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Identification of [4-[4-(methylsulfonyl)phenyl]-6-(trifluoromethyl)-2-pyrimidinyl] amines and ethers as potent and selective cyclooxygenase-2 inhibitors

Bioorganic & medicinal chemistry letters, 2009-08, Vol.19 (15), p.4504-4508

2009

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Potent Pre-Clinical and Early Phase Clinical Activity of EP300/CBP Bromodomain Inhibitor CCS1477 in Multiple Myeloma

Blood, 2022-11, Vol.140 (Supplement 1), p.852-853

2022

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CCS1477, a Novel p300/CBP Bromodomain Inhibitor, Enhances Efficacy of Azacitidine and Venetoclax in Pre-Clinical Models of Acute Myeloid Leukaemia and Lymphoma

Blood, 2021-11, Vol.138 (Supplement 1), p.3291-3291

2021

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CCS1477: A Novel Small Molecule Inhibitor of p300/CBP Bromodomain for the Treatment of Acute Myeloid Leukaemia and Multiple Myeloma

Blood, 2019-11, Vol.134 (Supplement_1), p.2560-2560

2019

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Therapeutic Targeting of EP300/CBP By Bromodomain Inhibition in Acute Myeloid Leukemia

Blood, 2022-11, Vol.140 (Supplement 1), p.8774-8775

2022

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An Open-Label Phase I/IIa Study to Evaluate the Safety and Efficacy of CCS1477, a First in Clinic Inhibitor of the p300/CPB Bromodomains, As Monotherapy in Patients with Advanced Haematological Malignancies

Blood, 2019-11, Vol.134 (Supplement_1), p.1266-1266

2019

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Thrombin inhibitors based on [5,5] trans-fused indane lactams

Bioorganic & medicinal chemistry letters, 1999-06, Vol.9 (12), p.1657-1662

1999

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Lewis acid induced rearrangement of 2,3-epoxy sulfides; regiospecific trapping of thiiranium ion intermediates with nitrogen heterocycles and amides. Use of imines as nucleophilic equivalents for the selective monoalkylation of primary amines

Tetrahedron, 1996, Vol.52 (10), p.3609-3630

1996

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[3.3] Sigmatropy within 1-vinyl-2-alkenyl-7,7-dimethyl-exo-norbornan-2-ols. The first atropselective oxyanionic Cope rearrangement

Journal of the American Chemical Society, 1990, Vol.112 (1), p.277-283

1990

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Synthesis of trans-fused [5,5] bicyclic lactones/lactams as templates for serine protease inhibition

Tetrahedron letters, 1998-09, Vol.39 (38), p.6979-6982

1998

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Functionalization reactions of a medium-ring bridgehead enone that skirt transannular bond formation

Journal of organic chemistry, 1991-03, Vol.56 (7), p.2461-2468

1991

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Direct oxygenation of enolates generated by anionic oxy-Cope rearrangement. Expedient preparation of polycyclic .alpha.-hydroxy ketones

Journal of organic chemistry, 1989-09, Vol.54 (19), p.4576-4581

1989

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Identification of [4-[4-(methylsulfonyl)phenyl]-6-(trifluoromethyl)-2-pyrimi-dinyl] amines and ethers as potent and selective cyclooxygenase-2 inhibitors

Bioorganic & medicinal chemistry letters, 2009, Vol.19 (15), p.4504-4508

2009

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Lewis acid-induced rearrangement of 2,3-epoxy sulfides: regiospecific nucleophilic trapping of thiiranium ion intermediates with nitrogen nucleophiles

Journal of the Chemical Society, Perkin Transactions 1, 1993 (13), p.1371

1993

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Synthesis of grevillins, novel pyrandione pigments of fungi. Biogenetic interrelationships between grevillins, pulvinic acids, terphenylquinones and xylerythrins

Journal of the Chemical Society, Perkin Transactions 1, 1991 (10), p.2363

1991

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Discovery of an Orally Bioavailable NK1 Receptor Antagonist, (2S,3S)-(2-Methoxy-5-tetrazol-1-ylbenzyl)(2-phenylpiperidin-3-yl)amine (GR203040), with Potent Antiemetic Activity

Journal of medicinal chemistry, 1995-12, Vol.38 (26), p.4985-4992

1995

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The synthesis of a conformationally restrained, combined thromboxane antagonist / synthase inhibitor using an intramolecular ‘Stille’- or ‘Grigg’-palladium-catalysed cyclisation strategy

Tetrahedron letters, 1993-12, Vol.34 (51), p.8353-8356

1993

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5,5- Trans lactone-containing inhibitors of serine proteases: Identification of a novel, acylating thrombin inhibitor

Bioorganic & medicinal chemistry letters, 1998-11, Vol.8 (21), p.2955-2960

1998

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Synthetic [5,5] trans-fused indane lactones as inhibitors of thrombin

Bioorganic & medicinal chemistry letters, 1999-02, Vol.9 (3), p.431-436

1999

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Reaction of α-amino esters and α-amino ester imines with thiiranium ion intermediates. Application to the synthesis of new potential aminopeptidase inhibitors and mechanistic implications

Tetrahedron, 1997-03, Vol.53 (9), p.3383-3394

1997

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Addition of amino esters to thiiranium ion intermediates: A novel approach to the synthesis of new potential aminopeptidase inhibitors

Tetrahedron letters, 1995, Vol.36 (45), p.8327-8330

1995

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Addition of Amino Esters to Thiiranium Ion Intermediates: A Novel Approach to the Synthesis of New Potential Aminopeptidase Inhibitors

Tetrahedron letters, 1995-11, Vol.36 (45), p.8327-8330

Gill, D

1995

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Imines as Synthetic Equivalents of Primary Amines for the Nucleophilic Trapping of Thiiranium Ion Intermediates

Synlett, 1995-12, Vol.1995 (12), p.1275-1276

1995

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Synthesis of grevillins and their biogenetic interrelationship with terphenylquinones, xylerythrins and pulvinic acid

Tetrahedron letters, 1987, Vol.28 (40), p.4749-4752

1987

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Identification of [4-[4-(methylsulfonyl)phenyl]-6-(trifluoromethyl)-2-pyrimidinyl] amines and ethers as potent and selective cyclooxygenase-2 inhibitors

Potent Pre-Clinical and Early Phase Clinical Activity of EP300/CBP Bromodomain Inhibitor CCS1477 in Multiple Myeloma

CCS1477, a Novel p300/CBP Bromodomain Inhibitor, Enhances Efficacy of Azacitidine and Venetoclax in Pre-Clinical Models of Acute Myeloid Leukaemia and Lymphoma

CCS1477: A Novel Small Molecule Inhibitor of p300/CBP Bromodomain for the Treatment of Acute Myeloid Leukaemia and Multiple Myeloma

Therapeutic Targeting of EP300/CBP By Bromodomain Inhibition in Acute Myeloid Leukemia

An Open-Label Phase I/IIa Study to Evaluate the Safety and Efficacy of CCS1477, a First in Clinic Inhibitor of the p300/CPB Bromodomains, As Monotherapy in Patients with Advanced Haematological Malignancies

Thrombin inhibitors based on [5,5] trans-fused indane lactams

Lewis acid induced rearrangement of 2,3-epoxy sulfides; regiospecific trapping of thiiranium ion intermediates with nitrogen heterocycles and amides. Use of imines as nucleophilic equivalents for the selective monoalkylation of primary amines

[3.3] Sigmatropy within 1-vinyl-2-alkenyl-7,7-dimethyl-exo-norbornan-2-ols. The first atropselective oxyanionic Cope rearrangement

Synthesis of trans-fused [5,5] bicyclic lactones/lactams as templates for serine protease inhibition

Functionalization reactions of a medium-ring bridgehead enone that skirt transannular bond formation

Direct oxygenation of enolates generated by anionic oxy-Cope rearrangement. Expedient preparation of polycyclic .alpha.-hydroxy ketones

Identification of [4-[4-(methylsulfonyl)phenyl]-6-(trifluoromethyl)-2-pyrimi-dinyl] amines and ethers as potent and selective cyclooxygenase-2 inhibitors

Lewis acid-induced rearrangement of 2,3-epoxy sulfides: regiospecific nucleophilic trapping of thiiranium ion intermediates with nitrogen nucleophiles

Synthesis of grevillins, novel pyrandione pigments of fungi. Biogenetic interrelationships between grevillins, pulvinic acids, terphenylquinones and xylerythrins

Discovery of an Orally Bioavailable NK1 Receptor Antagonist, (2S,3S)-(2-Methoxy-5-tetrazol-1-ylbenzyl)(2-phenylpiperidin-3-yl)amine (GR203040), with Potent Antiemetic Activity

The synthesis of a conformationally restrained, combined thromboxane antagonist / synthase inhibitor using an intramolecular ‘Stille’- or ‘Grigg’-palladium-catalysed cyclisation strategy

5,5- Trans lactone-containing inhibitors of serine proteases: Identification of a novel, acylating thrombin inhibitor

Synthetic [5,5] trans-fused indane lactones as inhibitors of thrombin

Reaction of α-amino esters and α-amino ester imines with thiiranium ion intermediates. Application to the synthesis of new potential aminopeptidase inhibitors and mechanistic implications

Addition of amino esters to thiiranium ion intermediates: A novel approach to the synthesis of new potential aminopeptidase inhibitors

Addition of Amino Esters to Thiiranium Ion Intermediates: A Novel Approach to the Synthesis of New Potential Aminopeptidase Inhibitors

Imines as Synthetic Equivalents of Primary Amines for the Nucleophilic Trapping of Thiiranium Ion Intermediates

Synthesis of grevillins and their biogenetic interrelationship with terphenylquinones, xylerythrins and pulvinic acid

Targeting the p300/CBP Axis in Lethal Prostate Cancer

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