- Synthesis and antiproliferative activity of novobiocin analogues as potential hsp90 inhibitors.
Synthesis and antiproliferative activity of novobiocin analogues as potential hsp90 inhibitors.
European journal of medicinal chemistry (2014-07-06)
Davide Audisio, Délphine Methy-Gonnot, Christine Radanyi, Jack-Michel Renoir, Stéphanie Denis, Félix Sauvage, Juliette Vergnaud-Gauduchon, Jean-Daniel Brion, Samir Messaoudi, Mouad Alami
PMID24992077
ABSTRACT
A series of substituted coumarins1-10 was designed and synthesized as a novel class of 4TCNA analogues. Compound 2a showed excellent antiproliferative activity with mean GI50 values at a micromolar level in a diverse set of human cancer cells (GI50 = 2-30 μM) and induced a high apoptosis level in MCF-7 breast cancer cell line. The molecular signature of hsp90 inhibition was assessed by depletion of the Erα hsp90 client protein.
MATERIALS
Product Number
Brand
Product Description
Sigma-Aldrich
L-Glutamine, meets USP testing specifications, suitable for cell culture, 99.0-101.0%, from non-animal source
Supelco
L-Glutamine, certified reference material, TraceCERT®, Manufactured by: Sigma-Aldrich Production GmbH, Switzerland