Synthesis, anti-cancer evaluation and molecular docking studies of aryl bisindole derivatives

Abstract

Abstract A simple and efficient method has been developed for the synthesis of aryl bis-indolyl derivatives (9a-9k) by the catalytic amount of 18-Crown-6 and evaluated for their cytotoxicity using lung cancer, breast cancer, colon and melanoma cancer cell lines. Among them, compounds 9f and 9i with methoxy substitutions on phenyl ring was found be to be potent inhibitors (IC50 = 0.11 to 0.19 µM) of all the tested cell lines. Compound 9c with difluoro substitution on phenyl ring was inhibited first three cell lines (IC50 = 0.12 to 0.15 µM) except melanoma. Compound 9h with both chloro and fluoro on phenyl ring were found to be having the higher potency against only lung cancer cell line (IC50 = 0.11 µM). These compounds showed higher anticancer potency than Adriamycin drug (0.9 to 3.5 µM). Molecular docking studies have been carried out to understand the binding modes of the active and inactive compounds.