Synthesis and biological evaluation of novel coumarin-based inhibitors of Cdc25 phosphatases

Sergio Valente; Emilie Bana; Elodie Viry; Denyse Bagrel; Gilbert Kirsch

doi:10.1016/j.bmcl.2010.07.130

Synthesis and biological evaluation of novel coumarin-based inhibitors of Cdc25 phosphatases

Sergio Valente
, Emilie Bana
, Elodie Viry
, Denyse Bagrel
, Gilbert Kirsch^*

^*Corresponding author for this work

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

39 Citations (Scopus)

Abstract

The cell division cycle 25 (Cdc25) family of proteins are dual specificity phosphatases that activate cyclin-dependent kinase (CDK) complexes, which in turn regulate progression through the cell division cycle. Overexpression of Cdc25 proteins has been reported in a wide variety of cancers; their inhibition may thus represent a novel approach for the development of anticancer therapeutics. Herein we report new coumarin-based scaffolds endowed with a selective inhibition against Cdc25A and Cdc25C, being 6a and 6d the most efficient inhibitors and worthy of further investigation as anticancer agents.

Original language	English
Pages (from-to)	5827-5830
Number of pages	4
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	20
Issue number	19
DOIs	https://doi.org/10.1016/j.bmcl.2010.07.130
Publication status	Published - 1 Oct 2010
Externally published	Yes

Keywords

Cdc25 phosphatases
Chalcones
Coumarins
Heck coupling

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10.1016/j.bmcl.2010.07.130

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title = "Synthesis and biological evaluation of novel coumarin-based inhibitors of Cdc25 phosphatases",

abstract = "The cell division cycle 25 (Cdc25) family of proteins are dual specificity phosphatases that activate cyclin-dependent kinase (CDK) complexes, which in turn regulate progression through the cell division cycle. Overexpression of Cdc25 proteins has been reported in a wide variety of cancers; their inhibition may thus represent a novel approach for the development of anticancer therapeutics. Herein we report new coumarin-based scaffolds endowed with a selective inhibition against Cdc25A and Cdc25C, being 6a and 6d the most efficient inhibitors and worthy of further investigation as anticancer agents.",

keywords = "Cdc25 phosphatases, Chalcones, Coumarins, Heck coupling",

author = "Sergio Valente and Emilie Bana and Elodie Viry and Denyse Bagrel and Gilbert Kirsch",

note = "Funding Information: The research leading to these results has received funding from the [ European Community{\textquoteright}s ] Seventh Framework Programme ([FP7/2007-2013] under Grant Agreement No. 215009 . Funding Information: Region de Lorraine , Conseil G{\'e}n{\'e}ral de la Moselle , and Ligue contre le Cancer (54, 55, 57 Departmental comitees) are acknowledged for financial support. Funding Information: E.B. is recipient of an AFR grant from the “ Fonds national de la Recherche (Luxembourg) ”.",

year = "2010",

month = oct,

day = "1",

doi = "10.1016/j.bmcl.2010.07.130",

language = "English",

volume = "20",

pages = "5827--5830",

journal = "Bioorganic and Medicinal Chemistry Letters",

issn = "0960-894X",

publisher = "Elsevier Ltd.",

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}

TY - JOUR

T1 - Synthesis and biological evaluation of novel coumarin-based inhibitors of Cdc25 phosphatases

AU - Valente, Sergio

AU - Bana, Emilie

AU - Viry, Elodie

AU - Bagrel, Denyse

AU - Kirsch, Gilbert

N1 - Funding Information: The research leading to these results has received funding from the [ European Community’s ] Seventh Framework Programme ([FP7/2007-2013] under Grant Agreement No. 215009 . Funding Information: Region de Lorraine , Conseil Général de la Moselle , and Ligue contre le Cancer (54, 55, 57 Departmental comitees) are acknowledged for financial support. Funding Information: E.B. is recipient of an AFR grant from the “ Fonds national de la Recherche (Luxembourg) ”.

PY - 2010/10/1

Y1 - 2010/10/1

N2 - The cell division cycle 25 (Cdc25) family of proteins are dual specificity phosphatases that activate cyclin-dependent kinase (CDK) complexes, which in turn regulate progression through the cell division cycle. Overexpression of Cdc25 proteins has been reported in a wide variety of cancers; their inhibition may thus represent a novel approach for the development of anticancer therapeutics. Herein we report new coumarin-based scaffolds endowed with a selective inhibition against Cdc25A and Cdc25C, being 6a and 6d the most efficient inhibitors and worthy of further investigation as anticancer agents.

AB - The cell division cycle 25 (Cdc25) family of proteins are dual specificity phosphatases that activate cyclin-dependent kinase (CDK) complexes, which in turn regulate progression through the cell division cycle. Overexpression of Cdc25 proteins has been reported in a wide variety of cancers; their inhibition may thus represent a novel approach for the development of anticancer therapeutics. Herein we report new coumarin-based scaffolds endowed with a selective inhibition against Cdc25A and Cdc25C, being 6a and 6d the most efficient inhibitors and worthy of further investigation as anticancer agents.

KW - Cdc25 phosphatases

KW - Chalcones

KW - Coumarins

KW - Heck coupling

UR - https://www.scopus.com/pages/publications/77957590019

U2 - 10.1016/j.bmcl.2010.07.130

DO - 10.1016/j.bmcl.2010.07.130

M3 - Article

C2 - 20800482

AN - SCOPUS:77957590019

SN - 0960-894X

VL - 20

SP - 5827

EP - 5830

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 19

ER -

Synthesis and biological evaluation of novel coumarin-based inhibitors of Cdc25 phosphatases

Abstract

Keywords

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