Publications
497 results found
Ali S, Patel H, Periyasamy M, et al., 2016, ICEC0942, an orally bioavailable selective inhibitor of CDK7 for breast cancer, UK Breast Cancer Research Symposium, Publisher: Springer Verlag, Pages: 195-195, ISSN: 0167-6806
Barrett AGM, Elliott D, Ma T, et al., 2016, Sequential Ketene Generation from Dioxane-4,6-dione-keto-dioxinones for the Synthesis of Terpenoid Resorcylates, Organic Letters, Vol: 18, Pages: 1800-1803, ISSN: 1523-7060
Trapping of the ketene generated from the thermolysis of 2-methyl-2-phenyl-1,3-dioxane-4,6-dione-ketodioxinoneat 50 °C with primary, secondary, or tertiary alcohols gave the corresponding dioxinone β-keto-esters in good yieldunder neutral conditions. These intermediates were converted by palladium(0)-catalyzed decarboxylative allyl migration andaromatization into the corresponding β-resorcylates. These transformations were applied to the syntheses of the natural products(±)-cannabiorcichromenic and (±)-daurichromenic acid.
Doepner AM, Aboagye EO, Barrett AGM, 2015, 2 '-Deoxy-2 ',2 '-difluorothymidine analogues for radiolabeling with fluorine-18 and other biomedical applications, TETRAHEDRON LETTERS, Vol: 56, Pages: 3293-3297, ISSN: 0040-4039
Cookson R, Barrett TN, Barrett AGM, 2015, β-Keto-dioxinones and β,δ-Diketo-dioxinones in Biomimetic Resorcylate Total Synthesis, ACCOUNTS OF CHEMICAL RESEARCH, Vol: 48, Pages: 628-642, ISSN: 0001-4842
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- Citations: 38
Palma A, Serginson JM, Barrett AGM, 2015, Synthesis of poly β ketoesters via double acylketene trapping, TETRAHEDRON LETTERS, Vol: 56, Pages: 674-676, ISSN: 0040-4039
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- Citations: 1
Barrett TN, Barrett AGM, 2014, Cascade polyketide and polyene cyclizations: biomimetic total synthesis of hongoquercin B, Journal of the American Chemical Society, Vol: 136, Pages: 17013-17015, ISSN: 0002-7863
The total synthesis of hongoquercin B was carried out in 9 steps from trans,trans-farnesyl acetate using a palladium catalyzed decarboxylative π-farnesyl rearrangement of a diketo-dioxinone ester, aromatization and cationic diene-epoxide cyclization as key steps. This cascade tetracyclization simplifies the synthesis of terpenoid resorcylate natural products.
Kim M-S, Buisson LA, Heathcote DA, et al., 2014, Approaches to design non-covalent inhibitors for human granzyme B (hGrB), ORGANIC & BIOMOLECULAR CHEMISTRY, Vol: 12, Pages: 8952-8965, ISSN: 1477-0520
Reid S, Barrett AGM, Hill MS, et al., 2014, Heavier Alkaline Earth Catalyzed Ene-yne Cyclizations: Atom-Efficient Access to Tetrahydroisoquinoline Frameworks, ORGANIC LETTERS, Vol: 16, Pages: 6016-6019, ISSN: 1523-7060
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- Citations: 11
Barrett TN, Patel BH, Barrett AGM, 2014, Synthesis of <i>C</i>-5-substituted resorcylates and resorcinamides via formylation-aromatization of functionalized keto-dioxinones, TETRAHEDRON, Vol: 70, Pages: 6894-6901, ISSN: 0040-4020
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- Citations: 4
Brookes PA, Barrett AGM, 2014, Iodoaromatization Reactions of Enyne-Dioxinones: Syntheses of 4<i>H</i>-1,3-Benzodioxin-4-ones, Masked Pentasubstituted Arenes, JOURNAL OF ORGANIC CHEMISTRY, Vol: 79, Pages: 8706-8714, ISSN: 0022-3263
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- Citations: 8
Anderson K, Laclef S, Barrett AGM, 2014, Mechanistic studies of highly regioselective decarboxylative-prenyl migration reactions of prenyloxycarbonyl-diketo-dioxinones, TETRAHEDRON, Vol: 70, Pages: 5569-5579, ISSN: 0040-4020
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- Citations: 7
Loerbroks C, Boeker B, Cordes J, et al., 2014, Spiroaminals - Crystal Structure and Computational Investigation of Conformational Preferences and Tautomerization Reactions, EUROPEAN JOURNAL OF ORGANIC CHEMISTRY, Vol: 2014, Pages: 5476-5486, ISSN: 1434-193X
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- Citations: 3
Blencowe PS, Barrett AGM, 2014, Biomimetic Synthesis of Functionalized γ-Resorcylates from Dioxinone Derivatives, EUROPEAN JOURNAL OF ORGANIC CHEMISTRY, Vol: 2014, Pages: 4844-4853, ISSN: 1434-193X
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- Citations: 5
Cookson R, Poeverlein C, Lachs J, et al., 2014, Synthetic Studies towards Radicicol through Biomimetic Macrolactonization and Transannular Aromatization Reactions, EUROPEAN JOURNAL OF ORGANIC CHEMISTRY, Vol: 2014, Pages: 4523-4535, ISSN: 1434-193X
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- Citations: 8
Trivedi ER, Ma Z, Waters EA, et al., 2014, Synthesis and characterization of a porphyrazine-Gd(III) MRI contrast agent and <i>in vivo</i> imaging of a breast cancer xenograft model, CONTRAST MEDIA & MOLECULAR IMAGING, Vol: 9, Pages: 313-322, ISSN: 1555-4309
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- Citations: 16
Brookes PA, Cordes J, White AJP, et al., 2013, Total Synthesis of Mycophenolic Acid by a Palladium-Catalyzed Decarboxylative Allylation and Biomimetic Aromatization Sequence, EUROPEAN JOURNAL OF ORGANIC CHEMISTRY, Vol: 2013, Pages: 7313-7319, ISSN: 1434-193X
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- Citations: 20
George NS, Anderson KE, Barrett AGM, 2013, Total Synthesis of Cristatic Acid Based on Late-Stage Decarboxylative Allylic Migration and Biomimetic Aromatization of a Diketo Dioxinone, EUROPEAN JOURNAL OF ORGANIC CHEMISTRY, Vol: 2013, Pages: 7604-7610, ISSN: 1434-193X
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- Citations: 8
Cordes J, Murray PRD, White AJP, et al., 2013, 1,7-Diazaspiro[5.5]undecane - A Neglected Heterocycle, ORGANIC LETTERS, Vol: 15, Pages: 4992-4995, ISSN: 1523-7060
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- Citations: 7
Kaliszczak M, Patel H, Kroll SHB, et al., 2013, Development of a cyclin-dependent kinase inhibitor devoid of ABC transporter-dependent drug resistance, British Journal of Cancer, Vol: 109, Pages: 2356-2367, ISSN: 1532-1827
background: Cyclin-dependent kinases (CDKs) control cell cycle progression, RNA transcription and apoptosis, making them attractive targets for anticancer drug development. Unfortunately, CDK inhibitors developed to date have demonstrated variable efficacy.methods: We generated drug-resistant cells by continuous low-dose exposure to a model pyrazolo[1,5-a]pyrimidine CDK inhibitor and investigated potential structural alterations for optimal efficacy.results: We identified induction of the ATP-binding cassette (ABC) transporters, ABCB1 and ABCG2, in resistant cells. Assessment of features involved in the ABC transporter substrate specificity from a compound library revealed high polar surface area (>100 Å2) as a key determinant of transporter interaction. We developed ICEC-0782 that preferentially inhibited CDK2, CDK7 and CDK9 in the nanomolar range. The compound inhibited phosphorylation of CDK substrates and downregulated the short-lived proteins, Mcl-1 and cyclin D1. ICEC-0782 induced G2/M arrest and apoptosis. The permeability and cytotoxicity of ICEC-0782 were unaffected by ABC transporter expression. Following daily oral dosing, the compound inhibited growth of human colon HCT-116 and human breast MCF7 tumour xenografts in vivo by 84% and 94%, respectively.conclusion: We identified a promising pyrazolo[1,5-a]pyrimidine compound devoid of ABC transporter interaction, highly suitable for further preclinical and clinical evaluation for the treatment of cancer.
Miyatake-Ondozabal H, Barrett AGM, 2013, Synthetic studies towards tragoponol: preparation of a highly functionalized resorcylate, TETRAHEDRON LETTERS, Vol: 54, Pages: 4817-4820, ISSN: 0040-4039
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- Citations: 6
Cordes J, Barrett AGM, 2013, Synthesis of Macrosporin and Related 9,10-Anthraquinones by Biomimetic Polyketide Aromatization and Cyclization of 6-Benzylresorcylates, EUROPEAN JOURNAL OF ORGANIC CHEMISTRY, Vol: 2013, Pages: 1318-1326, ISSN: 1434-193X
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- Citations: 15
Patel BH, Barrett AGM, 2012, Total Synthesis of Resorcinol Amide Hsp90 Inhibitor AT13387, JOURNAL OF ORGANIC CHEMISTRY, Vol: 77, Pages: 11296-11301, ISSN: 0022-3263
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- Citations: 16
Rey J, Hu H, Snyder JP, et al., 2012, Synthesis on novel Tamoxifen derivatives, TETRAHEDRON, Vol: 68, Pages: 9211-9217, ISSN: 0040-4020
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- Citations: 11
Blencowe PS, Barrett AGM, 2012, Synthesis of 6-substituted salicylates via biomimetic aromatization utilizing the cross metathesis of a vinyl dioxinone with homoallylic alcohols, CANADIAN JOURNAL OF CHEMISTRY-REVUE CANADIENNE DE CHIMIE, Vol: 90, Pages: 975-984, ISSN: 0008-4042
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- Citations: 4
Rey J, Hu H, Kyle F, et al., 2012, Discovery of a New Class of Liver Receptor Homolog-1 (LRH-1) Antagonists: Virtual Screening, Synthesis and Biological Evaluation, CHEMMEDCHEM, Vol: 7, Pages: 1909-1914, ISSN: 1860-7179
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- Citations: 18
Brinkmann C, Barrett AGM, Hill MS, et al., 2012, Alkaline Earth Catalysis of Alkynyl Alcohol Hydroalkoxylation/Cyclization, ORGANOMETALLICS, Vol: 31, Pages: 7287-7297, ISSN: 0276-7333
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- Citations: 39
Trivedi ER, Blumenfeld CM, Wielgos T, et al., 2012, Multi-gram synthesis of a porphyrazine platform for cellular translocation, conjugation to Doxorubicin, and cellular uptake, TETRAHEDRON LETTERS, Vol: 53, Pages: 5475-5478, ISSN: 0040-4039
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- Citations: 15
Rey J, O'Riordan TJC, Hu H, et al., 2012, Design and Diastereoselective Synthesis of C-2,C-20-Diaryl Steroidal Derivatives, EUROPEAN JOURNAL OF ORGANIC CHEMISTRY, Vol: 2012, Pages: 3781-3794, ISSN: 1434-193X
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- Citations: 2
Fouche M, Rooney L, Barrett AGM, 2012, Biomimetic Total Synthesis of Cruentaren A via Aromatization of Diketodioxinones, JOURNAL OF ORGANIC CHEMISTRY, Vol: 77, Pages: 3060-3070, ISSN: 0022-3263
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- Citations: 50
Cordes J, Laclef S, White AJP, et al., 2012, Palladium(0)-Catalyzed Allylic Alkylation of Diketoester-Dioxinones with Allyl Acetates under Neutral Conditions: Synthesis of Hexasubstituted Benzene Derivatives, JOURNAL OF ORGANIC CHEMISTRY, Vol: 77, Pages: 3524-3530, ISSN: 0022-3263
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- Citations: 14
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