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 microM. 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.
Simoni
Daniele
D
Dipartimento di Scienze Farmaceutiche, Via Fossato di Mortara 17-19, Università di Ferrara, 44100 Ferrara, Italy. smd@unife.it
Roberti
Marinella
M
Invidiata
Francesco Paolo
FP
Aiello
Enrico
E
Aiello
Stefania
S
Marchetti
Paolo
P
Baruchello
Riccardo
R
Eleopra
Marco
M
Di Cristina
Antonietta
A
Grimaudo
Stefania
S
Gebbia
Nicola
N
Crosta
Lucia
L
Dieli
Francesco
F
Tolomeo
Manlio
M
D000965:Antimony / Q000737:chemistry*; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D049109:Cell Proliferation / Q000187:drug effects; D018922:HL-60 Cells; D006801:Humans; D015394:Molecular Structure; D000077185:Resveratrol; D013267:Stilbenes / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D013329:Structure-Activity Relationship
D000970:Antineoplastic Agents; D013267:Stilbenes; C021254:stibine; D000965:Antimony; D000077185:Resveratrol