Phenothiazines Modified with the Pyridine Ring as Promising Anticancer Agents
Azaphenothiazines are the largest and most perspective group of modified phenothiazines, and they exhibit variety of biological activities. The review sums up the current knowledge on the anticancer activity of isomeric pyridobenzothiazines and dipyridothiazines, which are modified azaphenothiazines...
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| Format: | Article |
| Language: | English |
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MDPI AG
2021-03-01
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| Series: | Life |
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| Online Access: | https://www.mdpi.com/2075-1729/11/3/206 |
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| author | Beata Morak-Młodawska Małgorzata Jeleń Krystian Pluta |
| author_facet | Beata Morak-Młodawska Małgorzata Jeleń Krystian Pluta |
| author_sort | Beata Morak-Młodawska |
| collection | DOAJ |
| description | Azaphenothiazines are the largest and most perspective group of modified phenothiazines, and they exhibit variety of biological activities. The review sums up the current knowledge on the anticancer activity of isomeric pyridobenzothiazines and dipyridothiazines, which are modified azaphenothiazines with one and two pyridine rings, respectively, against 10 types of cancer cell lines. Some 10-substituted dipyridothiazines and even 10-unsubstituted parent compounds, such as 10<i>H</i>-1,9-diazaphenothiazine and 10<i>H</i>-3,6-diazaphenothiazine, exhibited very potent action with the IC<sub>50</sub> values less than 1 µg/mL and 1 µM against selected cancer cell lines. The strength of the anticancer action depends both on the tricyclic ring scaffolds and the substituents at the thiazine nitrogen atom. The review discusses the kind of the substituents, nature of tricyclic ring scaffolds with the location of the azine nitrogen atoms, the types of the cancer cell lines, and the mechanism of action. |
| first_indexed | 2024-03-09T05:18:11Z |
| format | Article |
| id | doaj.art-7d2695b638ce4ee1ae2d7479d51bad19 |
| institution | Directory Open Access Journal |
| issn | 2075-1729 |
| language | English |
| last_indexed | 2024-03-09T05:18:11Z |
| publishDate | 2021-03-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Life |
| spelling | doaj.art-7d2695b638ce4ee1ae2d7479d51bad192023-12-03T12:43:14ZengMDPI AGLife2075-17292021-03-0111320610.3390/life11030206Phenothiazines Modified with the Pyridine Ring as Promising Anticancer AgentsBeata Morak-Młodawska0Małgorzata Jeleń1Krystian Pluta2Department of Organic Chemistry, Faculty of Pharmaceutical Sciences, The Medical University of Silesia, Jagiellońska 4, 41-200 Sosnowiec, PolandDepartment of Organic Chemistry, Faculty of Pharmaceutical Sciences, The Medical University of Silesia, Jagiellońska 4, 41-200 Sosnowiec, PolandDepartment of Organic Chemistry, Faculty of Pharmaceutical Sciences, The Medical University of Silesia, Jagiellońska 4, 41-200 Sosnowiec, PolandAzaphenothiazines are the largest and most perspective group of modified phenothiazines, and they exhibit variety of biological activities. The review sums up the current knowledge on the anticancer activity of isomeric pyridobenzothiazines and dipyridothiazines, which are modified azaphenothiazines with one and two pyridine rings, respectively, against 10 types of cancer cell lines. Some 10-substituted dipyridothiazines and even 10-unsubstituted parent compounds, such as 10<i>H</i>-1,9-diazaphenothiazine and 10<i>H</i>-3,6-diazaphenothiazine, exhibited very potent action with the IC<sub>50</sub> values less than 1 µg/mL and 1 µM against selected cancer cell lines. The strength of the anticancer action depends both on the tricyclic ring scaffolds and the substituents at the thiazine nitrogen atom. The review discusses the kind of the substituents, nature of tricyclic ring scaffolds with the location of the azine nitrogen atoms, the types of the cancer cell lines, and the mechanism of action.https://www.mdpi.com/2075-1729/11/3/206pirydobenzothiazinesdipyridothiazinesanticancer agentsgens analysisapoptosis |
| spellingShingle | Beata Morak-Młodawska Małgorzata Jeleń Krystian Pluta Phenothiazines Modified with the Pyridine Ring as Promising Anticancer Agents Life pirydobenzothiazines dipyridothiazines anticancer agents gens analysis apoptosis |
| title | Phenothiazines Modified with the Pyridine Ring as Promising Anticancer Agents |
| title_full | Phenothiazines Modified with the Pyridine Ring as Promising Anticancer Agents |
| title_fullStr | Phenothiazines Modified with the Pyridine Ring as Promising Anticancer Agents |
| title_full_unstemmed | Phenothiazines Modified with the Pyridine Ring as Promising Anticancer Agents |
| title_short | Phenothiazines Modified with the Pyridine Ring as Promising Anticancer Agents |
| title_sort | phenothiazines modified with the pyridine ring as promising anticancer agents |
| topic | pirydobenzothiazines dipyridothiazines anticancer agents gens analysis apoptosis |
| url | https://www.mdpi.com/2075-1729/11/3/206 |
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