摘要：A series of 1-(N-substituted-1H-indol-3-yl)-3-arylprop-2- -ene-1-ones (2a,b-4a,b) were prepared and allowed to react with urea,thiourea or guanidine to give pyrimidine derivatives 5a,b-13a,b.Reaction of 2a,b-4a,b with ethyl acetoacetate in the presence of a base gave cyclohexanone derivatives 14a,b-16a,b.Reaction of the latter compounds with hydrazine hydrate afforded indazole derivatives 17a,b-19a,b.On the other hand,reaction of 2a,b-4a,b with some hydrazine derivatives,namely hydrazine hydrate,acetyl hydrazine,phenylhydrazine and benzylhydrazine hydrochloride,led to the formation of pyrazole derivatives 20a,b-31a,b.Moreover,reaction of 2a,b-4a,b with hydroxylamine hydrochloride gave isoxazole derivatives 32a,b-34a,b.The newly synthesized compounds were tested for their antimicrobial activity and showed that 4-(N-ethyl-1H-indol-3-yl)-6-(p-chlorophenyl)-pyrimidine-2-amine (11b) was the most active of all the test compounds towards Candida albicans compared to the reference drug cycloheximide.Eighteen new compounds,namely pyrimidin-2(1H)-ones 5a,b-7a,b,pyrimidin-2(1H)- -thiones 8a,b-10a,b and pyrimidin-2-amines 11a,b-13a,b derivatives,were tested for their in vitro antiproliferative activity against HEPG2,MCF7 and HCT-116 cancer cell lines.4-(N-ethyl-1H-indol-3-yl)-6-(p-methoxyphenyl)-pyrimidin-2-amine (11a) was found to be highly active with IC50 of 0.7 mmol L–1.
