List of works - Bertrand Leblond

2-difluoromethyloestrone 3-O-sulphamate, a highly potent steroid sulphatase inhibitor.

scientific article published in April 2004

2-substituted estradiol bis-sulfamates, multitargeted antitumor agents: synthesis, in vitro SAR, protein crystallography, and in vivo activity

scientific article

A novel DYRK1A (dual specificity tyrosine phosphorylation-regulated kinase 1A) inhibitor for the treatment of Alzheimer's disease: effect on Tau and amyloid pathologies in vitro.

scientific article published on 26 January 2015

An Unusual Binding Model of the Methyl 9-Anilinothiazolo[5,4-f] quinazoline-2-carbimidates (EHT 1610 and EHT 5372) Confers High Selectivity for Dual-Specificity Tyrosine Phosphorylation-Regulated Kinases

scientific article

Anti-cancer activities of novel D-ring modified 2-substituted estrogen-3-O-sulfamates.

scientific article

DYRK1A controls the transition from proliferation to quiescence during lymphoid development by destabilizing Cyclin D3

scientific article published on 25 May 2015

Design and synthesis of thiazolo[5,4-f]quinazolines as DYRK1A inhibitors, part I.

scientific article

Design and synthesis of thiazolo[5,4-f]quinazolines as DYRK1A inhibitors, part II.

scientific article

Growth inhibition of human in vitro and mouse in vitro and in vivo mammary tumor models by retinoids in comparison with tamoxifen and the RU-486 anti-progestagen.

scientific article published on September 1998

Inhibition of superoxide dismutase by 2-methoxyoestradiol analogues and oestrogen derivatives: structure-activity relationships.

scientific article published in August 2001

Inhibitors of tripeptidyl peptidase II. 3. Derivation of butabindide by successive structure optimizations leading to a potential general approach to designing exopeptidase inhibitors.

scientific article published in November 2005

Phosphorylation of CLEC-2 is dependent on lipid rafts, actin polymerization, secondary mediators, and Rac.

scientific article published on 12 February 2010

RAC1 inhibition targets amyloid precursor protein processing by gamma-secretase and decreases Abeta production in vitro and in vivo.

scientific article published on 8 September 2005

Rap1-Rac1 circuits potentiate platelet activation

scientific article published on 10 November 2011

Recovery of dopamine neuronal transporter but lack of change of its mRNA in substantia nigra after inactivation by a new irreversible inhibitor characterized in vitro and ex vivo in the rat.

scientific article published in September 1999

Specificity and mechanism of action of EHT 1864, a novel small molecule inhibitor of Rac family small GTPases.

scientific article

Structure-activity relationship of isoform selective inhibitors of Rac1/1b GTPase nucleotide binding.

scientific article published on 13 August 2009

Synthesis and evaluation of analogues of estrone-3-O-sulfamate as potent steroid sulfatase inhibitors

scientific article published on 08 March 2012

Vascular disrupting activity and the mechanism of action of EHT 6706, a novel anticancer tubulin polymerization inhibitor.

scientific article

List of works by Bertrand Leblond

2-difluoromethyloestrone 3-O-sulphamate, a highly potent steroid sulphatase inhibitor.

2-substituted estradiol bis-sulfamates, multitargeted antitumor agents: synthesis, in vitro SAR, protein crystallography, and in vivo activity

A novel DYRK1A (dual specificity tyrosine phosphorylation-regulated kinase 1A) inhibitor for the treatment of Alzheimer's disease: effect on Tau and amyloid pathologies in vitro.

An Unusual Binding Model of the Methyl 9-Anilinothiazolo[5,4-f] quinazoline-2-carbimidates (EHT 1610 and EHT 5372) Confers High Selectivity for Dual-Specificity Tyrosine Phosphorylation-Regulated Kinases

Anti-cancer activities of novel D-ring modified 2-substituted estrogen-3-O-sulfamates.

DYRK1A controls the transition from proliferation to quiescence during lymphoid development by destabilizing Cyclin D3

Design and synthesis of thiazolo[5,4-f]quinazolines as DYRK1A inhibitors, part I.

Design and synthesis of thiazolo[5,4-f]quinazolines as DYRK1A inhibitors, part II.

Growth inhibition of human in vitro and mouse in vitro and in vivo mammary tumor models by retinoids in comparison with tamoxifen and the RU-486 anti-progestagen.

Inhibition of superoxide dismutase by 2-methoxyoestradiol analogues and oestrogen derivatives: structure-activity relationships.

Inhibitors of tripeptidyl peptidase II. 3. Derivation of butabindide by successive structure optimizations leading to a potential general approach to designing exopeptidase inhibitors.

Phosphorylation of CLEC-2 is dependent on lipid rafts, actin polymerization, secondary mediators, and Rac.

RAC1 inhibition targets amyloid precursor protein processing by gamma-secretase and decreases Abeta production in vitro and in vivo.

Rap1-Rac1 circuits potentiate platelet activation

Recovery of dopamine neuronal transporter but lack of change of its mRNA in substantia nigra after inactivation by a new irreversible inhibitor characterized in vitro and ex vivo in the rat.

Specificity and mechanism of action of EHT 1864, a novel small molecule inhibitor of Rac family small GTPases.

Structure-activity relationship of isoform selective inhibitors of Rac1/1b GTPase nucleotide binding.

Synthesis and evaluation of analogues of estrone-3-O-sulfamate as potent steroid sulfatase inhibitors

Vascular disrupting activity and the mechanism of action of EHT 6706, a novel anticancer tubulin polymerization inhibitor.