Synthesis and antiproliferative activity of novobiocin analogues as potential hsp90 inhibitors Dedicated to the memory of Dr. Christine Radanyi.

Davide Audisio; Délphine Methy-Gonnot; Christine Radanyi; Jack Michel Renoir; Stéphanie Denis; Félix Sauvage; Juliette Vergnaud-Gauduchon; Jean Daniel Brion; Samir Messaoudi; Mouad Alami

doi:10.1016/j.ejmech.2014.06.067

Synthesis and antiproliferative activity of novobiocin analogues as potential hsp90 inhibitors Dedicated to the memory of Dr. Christine Radanyi.

Davide Audisio
, Délphine Methy-Gonnot
, Christine Radanyi
, Jack Michel Renoir
, Stéphanie Denis
, Félix Sauvage
, Juliette Vergnaud-Gauduchon
, Jean Daniel Brion
, Samir Messaoudi
, Mouad Alami

Université Paris-Saclay
Université Paris-Sud
Gustave Roussy Comprehensive Cancer Institute

Research output: Contribution to journal › Article › peer-review

31 Citations (Scopus)

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.

Original language	English
Pages (from-to)	498-507
Number of pages	10
Journal	European Journal of Medicinal Chemistry
Volume	83
DOIs	https://doi.org/10.1016/j.ejmech.2014.06.067
Publication status	Published - 18 Aug 2014
Externally published	Yes

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

SDG 3 Good Health and Well-being

Keywords

4TCNA
6BrCaQ
Apoptosis
Cytotoxicity
Hsp90

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10.1016/j.ejmech.2014.06.067

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Audisio, D., Methy-Gonnot, D., Radanyi, C., Renoir, J. M., Denis, S., Sauvage, F., Vergnaud-Gauduchon, J., Brion, J. D., Messaoudi, S., & Alami, M. (2014). Synthesis and antiproliferative activity of novobiocin analogues as potential hsp90 inhibitors Dedicated to the memory of Dr. Christine Radanyi. European Journal of Medicinal Chemistry, 83, 498-507. https://doi.org/10.1016/j.ejmech.2014.06.067

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title = "Synthesis and antiproliferative activity of novobiocin analogues as potential hsp90 inhibitors Dedicated to the memory of Dr. Christine Radanyi.",

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.",

keywords = "4TCNA, 6BrCaQ, Apoptosis, Cytotoxicity, Hsp90",

author = "Davide Audisio and D{\'e}lphine Methy-Gonnot and Christine Radanyi and Renoir, \{Jack Michel\} and St{\'e}phanie Denis and F{\'e}lix Sauvage and Juliette Vergnaud-Gauduchon and Brion, \{Jean Daniel\} and Samir Messaoudi and Mouad Alami",

year = "2014",

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doi = "10.1016/j.ejmech.2014.06.067",

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Audisio, D, Methy-Gonnot, D, Radanyi, C, Renoir, JM, Denis, S, Sauvage, F, Vergnaud-Gauduchon, J, Brion, JD, Messaoudi, S & Alami, M 2014, 'Synthesis and antiproliferative activity of novobiocin analogues as potential hsp90 inhibitors Dedicated to the memory of Dr. Christine Radanyi.', European Journal of Medicinal Chemistry, vol. 83, pp. 498-507. https://doi.org/10.1016/j.ejmech.2014.06.067

TY - JOUR

T1 - Synthesis and antiproliferative activity of novobiocin analogues as potential hsp90 inhibitors Dedicated to the memory of Dr. Christine Radanyi.

AU - Audisio, Davide

AU - Methy-Gonnot, Délphine

AU - Radanyi, Christine

AU - Renoir, Jack Michel

AU - Denis, Stéphanie

AU - Sauvage, Félix

AU - Vergnaud-Gauduchon, Juliette

AU - Brion, Jean Daniel

AU - Messaoudi, Samir

AU - Alami, Mouad

PY - 2014/8/18

Y1 - 2014/8/18

N2 - 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.

AB - 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.

KW - 4TCNA

KW - 6BrCaQ

KW - Apoptosis

KW - Cytotoxicity

KW - Hsp90

U2 - 10.1016/j.ejmech.2014.06.067

DO - 10.1016/j.ejmech.2014.06.067

M3 - Article

C2 - 24992077

AN - SCOPUS:84903693254

SN - 0223-5234

VL - 83

SP - 498

EP - 507

JO - European Journal of Medicinal Chemistry

JF - European Journal of Medicinal Chemistry

ER -

Synthesis and antiproliferative activity of novobiocin analogues as potential hsp90 inhibitors Dedicated to the memory of Dr. Christine Radanyi.

Abstract

UN SDGs

Keywords

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