Synthesis, in vitro and in vivo cytotoxicity of 6,7-diaryl-2,3,8,8a-tetrahydroindolizin-5(1H)-ones

A 6,7-diaryl-2,3,8,8a-tetrahydroindolizin-5(1H)-one library was constructed and tested against the colon cancer cell line HCT-116 as an initial screen for cytotoxic properties. Of this library, the parent compound, in which the southern aromatic ring remains unsubstituted, and the northern aromatic ring carries a 4-methoxy group, exhibited the most potent cytotoxicity with an IC50 value of 0.39 μM and displayed promising activity in vivo in the NCI’s mouse hollow fiber assay.

Graphical abstractA 6,7-diaryl-2,3,8,8a-tetrahydroindolizin-5(1H)-one library was constructed and assayed for cytotoxicity toward the HCT-116 colon cancer cell line. Micromolar and sub-micromolar potencies were observed. One of the compounds displayed promising activity in the NCI’s mouse hollow fiber assay.Figure optionsDownload full-size imageDownload as PowerPoint slide