Hydrazinyldiene-chroman-2,4-diones in inducing growth arrest and apoptosis in breast cancer cells: Synergism with doxorubicin and correlation with physicochemical properties
This study evaluates the effects of previously synthesized hydrazinyldiene-chroman-2,4-diones on cell proliferation and apoptosis, cell cycle distribution and migration capacity of MCF-7 breast cancer cells in synergy with doxorubicin. Physicochemical properties of the synthesized compounds were cor...
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| Format: | Article |
| Language: | English |
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Sciendo
2017-03-01
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| Series: | Acta Pharmaceutica |
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| Online Access: | https://doi.org/10.1515/acph-2017-0006 |
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| author | Ballazhi Lulzime Imeri Faik Jashari Ahmed Popovski Emil Stojković Goran Dimovski Aleksandar J. Mikhova Bozhana Mladenovska Kristina |
| author_facet | Ballazhi Lulzime Imeri Faik Jashari Ahmed Popovski Emil Stojković Goran Dimovski Aleksandar J. Mikhova Bozhana Mladenovska Kristina |
| author_sort | Ballazhi Lulzime |
| collection | DOAJ |
| description | This study evaluates the effects of previously synthesized hydrazinyldiene-chroman-2,4-diones on cell proliferation and apoptosis, cell cycle distribution and migration capacity of MCF-7 breast cancer cells in synergy with doxorubicin. Physicochemical properties of the synthesized compounds were correlated with their structure and activity. Significant cell viability decrease in comparison with the effect of doxorubicin alone and the reference 4-hydroxycoumarin was observed when combination treatment comprising doxorubicin and the title compounds was applied. Synergistic effect with doxorubicin was also observed in down-regulation of phospho-Thr308Akt levels, confirming reduced proliferation and increased apoptosis. Combined treatment increased the percentage of cells arrested at the G2/M stage. Additive inhibition of cell migration was also observed, pointing to the possibility of reducing the risk of metastases. With their solubility profile and log D7.4, all the synthesized compounds follow Lipinski’s rule of five for good permeability (absorption) potential. |
| format | Article |
| id | doaj-art-a1bbd0db50f1408586ed1dda2cec902b |
| institution | Kabale University |
| issn | 1846-9558 |
| language | English |
| publishDate | 2017-03-01 |
| publisher | Sciendo |
| record_format | Article |
| series | Acta Pharmaceutica |
| spelling | doaj-art-a1bbd0db50f1408586ed1dda2cec902b2025-02-02T12:11:59ZengSciendoActa Pharmaceutica1846-95582017-03-01671355210.1515/acph-2017-0006acph-2017-0006Hydrazinyldiene-chroman-2,4-diones in inducing growth arrest and apoptosis in breast cancer cells: Synergism with doxorubicin and correlation with physicochemical propertiesBallazhi Lulzime0Imeri Faik1Jashari Ahmed2Popovski Emil3Stojković Goran4Dimovski Aleksandar J.5Mikhova Bozhana6Mladenovska Kristina7Faculty of Pharmacy, Center of Biomolecular Pharmaceutical Analyses University “Ss Cyril and Methodius”, 1000 Skopje, Macedonia (the former Yugoslav Republic of)Institute of Physiology, University of Zürich, CH-8057, Zürich, SwitzerlandFaculty of Natural Sciences & Mathematics State University of Tetovo, 1200 Tetovo, Macedonia (the former Yugoslav Republic of)Institute of Chemistry, Faculty of Natural Sciences and Mathematics, University “Ss. Cyril and Methodius”, PO Box 162 1000 Skopje, Macedonia (the former Yugoslav Republic of)Institute of Chemistry, Faculty of Natural Sciences and Mathematics, University “Ss. Cyril and Methodius”, PO Box 162 1000 Skopje, Macedonia (the former Yugoslav Republic of)Faculty of Pharmacy, Center of Biomolecular Pharmaceutical Analyses University “Ss Cyril and Methodius”, 1000 Skopje, Macedonia (the former Yugoslav Republic of)Bulgarian Academy of Sciences Institute of Organic Chemistry with Centre of Phytochemistry, 1113 Sofia, BulgariaFaculty of Pharmacy, Center of Biomolecular Pharmaceutical Analyses University “Ss Cyril and Methodius”, 1000 Skopje, Macedonia (the former Yugoslav Republic of)This study evaluates the effects of previously synthesized hydrazinyldiene-chroman-2,4-diones on cell proliferation and apoptosis, cell cycle distribution and migration capacity of MCF-7 breast cancer cells in synergy with doxorubicin. Physicochemical properties of the synthesized compounds were correlated with their structure and activity. Significant cell viability decrease in comparison with the effect of doxorubicin alone and the reference 4-hydroxycoumarin was observed when combination treatment comprising doxorubicin and the title compounds was applied. Synergistic effect with doxorubicin was also observed in down-regulation of phospho-Thr308Akt levels, confirming reduced proliferation and increased apoptosis. Combined treatment increased the percentage of cells arrested at the G2/M stage. Additive inhibition of cell migration was also observed, pointing to the possibility of reducing the risk of metastases. With their solubility profile and log D7.4, all the synthesized compounds follow Lipinski’s rule of five for good permeability (absorption) potential.https://doi.org/10.1515/acph-2017-0006hydrazinyldiene chroman 2,4 dionesphysicochemical propertiesdoxorubicincytotoxicitybreast cancer cells |
| spellingShingle | Ballazhi Lulzime Imeri Faik Jashari Ahmed Popovski Emil Stojković Goran Dimovski Aleksandar J. Mikhova Bozhana Mladenovska Kristina Hydrazinyldiene-chroman-2,4-diones in inducing growth arrest and apoptosis in breast cancer cells: Synergism with doxorubicin and correlation with physicochemical properties Acta Pharmaceutica hydrazinyldiene chroman 2,4 diones physicochemical properties doxorubicin cytotoxicity breast cancer cells |
| title | Hydrazinyldiene-chroman-2,4-diones in inducing growth arrest and apoptosis in breast cancer cells: Synergism with doxorubicin and correlation with physicochemical properties |
| title_full | Hydrazinyldiene-chroman-2,4-diones in inducing growth arrest and apoptosis in breast cancer cells: Synergism with doxorubicin and correlation with physicochemical properties |
| title_fullStr | Hydrazinyldiene-chroman-2,4-diones in inducing growth arrest and apoptosis in breast cancer cells: Synergism with doxorubicin and correlation with physicochemical properties |
| title_full_unstemmed | Hydrazinyldiene-chroman-2,4-diones in inducing growth arrest and apoptosis in breast cancer cells: Synergism with doxorubicin and correlation with physicochemical properties |
| title_short | Hydrazinyldiene-chroman-2,4-diones in inducing growth arrest and apoptosis in breast cancer cells: Synergism with doxorubicin and correlation with physicochemical properties |
| title_sort | hydrazinyldiene chroman 2 4 diones in inducing growth arrest and apoptosis in breast cancer cells synergism with doxorubicin and correlation with physicochemical properties |
| topic | hydrazinyldiene chroman 2,4 diones physicochemical properties doxorubicin cytotoxicity breast cancer cells |
| url | https://doi.org/10.1515/acph-2017-0006 |
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