Structural optimization of indole based compounds for highly promising anti-cancer activities: structure activity relationship studies and identification of lead molecules.

Based on the anti-cancer data of previous compounds, 27 more compounds were synthesized and subjected to anti-cancer screening. Compounds were tested over 60 human tumor cell lines of different types of cancer. As per the data available, some compounds exhibited appreciable anti-cancer properties over certain cell lines with their GI₅₀ in nM range. With the help of UV-vis spectral studies, enzyme immunoassay and molecular modeling studies, dihydrofolate reductase was found to be the probable cellular target of the compounds under present investigation.