2. Academic Validation
  3. Stilbene-based anticancer agents: resveratrol analogues active toward HL60 leukemic cells with a non-specific phase mechanism

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

  • Bioorg Med Chem Lett. 2006 Jun 15;16(12):3245-8. doi: 10.1016/j.bmcl.2006.03.028.
Daniele Simoni 1,  Marinella Roberti,  Francesco Paolo Invidiata,  Enrico Aiello,  Stefania Aiello,  Paolo Marchetti,  Riccardo Baruchello,  Marco Eleopra,  Antonietta Di Cristina,  Stefania Grimaudo,  Nicola Gebbia,  Lucia Crosta,  Francesco Dieli,  Manlio Tolomeo
Affiliations

Affiliation

  • 1 Dipartimento di Scienze Farmaceutiche, Via Fossato di Mortara 17-19, Università di Ferrara, 44100 Ferrara, Italy. [email protected]
PMID: 16580204 DOI: 10.1016/j.bmcl.2006.03.028
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-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.

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