2. Academic Validation
  3. Hydrogenative desulphurization of thienopyrrolizinones: an easy and selective access to (Z)-phenethylidenepyrrolizinones with in vitro cytotoxic activity

Hydrogenative desulphurization of thienopyrrolizinones: an easy and selective access to (Z)-phenethylidenepyrrolizinones with in vitro cytotoxic activity

  • Eur J Med Chem. 2010 Mar;45(3):1146-50. doi: 10.1016/j.ejmech.2009.12.021.
Vittoria Perri 1,  Christophe Rochais,  Jana Sopkova-de Oliveira Santos,  Rémi Legay,  Thierry Cresteil,  Patrick Dallemagne,  Sylvain Rault
Affiliations

Affiliation

  • 1 Centre d'Etudes et de Recherche sur le Médicament de Normandie, UPRES EA 4258, FR CNRS 3038 INC3M UFR des Sciences Pharmaceutiques, Université de Caen Basse Normandie, Bd Becquerel, 14032 Caen cedex France.
PMID: 20053482 DOI: 10.1016/j.ejmech.2009.12.021
Abstract

Attempts in view to dearomatize some previously reported tripentones with potent antineoplastic activities led in thiophene series to an unexpected hydrogenative desulphurization reaction. The resulting (Z)-phenethylidenepyrrolizinones were tested in vitro over human epidermoid carcinoma KB cell line. The results of this biological evaluation indicated that the tricyclic core of our model can be cleaved with a partial respect of the activity.

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