The synthesis of a series of 2-arylamido and 2-alkylamido derivatives of 2-amino-4-(isothiocyanatomethyl)thiazole and 2-amino-4-(isothiocyanatomethyl)selenazole is described. In vitro antiproliferative evaluations were carried out using L1210 cells. The 2-(alkylamido)thiazole derivatives were moderately antiproliferative, with IC50's of 4–8 µM. A significant increase in activity was obtained for the arylamido derivatives, with IC50's of 0.2–1 µM. The results obtained for the selenazoles were similar to those for the thiazoles. 2-Benzamido-4-(isothiocyanatomethyl)-thiazole (19) was found to be a potent inhibitor of GMP synthetase. None of the compounds prepared in this study demonstrated antifilarial activity.
|Original language||English (US)|
|Number of pages||4|
|Journal||Journal of medicinal chemistry|
|State||Published - 1993|
ASJC Scopus subject areas
- Molecular Medicine
- Drug Discovery