SYNTHESIS, CHARACTERIZATION AND ANTICANCER EVALUATION OF NOVEL SUBSTITUTED-[1, 3, 4]-THIADIAZOLE DERIVATIVES
Dr. Faruk Alam* and Dr. Biplab Kumar Dey
series of 1-(substituted phenyl)-3-[5-(2-substitutedphenyl)-1, 3, 4-thiadiazol-2yl] urea derivatives Cp1-Cp6 have been prepared by reaction of 5-(substituted phenyl)-2-amino - [1, 3, 4]-thiadiazole and an appropriate phenyl isocyanate. Further meta and para- chloro phenyl derivatives were synthesized in order to study the effect of these substituents on antitumor activity. Structures of these compounds were established by IR, 1HNMR, Mass spectroscopy and CHN analysis. All six compounds were used for anticancer activity by using EAC cells (0.2 ml of 2 x 106 cells/mice) panel. Among the compounds tested, N-(4-chlorophenyl)-3-[5-(2-hydroxy phenyl)-1,3,4-thiadiazol-2-yl]urea,Cp2 was found to be the most active candidate of the series at five dose level screening with degree of selectivity toward EAC cancer cell line.
Keywords: Synthesis, 1, 3, 4-thiadiazole, anti tumor agents, EAC cell.
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