title: Synthesis and biological activity of novel 3-heteroaryl-2H-pyrido[4,3-e][1,2,4]thiadiazine and 3-heteroaryl-2H-benzo[e][1,2,4]thiadiazine 1,1-dioxides.
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.
authors.affiliation: Department of Organic Chemistry, Medical University of Gdańsk, Gdańsk, Poland.
authors.forename: Katarzyna
authors.initials: K
authors.lastname: Gobis
authors.affiliation: Department of Organic Chemistry, Medical University of Gdańsk, Gdańsk, Poland.
authors.forename: Henryk
authors.initials: H
authors.lastname: Foks
authors.affiliation: Department of Organic Chemistry, Medical University of Gdańsk, Gdańsk, Poland.
authors.forename: Jarosłw
authors.initials: J
authors.lastname: Sławiński
authors.affiliation: Department of Microbiology, Institute of Tuberculosis and Pulmonary Diseases, Warsaw, Poland.
authors.forename: Ewa
authors.initials: E
authors.lastname: Augustynowicz-Kopeć
authors.affiliation: Department of Microbiology, Institute of Tuberculosis and Pulmonary Diseases, Warsaw, Poland.
authors.forename: Agnieszka
authors.initials: A
authors.lastname: Napiórkowska
keywords: Anticancer activity; Heterocycles; Structure–activity relationship; Sulfonamidine; Synthesis