Indole represents one of the most important pharmacodynamic nucleus which has been actively explored in discovery and development of new drugs. Indole-based compounds exhibit broad range of biological properties viz., anti-inflammatory, anticonvulsant, cardiovascular, anti-HIV, antibacterial etc. In our efforts of designing new compounds, we synthesized a series of novel 3,5-diaryl indole-5-carboxylic acid derivates. These compounds were screened on National Caner Institute's 60 human cancer cell line panel which covers diverse histologies. A subset from this chemical library when tested in dose dependent manner showed anti-cancer activity against multiple cell lines. To understand the mechanism of activity, we performed further studies on the non-small cell lung cancer 'A 549 cells'. The in vitro assay using Annexin V-FITC showed early apoptosis. The immunofluorescence test showed reduction in Ki-67 proliferation marker but significant increase in phosphor P38 MAPK. This suggests new compounds to induce apoptosis in A549 cells by decreasing cellular proliferation and activation of P38 MAPK, ultimately leading to DNA fragmentation.

Synthesis and biological evaluation of substituted 3,5-diaryl indole-5-carboxylic acid derivatives as anticancer agents

246th National Meeting (2013)

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