Synthesis and Antitumor Screening of Novel 3-Phenylthiazolo [4,5-d]pyrimidin-2-thione Derivatives

Abstract

A series of new derivatives of 3-phenylthiazolo[4,5-d]pyrimidine-2-thiones were synthesized by the cyclization of 4-amino-5-alkyl(aryl) carboxamido-2,3-dihydrothiazolo-2-thione with aromatic aldehydes. Amine moieties were substituted in position 7 of the obtained bicyclic compounds. The synthesized compounds were characterized by elemental analysis, IR, ¹H-NMR, and ¹³C-NMR spectral data. Some of the newly synthesized compounds were selected by the US National Cancer Institute for in vitro antitumor screening. The two compounds 3d 7-chloro-5-(4-fluorophenyl)-3-phenyl-4,5-di-hydro-3H-thiazolo[4,5-(flpyrimidine-2-thione and 4i 5-(2-chlorophenyl)-7-(4-fluorobenzylamino)-3-phenyl-4,5-dihydro-3H-thiazolo[4,5-d]pyrimidine-2-thione proved to be the most active in the present study and their antitumor activities against 60 human tumor cell lines were described.

Key words

Antitumor agents - Thiazolo[4,5-d]pyrimidines, in vitro studies, synthesis

• References

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