds for drug discovery as novel anticancer 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

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

Institute of Pharmaceutical Chemistry Faculty of Pharmacy University »Ss. Cyril and Methodius« 1000 Skopje, Republic of Macedonia

Institute of Chemistry, Faculty of Natural Sciences and Mathematics University »Ss. Cyril and Methodius« PO Box 162, 1000 Skopje Republic of Macedonia

Faculty of Natural Sciences and Mathematics, State University of Tetovo 1200 Tetovo, Republic of Macedonia

Institute of Pharmacology University of Bern CH-3010 Bern, Switzerland

Faculty of Medical Sciences State University of Tetovo 1200 Tetovo, Republic of Macedonia

Institute of Organic Chemistry with Centre of Phytochemistry Bulgarian Academy of Sciences 1113 Sofia, Bulgaria

Acta Pharmaceutica

This work is licensed under the Creative Commons Attribution-NonCommercial-NoDerivatives 3.0 License.

The study highlights the current progress in the development of coumarin scaffolds for drug discovery as novel anticancer agents in metastatic breast cancer....

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

Publié en ligne: 11 mars 2015

Pages: 53 - 63

Reçu: 13 oct. 2014

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

Mots clés
chromandiones, breast cancer, metastatic cells, antiproliferative effect

© by Kristina Mladenovska

This work is licensed under the Creative Commons Attribution-NonCommercial-NoDerivatives 3.0 License.

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

Publié en ligne: 11 mars 2015

Pages: 53 - 63

Reçu: 13 oct. 2014

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

Mots cléschromandiones, breast cancer, metastatic cells, antiproliferative effect

© by Kristina Mladenovska

This work is licensed under the Creative Commons Attribution-NonCommercial-NoDerivatives 3.0 License.

Mots clés
chromandiones, breast cancer, metastatic cells, antiproliferative effect