Potential antiproliferative effect of isoxazolo- and thiazolo coumarin derivatives on breast cancer mediated bone and lung metastases
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...
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| Format: | Article |
| Language: | English |
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Sciendo
2015-03-01
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| Series: | Acta Pharmaceutica |
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| Online Access: | https://doi.org/10.1515/acph-2015-0002 |
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| author | Ballazhi Lulzime Popovski Emil Jashari Ahmed Imeri Faik Ibrahimi Ibrahim Mikhova Bozhana Mladenovska Kristina |
| author_facet | Ballazhi Lulzime Popovski Emil Jashari Ahmed Imeri Faik Ibrahimi Ibrahim Mikhova Bozhana Mladenovska Kristina |
| author_sort | Ballazhi Lulzime |
| collection | DOAJ |
| description | 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 |
| format | Article |
| id | doaj-art-540062d9547a427191e9bf5bfb782107 |
| institution | Kabale University |
| issn | 1846-9558 |
| language | English |
| publishDate | 2015-03-01 |
| publisher | Sciendo |
| record_format | Article |
| series | Acta Pharmaceutica |
| spelling | doaj-art-540062d9547a427191e9bf5bfb7821072025-02-02T12:44:02ZengSciendoActa Pharmaceutica1846-95582015-03-01651536310.1515/acph-2015-0002acph-2015-0002Potential antiproliferative effect of isoxazolo- and thiazolo coumarin derivatives on breast cancer mediated bone and lung metastasesBallazhi Lulzime0Popovski Emil1Jashari Ahmed2Imeri Faik3Ibrahimi Ibrahim4Mikhova Bozhana5Mladenovska Kristina6Institute of Pharmaceutical Chemistry Faculty of Pharmacy University »Ss. Cyril and Methodius« 1000 Skopje, Republic of MacedoniaInstitute of Chemistry, Faculty of Natural Sciences and Mathematics University »Ss. Cyril and Methodius« PO Box 162, 1000 Skopje Republic of MacedoniaFaculty of Natural Sciences and Mathematics, State University of Tetovo 1200 Tetovo, Republic of MacedoniaInstitute of Pharmacology University of Bern CH-3010 Bern, SwitzerlandFaculty of Medical Sciences State University of Tetovo 1200 Tetovo, Republic of MacedoniaInstitute of Organic Chemistry with Centre of Phytochemistry Bulgarian Academy of Sciences 1113 Sofia, BulgariaInstitute of Pharmaceutical Chemistry Faculty of Pharmacy University »Ss. Cyril and Methodius« 1000 Skopje, Republic of MacedoniaThe 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-hydroxycoumarinhttps://doi.org/10.1515/acph-2015-0002chromandionesbreast cancermetastatic cellsantiproliferative effect |
| spellingShingle | Ballazhi Lulzime Popovski Emil Jashari Ahmed Imeri Faik Ibrahimi Ibrahim Mikhova Bozhana Mladenovska Kristina Potential antiproliferative effect of isoxazolo- and thiazolo coumarin derivatives on breast cancer mediated bone and lung metastases Acta Pharmaceutica chromandiones breast cancer metastatic cells antiproliferative effect |
| title | Potential antiproliferative effect of isoxazolo- and thiazolo coumarin derivatives on breast cancer mediated bone and lung metastases |
| title_full | Potential antiproliferative effect of isoxazolo- and thiazolo coumarin derivatives on breast cancer mediated bone and lung metastases |
| title_fullStr | Potential antiproliferative effect of isoxazolo- and thiazolo coumarin derivatives on breast cancer mediated bone and lung metastases |
| title_full_unstemmed | Potential antiproliferative effect of isoxazolo- and thiazolo coumarin derivatives on breast cancer mediated bone and lung metastases |
| title_short | Potential antiproliferative effect of isoxazolo- and thiazolo coumarin derivatives on breast cancer mediated bone and lung metastases |
| title_sort | potential antiproliferative effect of isoxazolo and thiazolo coumarin derivatives on breast cancer mediated bone and lung metastases |
| topic | chromandiones breast cancer metastatic cells antiproliferative effect |
| url | https://doi.org/10.1515/acph-2015-0002 |
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