Design, Synthesis and Evaluation of Novel 7-Azaindole Derivatives As Anti-Cancer Agents

Abstract

Azaindoles are an important class of nitrogen containing heterocyclics and were identified as the most active and potent classes of compounds with wide range of biological and pharmacological activities.A new series of 7-aza indole  derivatives  were characterized by spectral data and evaluated for anticancer activity  activity. The compounds 10m, 10n, were found to be good inhibitors of HELa and MCF-7. Most of the compounds inhibited HELa and MCF-7with the IC₅₀ values, ranging from 0.68 µM 6.24 µM. Amongst them, compounds 10m, 10n with dichlorophenyl anddibromophenyl substituted molecules exhibited strongest inhibitory activity against MCF-7 and HELa with IC₅₀   0.78±1.33, 1.31±0.02 µM and 0.92±0.03, 1.91±0.02 µM respectively. when compared to standard cisplain with IC₅₀ of 0.68±0.02 µM and 1.65±0.02, Thus, these new 7-aza indole derivatives have emerged as new cancer inhibitors for further exploitation as anti-cancer agents. Docking studies of all the molecules disclosed close hydrogen bond interactions within the binding site.