2,4-DISUBSTITUTED THIAZOLES .2. A NOVEL CLASS OF ANTITUMOR AGENTS, SYNTHESIS AND BIOLOGICAL EVALUATION

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.