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A variety of heterocycles of synthetic and biological importance were prepared from 3-(indol-3-ylmethylene)-5-phenyl-2(3 H )-furanone ( 1 ) and its hydrazide 2 . Compounds 1 and 2 were used for the construction of pyridazin-3(4 H )-ones 4 and 6 ; 1,3,4-oxadiazoles 7 , 8 , and 10 ; and 1,2,4 -triazoles 12 , 14 , and 15 , all bearing a 3-indolyl moiety. The antimicrobial activities of the synthesized compounds were examined against six types of bacteria and two types of fungi.

A novel class of 6-indolypyridine-3-carbonitrilile derivatives were synthesized and evaluated for antiproliferative activities to establish structure-activity relationship. The synthesis was carried out through one-pot multicomponent reaction of 3-acetylindole, aromatic aldehydes, ethyl cyanoacetate, and ammonium acetate in the presence of piperidine as a catalyst, using a microwave irradiation method or a traditional thermal method. This was followed by chlorination for compounds 13a–e and subsequent nucleophilic substitution of the chlorine group by ethylenediamine at C2 position of the pyridine ring. The antiproliferative activity of these new nicotinonitriles was evaluated against human ovarian adenocarcinoma (SK-OV-3), breast adenocarcinoma (MCF-7), and cervix adenocarcinoma (HeLa) cells. Among all compounds, 2-((2-aminoethyl)amino)-4-aryl-6-indolylnicotinonitriles series (15a, 15b, 15d, and 15e) exhibited higher antiproliferative activity cells with IC50 values of 4.1–13.4 μM.