Nicolas Warin

JDQ443, a Structurally Novel, Pyrazole-Based, Covalent Inhibitor of KRAS G12C for the Treatment of Solid Tumors

Edwige Lorthiois, Marc Gerspacher, Kim S. Beyer, Andrea Vaupel et autres

Rapid emergence of tumor resistance via RAS pathway reactivation has been reported from clinical studies of covalent KRAS G12C inhibitors. Thus, inhibitors with broad potential for combination treatment and distinct binding modes to overcome resistance mutations may prove beneficial. JDQ443 is an …

ch, us (code pays fourni par la source)

CCDC 2009566: Experimental Crystal Structure Determination

Robin A. Fairhurst, Thomas F. Knoepfel, Nicole Buschmann, Catherine Leblanc et autres

An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available from the CCDC and typically includes 3D coordinates, …

Discovery of Roblitinib (FGF401) as a Reversible-Covalent Inhibitor of the Kinase Activity of Fibroblast Growth Factor Receptor 4

Robin A. Fairhurst, Thomas F. Knoepfel, Nicole Buschmann, Catherine Leblanc et autres

FGF19 signaling through the FGFR4/β-klotho receptor complex has been shown to be a key driver of growth and survival in a subset of hepatocellular carcinomas, making selective FGFR4 inhibition an attractive treatment opportunity. A kinome-wide sequence alignment highlighted a poorly conserved cysteine …

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Discovery of a series of 8-(1-phenylpyrrolidin-2-yl)-6-carboxamide-2-morpholino-4H-chromen-4-one as PI3Kβ/δ inhibitors for the treatment of PTEN-deficient tumours

Bernard C. Barlaam, Sabina C. Cosulich, Sébastien L. Degorce, Rebecca P.A. Ellston et autres

gb, fr (code pays fourni par la source)

Discovery of a series of 8-(2,3-dihydro-1,4-benzoxazin-4-ylmethyl)-2-morpholino-4-oxo-chromene-6-carboxamides as PI3Kβ/δ inhibitors for the treatment of PTEN-deficient tumours

Bernard C. Barlaam, Sabina C. Cosulich, Sébastien L. Degorce, Martina Fitzek et autres

gb, fr (code pays fourni par la source)

Discovery of ( R )-8-(1-(3,5-Difluorophenylamino)ethyl)- N , N -dimethyl-2-morpholino-4-oxo-4 H -chromene-6-carboxamide (AZD8186): A Potent and Selective Inhibitor of PI3Kβ and PI3Kδ for the Treatment of PTEN-Deficient Cancers

Bernard C. Barlaam, Sabina C. Cosulich, Sébastien L. Degorce, Martina Fitzek et autres

Several studies have highlighted the dependency of PTEN deficient tumors to PI3Kβ activity and specific inhibition of PI3Kδ has been shown activity against human B-cell cancers. We describe the discovery and optimization of a series of 8-(1-anilino)ethyl)-2-morpholino-4-oxo-4H-chromene-6-carboxamides as PI3Kβ/δ inhibitors, which led …

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272 8-(1-Anilino)ethyl)-2-morpholino-4-oxo-4H-chromene-6-carboxamides as PI3Kbeta/delta inhibitors: structure–activity relationships and identification of AZD8186, a clinical candidate for the treatment of PTEN deficient tumours

Bernard C. Barlaam, Sabina C. Cosulich, Sébastien L. Degorce, Martina Fitzek et autres

Structure–activity relationship of a series of non peptidic RGD integrin antagonists targeting α5β1: Part 2

Bénédicte Delouvrié, Katherine J. Al-Kadhimi, Jean-Claude Arnould, Simon T. Barry et autres

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Structure–activity relationship of a series of non peptidic RGD integrin antagonists targeting α5β1: Part 1

Bénédicte Delouvrié, Katherine J. Al-Kadhimi, Jean-Claude Arnould, Simon T. Barry et autres

fr, gb, cn (code pays fourni par la source)

ChemInform Abstract: Facile Preparation of Alkoxybenzoxazoles via Direct SNAr on the Benzoxazole Ring.

Hervé Germain, Craig Steven Harris, Michel Vautier, Nicolas Warin

Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article …

fr (code pays fourni par la source)

Facile preparation of alkoxybenzoxazoles via direct SNAr on the benzoxazole ring

Hervé Germain, Craig Steven Harris, Michel Vautier, Nicolas Warin

ChemInform Abstract: Efficient Large‐Scale Synthesis of Boc‐L‐azatyrosine.

Hervé Germain, Craig Steven Harris, Fabrice G. Renaud, Nicolas Warin

Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article …

fr (code pays fourni par la source)