Discovery of 2-(3-Benzamidopropanamido)thiazole-5-carboxylate Inhibitors of the Kinesin HSET (KIFC1) and the Development of Cellular Target Engagement Probes.

Autor: Saint-Dizier F; Centre for Cancer Drug Discovery, Division of Cancer Therapeutics, The Institute of Cancer Research, London SW7 3RP, U.K., Matthews TP; Centre for Cancer Drug Discovery, Division of Cancer Therapeutics, The Institute of Cancer Research, London SW7 3RP, U.K., Gregson AM; Centre for Cancer Drug Discovery, Division of Cancer Therapeutics, The Institute of Cancer Research, London SW7 3RP, U.K., Prevet H; Centre for Cancer Drug Discovery, Division of Cancer Therapeutics, The Institute of Cancer Research, London SW7 3RP, U.K., McHardy T; Centre for Cancer Drug Discovery, Division of Cancer Therapeutics, The Institute of Cancer Research, London SW7 3RP, U.K., Colombano G; Centre for Cancer Drug Discovery, Division of Cancer Therapeutics, The Institute of Cancer Research, London SW7 3RP, U.K., Saville H; Centre for Cancer Drug Discovery, Division of Cancer Therapeutics, The Institute of Cancer Research, London SW7 3RP, U.K., Rowlands M; Centre for Cancer Drug Discovery, Division of Cancer Therapeutics, The Institute of Cancer Research, London SW7 3RP, U.K., Ewens C; Centre for Cancer Drug Discovery, Division of Cancer Therapeutics, The Institute of Cancer Research, London SW7 3RP, U.K., McAndrew PC; Centre for Cancer Drug Discovery, Division of Cancer Therapeutics, The Institute of Cancer Research, London SW7 3RP, U.K., Tomlin K; Centre for Cancer Drug Discovery, Division of Cancer Therapeutics, The Institute of Cancer Research, London SW7 3RP, U.K., Guillotin D; Centre for Cancer Drug Discovery, Division of Cancer Therapeutics, The Institute of Cancer Research, London SW7 3RP, U.K., Mak GW; Centre for Cancer Drug Discovery, Division of Cancer Therapeutics, The Institute of Cancer Research, London SW7 3RP, U.K., Drosopoulos K; Breast Cancer Now Research Centre, The Institute of Cancer Research, London SW7 3RP, U.K., Poursaitidis I; Centre for Cancer Drug Discovery, Division of Cancer Therapeutics, The Institute of Cancer Research, London SW7 3RP, U.K., Burke R; Centre for Cancer Drug Discovery, Division of Cancer Therapeutics, The Institute of Cancer Research, London SW7 3RP, U.K., van Montfort R; Centre for Cancer Drug Discovery, Division of Cancer Therapeutics, The Institute of Cancer Research, London SW7 3RP, U.K.; Division of Structural Biology, The Institute of Cancer Research, London SW7 3RP, U.K., Linardopoulos S; Centre for Cancer Drug Discovery, Division of Cancer Therapeutics, The Institute of Cancer Research, London SW7 3RP, U.K.; Breast Cancer Now Research Centre, The Institute of Cancer Research, London SW7 3RP, U.K., Collins I; Centre for Cancer Drug Discovery, Division of Cancer Therapeutics, The Institute of Cancer Research, London SW7 3RP, U.K.

Publikováno v: Journal of medicinal chemistry [J Med Chem] 2023 Feb 23; Vol. 66 (4), pp. 2622-2645. Date of Electronic Publication: 2023 Feb 07.

A fragment-based approach towards the discovery of N-substituted tropinones as inhibitors of Mycobacterium tuberculosis transcriptional regulator EthR2.

Autor: Prevet H; Univ. Lille, Inserm, Institut Pasteur de Lille, U1177 - Drugs and Molecules for Living Systems, F-59000, Lille, France., Moune M; Institut Pasteur de Lille, Univ. Lille, CNRS, Inserm, CHU Lille, U1019-UMR8204-CIIL-Centre d'Infection et d'Immunité de Lille, F-59000, Lille, France., Tanina A; Unité Microbiologie, Bioorganique et Macromoléculaire (CP206/04), département R3D, Faculté de Pharmacie, Université Libre de Bruxelles, B-1050, Brussels, Belgium., Kemmer C; Bioversys AG, Hochbergerstrasse 60C, 4057, Basel, Switzerland., Herledan A; Univ. Lille, Inserm, Institut Pasteur de Lille, U1177 - Drugs and Molecules for Living Systems, F-59000, Lille, France., Frita R; Institut Pasteur de Lille, Univ. Lille, CNRS, Inserm, CHU Lille, U1019-UMR8204-CIIL-Centre d'Infection et d'Immunité de Lille, F-59000, Lille, France., Wohlkönig A; Structural Biology Brussels, Vlaams Instituut voor Biotechnology (VIB), B-1050, Brussels, Belgium., Bourotte M; Bioversys AG, Hochbergerstrasse 60C, 4057, Basel, Switzerland., Villemagne B; Univ. Lille, Inserm, Institut Pasteur de Lille, U1177 - Drugs and Molecules for Living Systems, F-59000, Lille, France., Leroux F; Univ. Lille, Inserm, Institut Pasteur de Lille, U1177 - Drugs and Molecules for Living Systems, F-59000, Lille, France., Gitzinger M; Bioversys AG, Hochbergerstrasse 60C, 4057, Basel, Switzerland., Baulard AR; Institut Pasteur de Lille, Univ. Lille, CNRS, Inserm, CHU Lille, U1019-UMR8204-CIIL-Centre d'Infection et d'Immunité de Lille, F-59000, Lille, France., Déprez B; Univ. Lille, Inserm, Institut Pasteur de Lille, U1177 - Drugs and Molecules for Living Systems, F-59000, Lille, France., Wintjens R; Unité Microbiologie, Bioorganique et Macromoléculaire (CP206/04), département R3D, Faculté de Pharmacie, Université Libre de Bruxelles, B-1050, Brussels, Belgium., Willand N; Univ. Lille, Inserm, Institut Pasteur de Lille, U1177 - Drugs and Molecules for Living Systems, F-59000, Lille, France. Electronic address: nicolas.willand@univ-lille.fr., Flipo M; Univ. Lille, Inserm, Institut Pasteur de Lille, U1177 - Drugs and Molecules for Living Systems, F-59000, Lille, France.

Publikováno v: European journal of medicinal chemistry [Eur J Med Chem] 2019 Apr 01; Vol. 167, pp. 426-438. Date of Electronic Publication: 2019 Feb 10.

Isothiourea-catalyzed asymmetric synthesis of β-lactams and β-amino esters from arylacetic acid derivatives and N-sulfonylaldimines.

Autor: Smith SR; EaStCHEM, School of Chemistry, University of St Andrews , North Haugh, St Andrews KY16 9ST, U.K., Douglas J, Prevet H, Shapland P, Slawin AM, Smith AD

Publikováno v: The Journal of organic chemistry [J Org Chem] 2014 Feb 21; Vol. 79 (4), pp. 1626-39. Date of Electronic Publication: 2014 Feb 05.

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Rubrolone production by Dactylosporangium vinaceum: biosynthesis, modulation and possible biological function.

Autor: Moureu, Sophie¹ (AUTHOR), Caradec, Thibault¹ (AUTHOR), Trivelli, Xavier² (AUTHOR), Drobecq, Hervé¹ (AUTHOR), Beury, Delphine^1,3 (AUTHOR), Bouquet, Peggy¹ (AUTHOR), Caboche, Segolene^1,3 (AUTHOR), Desmecht, Eva¹ (AUTHOR), Maurier, Florence^1,3 (AUTHOR), Muharram, Ghaffar¹ (AUTHOR), Villemagne, Baptiste⁴ (AUTHOR), Herledan, Adrien⁴ (AUTHOR), Hot, David^1,3 (AUTHOR), Willand, Nicolas⁴ (AUTHOR), Hartkoorn, Ruben Christiaan¹ (AUTHOR) ruben.hartkoorn@inserm.fr

Publikováno v: Applied Microbiology & Biotechnology. Jul2021, Vol. 105 Issue 13, p5541-5551. 11p.