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Discovery and biological activity of a novel class I PI3K inhibitor, CH5132799

Bioorganic & medicinal chemistry letters, 2011-03, Vol.21 (6), p.1767-1772

2011

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Synthesis and structure–activity relationships of novel benzofuran farnesyltransferase inhibitors

Bioorganic & medicinal chemistry letters, 2009-03, Vol.19 (6), p.1753-1757

2009

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Synthesis and biological activities of benzofuran antifungal agents targeting fungal N-myristoyltransferase

Bioorganic & medicinal chemistry, 2003-10, Vol.11 (20), p.4463-4478

2003

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Design and synthesis of novel benzofurans as a new class of antifungal agents targeting fungal N-myristoyltransferase. Part 3

Bioorganic & medicinal chemistry letters, 2003-01, Vol.13 (1), p.87-91

2003

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Design and synthesis of novel benzofurans as a new class of antifungal agents targeting fungal N-myristoyltransferase. Part 1

Bioorganic & medicinal chemistry letters, 2001-07, Vol.11 (14), p.1833-1837

2001

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The fibroblast growth factor receptor genetic status as a potential predictor of the sensitivity to CH5183284/Debio 1347, a novel selective FGFR inhibitor

Molecular cancer therapeutics, 2014-11, Vol.13 (11), p.2547-2558

2014

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YES1 Is a Targetable Oncogene in Cancers Harboring YES1 Gene Amplification

Cancer research (Chicago, Ill.), 2019-11, Vol.79 (22), p.5734-5745

2019

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Discovery of [5-Amino-1-(2-methyl‑3H‑benzimidazol-5-yl)pyrazol-4-yl]-(1H‑indol-2-yl)methanone (CH5183284/Debio 1347), An Orally Available and Selective Fibroblast Growth Factor Receptor (FGFR) Inhibitor

Journal of medicinal chemistry, 2016-12, Vol.59 (23), p.10586-10600

2016

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The Selective Class I PI3K Inhibitor CH5132799 Targets Human Cancers Harboring Oncogenic PIK3CA Mutations

Clinical cancer research, 2011-05, Vol.17 (10), p.3272-3281

2011

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Modification of a dihydropyrrolopyrimidine phosphoinositide 3-kinase (PI3K) inhibitor to improve oral bioavailability

Bioorganic & medicinal chemistry, 2015-12, Vol.23 (24), p.7650-7660

2015

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Drastic solvent effect on lipase-catalyzed enantioselective hydrolysis of prochiral 1,4-dihydropyridines

Tetrahedron letters, 1992-11, Vol.33 (47), p.7157-7160

1992

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Optimization of the phenylurea moiety in a phosphoinositide 3-kinase (PI3K) inhibitor to improve water solubility and the PK profile by introducing a solubilizing group and ortho substituents

Bioorganic & medicinal chemistry, 2016-07, Vol.24 (13), p.2897-2906

2016

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Lead optimization of a dihydropyrrolopyrimidine inhibitor against phosphoinositide 3-kinase (PI3K) to improve the phenol glucuronic acid conjugation

Bioorganic & medicinal chemistry letters, 2013-02, Vol.23 (3), p.673-678

2013

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Abstract 2729: FGFR genetic alterations as a potential predictor of the sensitivity to CH5183284/Debio 1347, a selective FGFR inhibitor with a novel chemical scaffold

Cancer research (Chicago, Ill.), 2014-10, Vol.74 (19_Supplement), p.2729-2729

2014

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Abstract 2533: Design and preclinical profile of CH5183284/Debio 1347, a novel orally available and selective FGFR inhibitor acting on a gatekeeper mutant of FGFR2

Cancer research (Chicago, Ill.), 2014-10, Vol.74 (19_Supplement), p.2533-2533

2014

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Acyloxymethyl as an activating group in lipase-catalyzed enantioselective hydrolysis. A versatile approach to chiral 4-aryl-1,4-dihydro-2,6-dimethyl-3,5-pyridinedicarboxylates

Tetrahedron letters, 1991-10, Vol.32 (41), p.5805-5808

1991

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Asymmetric Synthesis of (R)-Nilvadipine and (S)-NB 818 via Regioselective Bromination of Chiral 1, 4-Dihydropyridines as a Key Step and Enzymatic Resolution of Racemic 2-Hydroxymethyl-1, 4-dihydropyridine Derivatives

Chemical and Pharmaceutical Bulletin, 1997/05/15, Vol.45(5), pp.869-876

1997

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Lipase-catalyzed asymmetric hydrolysis and regioselective bromination of 1,4-dihydropyridine. Synthesis of ( R)-(=)-nilvadipine

Tetrahedron: asymmetry, 1994-08, Vol.5 (8), p.1447-1450

1994

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Lipase-Catalyzed Enantioselective Hydrolysis of Bis(acyloxymethyl) 1, 4-Dihydro-3, 5-pyridinedicarboxylates Leading to Optically Active Medicines

Chemical and Pharmaceutical Bulletin, 1997/05/15, Vol.45(5), pp.863-868

1997

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ASYMMETRIC SYNTHESIS OF (S)-(+)-AND (R)-(-)-NZ-105 THROUGH THE MODIFIED MICHAELIS-ARBUZOV REARRANGEMENT AS A KEY STEP

Chemical and Pharmaceutical Bulletin, 1996/05/15, Vol.44(5), pp.1132-1134

1996

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Design and synthesis of novel benzofurans as a new class of antifungal agents targeting fungal N-myristoyltransferase. Part 2

Bioorganic & medicinal chemistry letters, 2002-02, Vol.12 (4), p.607-610

2002

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Enzymatic synthesis of optically active 2-carbamoyl-oxymethyl-1,4-dihydropyridines, ( R)-(+)- and ( S)-(−)-NB 818

Tetrahedron: asymmetry, 1992-09, Vol.3 (9), p.1153-1156

1992

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SYNTHESIS AND INHIBITORY ACTIVITY OF ISOINDOLINONE DERIVATIVES ON THROMBOXANE A2 ANALOG (U-46619)-INDUCED VASOCONTRACTION

Chemical and Pharmaceutical Bulletin, 1990/07/25, Vol.38(7), pp.2060-2062

1990

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Lipase-catalyzed enantiosynthesis of (R)- and (S)-2-(Benzyl(phenyl)amino)ethyl 5-(5,5-Dimethyl-2-oxo-1,3,2-dioxaphosphorinan-2-yl)-1,4-dihydro-2,6-dimethyl-4-(3-nitrophenyl)-3-pyridinecarboxylate (NZ 105)

Chemical & pharmaceutical bulletin, 1995, Vol.43 (7), p.1251-1253

1995

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Enzyme-catalyzed synthesis of biologically active (S)-nilvadipine

Heterocycles, 1993-05, Vol.35 (2), p.603-606

1993

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Discovery and biological activity of a novel class I PI3K inhibitor, CH5132799

Synthesis and structure–activity relationships of novel benzofuran farnesyltransferase inhibitors

Synthesis and biological activities of benzofuran antifungal agents targeting fungal N-myristoyltransferase

Design and synthesis of novel benzofurans as a new class of antifungal agents targeting fungal N-myristoyltransferase. Part 3

Design and synthesis of novel benzofurans as a new class of antifungal agents targeting fungal N-myristoyltransferase. Part 1

The fibroblast growth factor receptor genetic status as a potential predictor of the sensitivity to CH5183284/Debio 1347, a novel selective FGFR inhibitor

YES1 Is a Targetable Oncogene in Cancers Harboring YES1 Gene Amplification

Discovery of [5-Amino-1-(2-methyl‑3H‑benzimidazol-5-yl)pyrazol-4-yl]-(1H‑indol-2-yl)methanone (CH5183284/Debio 1347), An Orally Available and Selective Fibroblast Growth Factor Receptor (FGFR) Inhibitor

The Selective Class I PI3K Inhibitor CH5132799 Targets Human Cancers Harboring Oncogenic PIK3CA Mutations

Modification of a dihydropyrrolopyrimidine phosphoinositide 3-kinase (PI3K) inhibitor to improve oral bioavailability

Drastic solvent effect on lipase-catalyzed enantioselective hydrolysis of prochiral 1,4-dihydropyridines

Optimization of the phenylurea moiety in a phosphoinositide 3-kinase (PI3K) inhibitor to improve water solubility and the PK profile by introducing a solubilizing group and ortho substituents

Lead optimization of a dihydropyrrolopyrimidine inhibitor against phosphoinositide 3-kinase (PI3K) to improve the phenol glucuronic acid conjugation

Abstract 2729: FGFR genetic alterations as a potential predictor of the sensitivity to CH5183284/Debio 1347, a selective FGFR inhibitor with a novel chemical scaffold

Abstract 2533: Design and preclinical profile of CH5183284/Debio 1347, a novel orally available and selective FGFR inhibitor acting on a gatekeeper mutant of FGFR2

Acyloxymethyl as an activating group in lipase-catalyzed enantioselective hydrolysis. A versatile approach to chiral 4-aryl-1,4-dihydro-2,6-dimethyl-3,5-pyridinedicarboxylates

Asymmetric Synthesis of (R)-Nilvadipine and (S)-NB 818 via Regioselective Bromination of Chiral 1, 4-Dihydropyridines as a Key Step and Enzymatic Resolution of Racemic 2-Hydroxymethyl-1, 4-dihydropyridine Derivatives

Lipase-catalyzed asymmetric hydrolysis and regioselective bromination of 1,4-dihydropyridine. Synthesis of ( R)-(=)-nilvadipine

Lipase-Catalyzed Enantioselective Hydrolysis of Bis(acyloxymethyl) 1, 4-Dihydro-3, 5-pyridinedicarboxylates Leading to Optically Active Medicines

ASYMMETRIC SYNTHESIS OF (S)-(+)-AND (R)-(-)-NZ-105 THROUGH THE MODIFIED MICHAELIS-ARBUZOV REARRANGEMENT AS A KEY STEP

Design and synthesis of novel benzofurans as a new class of antifungal agents targeting fungal N-myristoyltransferase. Part 2

Enzymatic synthesis of optically active 2-carbamoyl-oxymethyl-1,4-dihydropyridines, ( R)-(+)- and ( S)-(−)-NB 818

SYNTHESIS AND INHIBITORY ACTIVITY OF ISOINDOLINONE DERIVATIVES ON THROMBOXANE A2 ANALOG (U-46619)-INDUCED VASOCONTRACTION

Lipase-catalyzed enantiosynthesis of (R)- and (S)-2-(Benzyl(phenyl)amino)ethyl 5-(5,5-Dimethyl-2-oxo-1,3,2-dioxaphosphorinan-2-yl)-1,4-dihydro-2,6-dimethyl-4-(3-nitrophenyl)-3-pyridinecarboxylate (NZ 105)

Enzyme-catalyzed synthesis of biologically active (S)-nilvadipine

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