C(sp3)–H arylation to construct all-syn cyclobutane-based heterobicyclic systems: a novel fragment collection

Autor: Thomas J. Osberger, Thomas A. King, David R. Spring, Sarah L. Kidd

Publikováno v: Chemical Communications. 56:7423-7426

All-syn fused cyclobutanes remain an elusive chemotype and thus present an interesting synthetic challenge. Herein, we report the successful application of Pd-catalysed C(sp3)-H arylation of cyclobutane compounds to generate all-syn heterobicyclic fr

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::46972eb493a01ed3b9cdd54b0d89ac58
https://doi.org/10.1039/d0cc03237a

Hydroxylated Rotenoids Selectively Inhibit the Proliferation of Prostate Cancer Cells

Autor: Sarah L. Kidd, Hannah F. Sore, Hannah R. Bridges, Judy Hirst, David R. Spring, Riccardo Serreli, Thomas J. Osberger, Natalia Mateu, David A. Russell

Publikováno v: J Nat Prod

Prostate cancer is one of the leading causes of cancer-related death in men. The identification of new therapeutics to selectively target prostate cancer cells is therefore vital. Recently, the rotenoids rotenone (1) and deguelin (2) were reported to

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4e15420281a66344ed014bb21a8bbf14
https://europepmc.org/articles/PMC7611836/

Fsp3-rich and diverse fragments inspired by natural products as a collection to enhance fragment-based drug discovery

Autor: Abigail R. Hanby, Sarah L. Kidd, Thomas J. Osberger, Kim T. Mortensen, Nikolaj S. Troelsen, David R. Spring

Publikováno v: Hanby, A R, Troelsen, N S, Osberger, T J, Kidd, S L, Mortensen, K T & Spring, D R 2020, ' Fsp 3-rich and diverse fragments inspired by natural products as a collection to enhance fragment-based drug discovery ', Chemical Communications, vol. 56, 2280 . https://doi.org/10.1039/c9cc09796a

Herein, we describe the natural product inspired synthesis of 38 complex small molecules based upon 20 unique frameworks suitable for fragment-based screening. Utilising an efficient strategy, two key building block diastereomers were harnessed to ge

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d6a1a40755682a5ada095e4f5f3638d9
https://orbit.dtu.dk/en/publications/cb26f2f3-abf9-4018-a2c5-b8d91361bb70

Oxidative diversification of amino acids and peptides by small-molecule iron catalysis

Autor: Thomas J. Osberger, Donald C. Rogness, Antonia F. Stepan, M. Christina White, Jeffrey T. Kohrt

Publikováno v: Nature

Secondary metabolites synthesized by nonribosomal peptide synthetases (NRPSs) display diverse and complex topologies and possess an impressive range of biological activities1,2 Much of this diversity derives from a synthetic strategy that entails the

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a91e2822b103e70bf5807e8612160887
https://doi.org/10.1038/nature18941

N-Boc Amines to Oxazolidinones via Pd(II)/Bis-sulfoxide/Brønsted Acid Co-Catalyzed Allylic C–H Oxidation

Autor: Thomas J. Osberger, M. Christina White

Publikováno v: Journal of the American Chemical Society

A Pd(II)/bis-sulfoxide/Brønsted acid catalyzed allylic C-H oxidation reaction for the synthesis of oxazolidinones from simple N-Boc amines is reported. A range of oxazolidinones are furnished in good yields (avg 63%) and excellent diastereoselectivi

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7026dd11ddd4921bcc41277723c5d8b7
https://doi.org/10.1021/ja506036q