R. Morgentin

发表

Investigation of (E)-3-[4-(2-Oxo-3-aryl-chromen-4-yl)oxyphenyl]acrylic Acids as Oral Selective Estrogen Receptor Down-Regulators.

R. A. Norman, James S. Scott, A. Bailey, 2015, Journal of medicinal chemistry.

Synthesis of 1,4,5 trisubstituted γ-lactams via a 3-component cascade reaction.

Thomas E Nielsen, Peng Wu, R. Morgentin, 2015, Bioorganic & medicinal chemistry.

Synthesis of sp(3)-rich scaffolds for molecular libraries through complexity-generating cascade reactions.

R. Morgentin, M. Clausen, T. Nielsen, 2016, Organic & biomolecular chemistry.

Realisation of small molecule libraries based on frameworks distantly related to natural products.

Adam Nelson, Mark Dow, Tuomo Kalliokoski, 2018, Organic & biomolecular chemistry.

Tandem Mannich/Diels–Alder reactions for the synthesis of indole compound libraries

R. Morgentin, M. Petersen, M. Clausen, 2016 .

A metal-catalyzed enyne-cyclization step for the synthesis of bi- and tricyclic scaffolds amenable to molecular library production.

R. Morgentin, M. Petersen, M. Clausen, 2016, Organic & biomolecular chemistry.

Design, synthesis and decoration of molecular scaffolds for exploitation in the production of alkaloid-like libraries.

Adam Nelson, Mark Dow, Tuomo Kalliokoski, 2015, Bioorganic & medicinal chemistry.

Imidazole piperazines: SAR and development of a potent class of cyclin-dependent kinase inhibitors with a novel binding mode.

D. M. Andrews, A. Barker, J. Tucker, 2008, Bioorganic & medicinal chemistry letters.

Petasis/Diels-Alder/Cyclization Cascade Reactions for the Generation of Scaffolds with Multiple Stereogenic Centers and Orthogonal Handles for Library Production

R. Morgentin, M. Clausen, T. Nielsen, 2018, European Journal of Organic Chemistry.

Discovery of new quinoline ether inhibitors with high affinity and selectivity for PDGFR tyrosine kinases.

S. Ashton, R. Morgentin, P. Plé, 2012, Bioorganic & medicinal chemistry letters.

Discovery of AZD2932, a new Quinazoline Ether Inhibitor with high affinity for VEGFR-2 and PDGFR tyrosine kinases.

S. Ashton, R. Morgentin, P. Plé, 2012, Bioorganic & medicinal chemistry letters.

Squaramides as novel class I and IIB histone deacetylase inhibitors for topical treatment of cutaneous t-cell lymphoma.

F. Joly, R. Morgentin, E. Thoreau, 2018, Bioorganic & medicinal chemistry letters.

The discovery of AZD0530: a novel, oral, highly selective and dual-specific inhibitor of the Src and Abl family kinases

R. Morgentin, P. Plé, L. Hennequin, 2005 .

Inhibitors of epidermal growth factor receptor tyrosine kinase: Novel C-5 substituted anilinoquinazolines designed to target the ribose pocket.

Andrew G. Leach, Paul D. Johnson, R. Morgentin, 2006, Bioorganic & medicinal chemistry letters.

Discovery of 9-(1-anilinoethyl)-2-morpholino-4-oxo-pyrido[1,2-a]pyrimidine-7-carboxamides as PI3Kβ/δ inhibitors for the treatment of PTEN-deficient tumours.

S. Green, B. Barlaam, S. Degorce, 2014, Bioorganic & medicinal chemistry letters.

Inhibitors of epidermal growth factor receptor tyrosine kinase: Novel C-5 substituted anilinoquinazolines designed to target the ribose pocket.

Paul D. Johnson, R. Morgentin, R. Bradbury, 2006, Bioorganic & medicinal chemistry letters.

New heterocyclic analogues of 4-(2-chloro-5-methoxyanilino)quinazolines as potent and selective c-Src kinase inhibitors.

B. Barlaam, R. Morgentin, P. Plé, 2005, Bioorganic & medicinal chemistry letters.

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.

S. Green, Rebecca P A Ellston, B. Barlaam, 2017, Bioorganic & medicinal chemistry letters.

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.

S. Green, B. Barlaam, S. Degorce, 2016, Bioorganic & medicinal chemistry letters.

Expansion of chemical space for collaborative lead generation and drug discovery: the European Lead Factory Perspective.

Adam Nelson, Tuomo Kalliokoski, Gerhard Müller, 2015, Drug discovery today.

ASYMMETRIC SYNTHESIS OF UNSATURATED PIPECOLIC ACID DERIVATIVES

R. Morgentin, D. Bihan, C. Agami, 1997 .

Two-Directional Approach for the Rapid Synthesis of 2,4-Bis-Aminoaryl Pyridine Derivatives

B. Barlaam, R. Morgentin, A. Peru, 2012 .

Strategic studies in the syntheses of novel 6,7-substituted quinolones and 7-or 6-substituted 1,6-and 1,7-naphthyridones

M. Maudet, R. Morgentin, P. Plé, 2008 .

An efficient large-scale synthesis of alkyl 5-hydroxy-pyridin- and pyrimidin-2-yl acetate

M. Maudet, R. Morgentin, P. Plé, 2009 .

Trichloroacetic acid hydrazones I: New formation of 1,3,4-oxadiazoles from aldehydes

R. Morgentin, L. E. Kaim, I. L. Menestrel, 1998 .

5-Substituted 4-anilinoquinazolines as potent, selective and orally active inhibitors of erbB2 receptor tyrosine kinase.

Paul D. Johnson, R. Morgentin, R. Bradbury, 2005, Bioorganic & medicinal chemistry letters.

Asymmetric Syntheses of Enantiopure 4‐Substituted Pipecolic Acid Derivatives

R. Morgentin, S. Comesse, S. Guesné, 2001 .

Discovery of (R)-8-(1-(3,5-difluorophenylamino)ethyl)-N,N-dimethyl-2-morpholino-4-oxo-4H-chromene-6-carboxamide (AZD8186): a potent and selective inhibitor of PI3Kβ and PI3Kδ for the treatment of PTEN-deficient cancers.

S. Green, B. Barlaam, S. Degorce, 2015, Journal of medicinal chemistry.

N-(5-chloro-1,3-benzodioxol-4-yl)-7-[2-(4-methylpiperazin-1-yl)ethoxy]-5- (tetrahydro-2H-pyran-4-yloxy)quinazolin-4-amine, a novel, highly selective, orally available, dual-specific c-Src/Abl kinase inhibitor.

L. Otterbein, J. Breed, R. A. Norman, 2006, Journal of medicinal chemistry.

One-pot synthesis of bis(amino)-1,2,4-thiadiazoles via direct SNAr

S. Degorce, R. Morgentin, H. Beeley, 2013 .

Discovery of 1-(4-(5-(5-amino-6-(5-tert-butyl-1,3,4-oxadiazol-2-yl)pyrazin-2-yl)-1-ethyl-1,2,4-triazol-3-yl)piperidin-1-yl)-3-hydroxypropan-1-one (AZD8835): A potent and selective inhibitor of PI3Kα and PI3Kδ for the treatment of cancers.

S. Green, Rebecca P A Ellston, B. Barlaam, 2015, Bioorganic & medicinal chemistry letters.

Generation of a Heteropolycyclic and sp3 -Rich Scaffold for Library Synthesis from a Highly Diastereoselective Petasis/Diels-Alder and ROM-RCM Reaction Sequence

R. Morgentin, M. Clausen, T. Nielsen, 2019, European Journal of Organic Chemistry.

Abstract 2830: Discovery of AZD8835, a potent and selective inhibitor of PI3Kα and PI3Kδ for the treatment ofPIK3CA-dependent cancers

S. Green, R. Morgentin, S. Cosulich, 2015 .

Strategic Studies in the Syntheses of Novel 6,7‐Substituted Quinolones and 7‐ or 6‐Substituted 1,6‐ and 1,7‐Naphthyridones.

M. Maudet, R. Morgentin, P. Plé, 2008 .