Morak-Młodawska Beata, Jeleń Małgorzata, Pluta Krystian
Department of Organic Chemistry, Faculty of Pharmaceutical Sciences, The Medical University of Silesia, Jagiellońska 4, 41-200 Sosnowiec, Poland.
Life (Basel). 2021 Mar 5;11(3):206. doi: 10.3390/life11030206.
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 10-1,9-diazaphenothiazine and 10-3,6-diazaphenothiazine, exhibited very potent action with the IC 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.
氮杂吩噻嗪是修饰吩噻嗪中最大且最具前景的一类，它们具有多种生物活性。本综述总结了关于异构吡啶并苯并噻嗪和二吡啶并噻嗪（分别为带有一个和两个吡啶环的修饰氮杂吩噻嗪）对10种癌细胞系的抗癌活性的现有知识。一些10-取代的二吡啶并噻嗪甚至10-未取代的母体化合物，如10-1,9-二氮杂吩噻嗪和10-3,6-二氮杂吩噻嗪，对选定的癌细胞系表现出非常强的活性，IC值小于1 µg/mL和1 µM。抗癌作用的强度既取决于三环骨架，也取决于噻嗪氮原子上的取代基。本综述讨论了取代基的种类、带有嗪氮原子位置的三环骨架的性质、癌细胞系的类型以及作用机制。
