<abstract xml:lang="en" xmlns="http://www.w3.org/1999/xhtml">A series of new benzothiazole derivatives <bold>6a-h</bold> have been synthesized, in five steps, from substituted phenols <italic>via</italic> the 1,3,4-oxadiazole-2-thiones <bold>5a-h.</bold> The <italic>in vitro</italic> antitumor activity of the compounds obtained was investigated and the benzothiazol derivatives <bold>6d</bold> and <bold>6e</bold> showed strong effects on leukaemia cell lines CCRF-CEM (CC50 = 12 ± 2 μmol L-1, 8 ± 1 μmol L-1, respectively). These compounds are leading candidates for further development. The title compounds were tested against representatives of several virus families containing single stranded RNA genomes, either positive-sense (ssRNA+), or negativesense (RNA-), and against double-stranded RNA genomes (dsRNA), as well as some <italic>Flaviviridae</italic> viruses.</abstract>

A series of new benzothiazole derivatives 6a-h have been synthesized, in five steps, from substituted phenols via the 1,3,4-oxadiazole-2-thiones 5a-h. The in vitro antitumor activity of the compounds obtained was investigated and the benzothiazol derivatives 6d and 6e showed strong effects on leukaemia cell lines CCRF-CEM (CC50 = 12 ± 2 μmol L-1, 8 ± 1 μmol L-1, respectively). These compounds are leading candidates for further development. The title compounds were tested against representatives of several virus families containing single stranded RNA genomes, either positive-sense (ssRNA+), or negativesense (RNA-), and against double-stranded RNA genomes (dsRNA), as well as some Flaviviridae viruses.

<italic>In vitro</italic> antitumor and antiviral activities of new benzothiazole and 1,3,4-oxadiazole-2-thione derivatives

Department of Chemistry, Quaid-I-Azam University, Islamabad-45320, Pakistan

Fachbereich Chemie Universität, Konstanz Postfach 5560, D-78457 Konstanz Germany (formerly)

Department of Biomedical Sciences and Technologies, University of Cagliari, Cittadella Universitaria 09042 Monserrato (CA), Italy

Acta Pharmaceutica

 antitumor and antiviral activities of new benzothiazole and 1,3,4-oxadiazole-2-thione derivatives

A series of new benzothiazole derivatives 6a-h have been synthesized, in five steps, from substituted phenols via the 1,3,4-oxadiazole-2-thiones 5a-h. The in...

In vitro antitumor and antiviral activities of new benzothiazole and 1,3,4-oxadiazole-2-thione derivatives

Publicado en línea: 30 may 2008

Páginas: 135 - 149

DOI: https://doi.org/10.2478/v10007-008-0007-2

Palabras clave
1,3,4-oksatiazoli, supstituirani benzotiazoli, antitumorsko djelovanje, antivirusno djelovanje

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