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-trimethoxy-stilbene (6b) which was active as apoptotic agent at 0.24 microM. Differently from other stilbenes (including resveratrol) that induce a prevalent recruitment of cells in S phase of cell cycle, we found peculiar behavior of 60b 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.
Simoni D., Roberti M., Invidiata F. P., Aiello E., Aiello S., Marchetti P., et al. (2006). Stilbene-based anticancer agents: Resveratrol analogues active toward HL60 leukemic cells with a non-specific phase mechanism. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 16, 3245-3248 [10.1016/j.bmcl.2006.03.028].
Stilbene-based anticancer agents: Resveratrol analogues active toward HL60 leukemic cells with a non-specific phase mechanism.
ROBERTI, MARINELLA;
2006
Abstract
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-trimethoxy-stilbene (6b) which was active as apoptotic agent at 0.24 microM. Differently from other stilbenes (including resveratrol) that induce a prevalent recruitment of cells in S phase of cell cycle, we found peculiar behavior of 60b 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.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
