Synthesis and biological activity of novel 3-heteroaryl-2 H-pyrido[4,3- e][1,2,4]thiadiazine and 3-heteroaryl-2 H-benzo[ e][1,2,4]thiadiazine 1,1-dioxides

新型 3-杂芳基-2 H-吡啶并[4,3-e][1,2,4]噻二嗪和 3-杂芳基-2 H-苯并[e][1,2,4]噻二嗪 1,1-二氧化物的合成及生物活性

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作者:Katarzyna Gobis, Henryk Foks, Jarosłw Sławiński, Ewa Augustynowicz-Kopeć, Agnieszka Napiórkowska

Abstract

A series of novel 1,2,4-thiadiazine 1,1-dioxides were synthesized by condensation of 2-chlorobenzenesulfonamide and 4-chloropyridine-3-sulfonamide with heterocyclic methyl carbimidates obtained from heterocyclic carbonitriles and used at the time of their creation. Substituted amidines were isolated as the intermediates in the reaction with 2-chlorobenzenesulfonamide. Those intermediates were successfully cyclized to corresponding 1,2,4-thiadiazine 1,1-dioxides in pyridine with the addition of DBU. The newly synthesized compounds were evaluated for their tuberculostatic and anticancer activities. Eight compounds were able to inhibit the growth of some renal and non-small cell lung cancer cell lines.

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