Détail

09/02/2017 Recherche

Publication : Approach to ferrocenyl-podophyllotoxin analogs and their evaluation as anti-tumor agents

Matthieu Beaupérin, Dilan Polat, Fares Roudesly, Siden Top, Anne Vessières, Julie Oble, Gérard Jaouen, Giovanni Poli

Revue : Journal of Organometallic Chemistry
DOI :
10.1016/j.jorganchem.2017.02.005

Highlights

  • Podophyllotoxin analogs have been synthesized
  • The ferrocenyl moiety was grafted on podophyllotoxin and on an analog of it
  • The importance of ferrocenyl conjugated motifs to generate antiproliferative effects is discussed.

Abstract

Podophyllotoxin is a natural product endowed of a high antimitotic activity and a high affinity for tubulin. Its action results in the cessation of cell division, inducing cell death. However, its high toxicity restrains its use as drug. To overcome this drawback, several chemical modifications of the native podophyllotoxin have been made. However, to date, no reports have so far been directed toward incorporation of a metallocene moiety. The search for new organometallic drugs is a central field in drug discovery, including the domain of cancer therapy. In particular, metallocenyl moieties are known to increase or decrease, depending on the degree of conjugation in the organometallic motif, the selectivity of drugs toward cancer cells. The conjugate organometallic compound reduces the damage of healthy tissues, yet permitting the selective desired antimitotic and cytotoxic effects of the active principle. We report here the synthesis of ferrocene-containing podophyllotoxin analogs and preliminary antiproliferative tests.

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