H. Elsubbagh et Am. Alobaid, 2,4-DISUBSTITUTED THIAZOLES .2. A NOVEL CLASS OF ANTITUMOR AGENTS, SYNTHESIS AND BIOLOGICAL EVALUATION, European journal of medicinal chemistry, 31(12), 1996, pp. 1017-1021
A series of 2,4-disubstituted thiazole derivatives bearing N-n-butyl o
r N-cyclohexylthioureido synthon at position 2 and N-substituted thios
emicarbazone moiety at position 4 have been synthesized and tested for
antitumor activity using the National Cancer Institute's in-vitro-dis
ease-oriented antitumor screen. All of the tested compounds showed ant
ineoplastic activity at concentrations less than 100 mu M. Compounds 7
, 9, 15 and 17 in particular showed activity with GI(50) (mean-graph m
idpoint) of 17.8, 8.5, 9.5 and 7.4 mu M, respectively. The detailed sy
ntheses, spectroscopic and biological data are discussed.