Reference

2,4-Disubstituted thiazoles

2,4-Disubstituted thiazoles. II. A novel class of antitumor agents, synthesis and biological evaluation.In this study， 5398-36-7 and 186750-98-1 are also used. El-Subbagh, H. I.; Al-Obaid, A. M. (College Pharmacy, King Saud Univ., Riyadh 11451, Saudi Arabia). European Journal of Medicinal Chemistry, 31(12), 1017-1021 (English) 1996 Elsevier. CODEN: EJMCA5. ISSN: 0223-5234. DOCUMENT TYPE: Journal CA Section: 28 (Heterocyclic Compounds (More Than One Hetero Atom)) Section cross-reference(s): 1 A series of 2,4-disubstituted thiazole derivs., I (R = n-Bu, c-C6H11, X = SO2, CO) and II (R' = Et, c-C6H11, Ph, PhCH2), bearing an N-Bu or N-cyclohexylthioureido synthon at position 2 and an N-substituted thiosemicarbazone moiety at position 4 have been synthesized and tested for antitumor activity using the National Cancer Institute's in-vitro-disease-oriented antitumor screen. All of the tested compds. showed antineoplastic activity at concns. less than 100 mM. Compds. I (R = n-Bu, cyclohexyl, X = CO) and II (R = cyclohexyl, R' = Et; R = R' = cyclohexyl) in particular showed activity with GI50 (mean-graph midpoint) of 17.8, 8.5, 9.5 and 7.4 mM, resp. The detailed syntheses, spectroscopic, and biol. data are discussed. .