Synthesis and activities towards resistant cancer cells of sulfone and sulfoxide griseofulvin derivatives

  • Bioorg Med Chem Lett. 2015;25(10):2078-81. doi: 10.1016/j.bmcl.2015.03.081.
Frédéric Liéby-Muller  1 ,  Quentin Heudré Le Baliner  2 ,  Serge Grisoni  2 ,  Emmanuel Fournier  2 ,  Nicolas Guilbaud  2 ,  Frédéric Marion  3
Affiliations
  • 1. Institut de Recherche Pierre Fabre, CRDPF/CROE, 3 avenue Hubert Curien, BP 13562, 31035 Toulouse Cedex 1, France. Electronic address: [email protected].
  • 2. Institut de Recherche Pierre Fabre, CRDPF/CROE, 3 avenue Hubert Curien, BP 13562, 31035 Toulouse Cedex 1, France.
  • 3. Institut de Recherche Pierre Fabre, CRDPF/CROE, 3 avenue Hubert Curien, BP 13562, 31035 Toulouse Cedex 1, France. Electronic address: [email protected].
PMID: 25872984 DOI: 10.1016/j.bmcl.2015.03.081
Abstract

Griseofulvin, an Antifungal drug, has been shown in recent years to have anti-proliferative activities. We report here the synthesis of new analogs of griseofulvin, substituted in 2' by a sulfonyl group or in 3' by a sulfinyl or sulfonyl group. These compounds exhibit good anti-proliferative activities against SCC114 cells, an oral squamous carcinoma cell line showing pronounced centrosome amplification, and unexpected cytotoxic activities on HCC1937 cells, a triple negative breast Cancer cell line resistant to microtubule inhibitors.

Keywords
Cytotoxicity; Griseofulvin; Sulfone; Sulfoxide.