Abstract
A series of new (3-(1
-benzo[
]imidazol-2-yl))/(3-(3
-imidazo[4,5-
]pyridin-2-yl))-(1
-indol-5-yl)(3,4,5-trimethoxyphenyl)methanone conjugates
were synthesized and evaluated for their antiproliferative activity on selected human cancer cell lines such as prostate (DU-145), lung (A549), cervical (HeLa) and breast (MCF-7). Most of these conjugates showed considerable cytotoxicity with IC
values ranging from 0.54 to 31.86 μM. Among them, compounds
and
showed significant activity against human prostate cancer cell line DU-145 with IC
values of 0.68 μM and 0.54 μM, respectively. Tubulin polymerization assay and immunofluorescence analysis results suggest that these compounds effectively inhibit microtubule assembly formation in DU-145. Further, the apoptosis-inducing ability of these derivatives (
and
) was confirmed by Hoechst staining, measurement of mitochondrial membrane potential and ROS generation and annexin V-FITC assays.