One-Pot Multi-Component Synthesis and Biological Evaluation of Novel Indole-Pyrimidine Derivatives as Potent Anti-Cancer and Anti-Microbial Agents

A series of novel hybrids of indole-pyrimidine moieties were synthesized and evaluated for their in vitro anti-cancer, in vitro anti-bacteria and in vitro anti-fungal activities. The results showed that most of these compounds possessed significant cytotoxic potency against four cancer cell lines, HeLa, HEK 293T and MCF-7. The compounds 4-(3-(benzyloxy)phenyl)-6-(1-methyl-1 H -indol-3-yl)pyrimidin-2-amine,4-(4-chlorophenyl)-6-(1-methyl-1 H -indol-3-yl) pyrimidin-2-amine and4-(1 H -indole-3-yl)-6-phenylpyrimidin-2-amine showed good activity against HEK 293T. The compounds 4-(3-(benzyloxy)phenyl)-6-(1-methyl-1 H -indol-3-yl)pyrimidin-2-amine and 4-(4-chlorophenyl)-6-(1-methyl-1 H -indol-3-yl)pyrimidin-2-amine showed good to moderate activity against MCF-7, whereas compound 4-(3-(benzyloxy)phenyl)-6-(1-methyl-1 H -indol-3-yl)pyrimidin-2-amine exhibit moderate activity against HaLa S3 cell line. The newly synthesized derivatives were also screened for their in vitro anti-bacterial activity against Bacillus subtilis , B. megatherium , B. pumilis , Proteus mirabilis , Klebsiella pneumoniae , Enterobacter aerogenes , Streptococcus pyogenes , Staphylococcus aureus , Proteus vulgaris , Escherichia coli , using streptomycin as a standard drug. Among tested compound 4-(3-(benzyloxy)phenyl)-6-(1-methyl-1 H -indol-3-yl)pyrimidin-2-amine shows more potent activity compared to standard, where as the remaining analogues exhibited well to moderate activity compared to standard. Anti-fungal screening results suggest that the compound 4-(4-chlorophenyl)-6-(1 H -indol-3-yl)pyrimidin-2-amineshowed potent activity against Dreschleria halides . The remaining compounds showed nearest activity against all the tested fungal strains compared to standard drug.