2. Academic Validation
  3. Synthesis and activities towards resistant cancer cells of sulfone and sulfoxide griseofulvin derivatives

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

Affiliations

  • 1 Institut de Recherche Pierre Fabre, CRDPF/CROE, 3 avenue Hubert Curien, BP 13562, 31035 Toulouse Cedex 1, France. Electronic address: frederic.lieby.muller@pierre-fabre.com.
  • 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: frederic.marion@pierre-fabre.com.
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.

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