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A new series of 6-aryl-5-cyano thiouracil derivatives were synthesized. Cyanouracil1was condensed with monochloroacetic acid and different aldehydes to give thiazolopyrimidine2. On the other hand, treatment of cyanouracil1with 2-chloro-N-substituted-phenylac etamide afforded4. Hydrazinolysis of6afforded the hydrazino derivatives7which upon reaction with different electrophilic reagents such as acetic anhydride, benzoyl chloride, and carbon disulfide yielded pyrimidine derivatives8–15. Some of the new derivatives were explored for their antimicrobial activities. Compounds7and9have a promising activity, relatively equipotent to the reference drug. All of the new synthesized compounds were testedin vitrofor their antiproliferative activities against HePG-2 and MCF-7 cell lines. Compounds7,9, and2ddisplayed potent growth inhibitory effect toward the two cell lines more than the standard drug 5-FU. Furthermore, a docking study of the most active compounds was performed with thymidylate synthase enzyme. [ABSTRACT FROM AUTHOR]