Stilbene-based anticancer agents: Resveratrol analogues active toward HL60 leukemic cells with a non-specific phase mechanism

Several stilbenes, related to known resveratrol, have been synthesized and tested for their anticancer effect on HL60 leukemia cell line, taking particular care of the cell cycle analysis. The most potent compound was the known (Z)-3,4′,5-trimethoxystilbene (6b) which was active as apoptotic agent at 0.24 μM. Differently from other stilbenes (including resveratrol) that induced a prevalent recruitment of cells in S phase of cell cycle, we found a peculiar behavior of 6b that caused a decrease of cells in all phases of cell cycle (G0–G1, S, and G2–M) and a proportional increase of apoptotic cells. The potent pro-apoptotic activity shown by compound 6b and its effects on cell cycle make this compound of great interest for further investigations.

Graphical abstractThe effects of several stilbenes on HL60 cell cycle have been detected. Particularly interesting is the non-selective phase block caused by a known compound.Figure optionsDownload full-size imageDownload as PowerPoint slide