Synthesis and Anticancer Activity of Some Novel 1h-Pyrazol-5(4H)-One Derivatives.

Refluxing pyrazolone with aromatic aldehydes in ethanol and in the presence of catalytic amount of piperidine afforded the Shift's bases 2a-e. When pyrazolone derivative 1 react with different diazonium salts, compounds 3a-c were obtained. On the other hand, glycosides 4a-c were produced when derivative 1 heated under reflux with different aldohexoses and aldopentoses in dioxane and few drops of piperdine. On treatment of compound 1 with phosphorous penta sulfide in dry pyridine, the thione derivative was obtained. When the potassium salt of the latter compound was stirred at room temperature with either semi sugars or tetra acetylated bromo sugars in dry DMF, compounds 7a-d and 8a, b were obtained respectively. Six out of the prepared compounds had been directed to anti-tumor activities against three human cancer cell lines using MTT assay. Two compounds showed good anticancer activities.