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2-Arylbenzothiazoles: Advances in Anti-Cancer and Diagnostic Pharmaceuticals Discovery

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Abstract

This review summarizes and analyzes published medicinal chemistry data regarding physiologically active 2-arylbenzothiazoles – a promising class of antiproliferative agents and potential diagnostic agents for Alzheimer’s disease. The data have been examined in the light of SAR approach to the properties of 2-arylbenzothiazoles and substances bioactivation mechanisms using labeled radiopharmaceuticals. The most promising leaders-in-class for which clinical trials have been recommended or conducted have been highlighted. Synthetic methods for the preparation of 2-arylbenzothiazoles as precursors of new-generation drugs have been analyzed in detail. Various methods for the preparation of fluorine-containing 2-arylbenzothiazoles, including synthetic pathway to antiproliferative drugs PMX 610, 5-F 203, and Phortress have been described. 2-Arylbenzothiazoles future application in biology and medicine has been discussed.

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Studentsov, E.P., Golovina, A.A., Krasikova, R.N. et al. 2-Arylbenzothiazoles: Advances in Anti-Cancer and Diagnostic Pharmaceuticals Discovery. Russ J Gen Chem 91, 1–33 (2021). https://doi.org/10.1134/S1070363221010011

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