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.
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| http://dx.doi.org/10.1039/c7md00450h | DOI Listing |
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