Pd(0)-Catalyzed Direct Inter- and Intramolecular C–H Functionalization of 4-Carboxyimidazoles

Autor: Virginie Sophie Poncelet, Christophe Hoarau, Antoine Peresson, Thibaut Perse, Steven Frippiat, Christine Baudequin, Olivier Querolle, Cédric Schneider, Vincent Levacher, Patrick Angibaud, Lieven Meerpoel, Yvan Ramondenc, Laurent Bischoff

Publikováno v: SYNLETT
SYNLETT, Georg Thieme Verlag, 2020, 31 (10), pp.1015-2021. ⟨10.1055/s-0040-1708003⟩
SYNLETT, Georg Thieme Verlag, 2020, 31 (10), pp.1015-1021. ⟨10.1055/s-0040-1708003⟩

International audience; The palladium-catalyzed arylation and alkenylation of N-substituted methyl imidazole-4-carboxylates are described through inter- and intramolecular pathways. Both direct C2–H and C5–H arylation and alkenylation proceed und

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c9434a083cc8e00032950a76fb30e594
https://hal-normandie-univ.archives-ouvertes.fr/hal-02548986

Long-Lasting Enfuvirtide Carrier Pentasaccharide Conjugates with Potent Anti-Human Immunodeficiency Virus Type 1 Activity

Autor: Thierry Huet, Guy Dubreucq, Romain Mazinghien, Heidi Bompais, Loïc Vincent, Maurice Petitou, Arnaud Salvador, Jérôme Lemoine, Jan Balzarini, Cécile Gauchet, Olivier Querolle, Pascal Clayette, Dominique Schols, Bruno Lucidi, Olivier Kerbarh

Publikováno v: Antimicrobial Agents and Chemotherapy. 54:134-142

Enfuvirtide (also known as Fuzeon, T-20, or DP-178) is an antiretroviral fusion inhibitor which prevents human immunodeficiency virus type 1 (HIV-1) from entering host cells. This linear 36-mer synthetic peptide is indicated, in combination with othe

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7d7d17aedc7e1f5327a73158280ea973
https://doi.org/10.1128/aac.00827-09

Synthesis of Novel Macrocyclic Docetaxel Analogues. Influence of Their Macrocyclic Ring Size on Tubulin Activity

Autor: Françoise Guéritte, Joëlle Dubois, Sara Montiel-Smith, Olivier Querolle, Sylviane Thoret, Fanny Roussi, Daniel Guenard

Publikováno v: Journal of Medicinal Chemistry. 46:3623-3630

This work describes the synthesis of a series of novel macrocyclic taxoids 3 and 3(H) designed to mimic the docetaxel solid-state ("nonpolar") conformation. These compounds, bearing 18-, 20-, 21-, and 22-membered rings connecting the C-2 OH and C-3'

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3508329addaf9b3cc391797ed25f5740
https://doi.org/10.1021/jm030770w

Abstract 4199: Inhibition of NF-kB inducing kinase (NIK) selectively abrogates NIK and TRAF3 mutant multiple myeloma tumor growth

Autor: Boudewijn Janssens, Ian Stansfield, Hillary Millar, Yannick Ligny, Marc Salvati, Matthias Versele, Lieven Meerpoel, Gross Gerhard Max, Ricardo Attar, Sophie Nocquet-Thibault, Charles P. Theuer, Csoka Imre Christian, James P. Edwards, Tamara Geerts, Lut Janssen, Edgar Jacoby, Virginie Tronel, Y R F Simonnet, Laurie Lenox, Olivier Querolle, Nathalie Claudie Isabelle Amblard, Sriram Balasubramanian, Wim Floren, Virginie Sophie Poncelet

Publikováno v: Cancer Research. 77:4199-4199

Enhanced NF-kB signaling is a hallmark of aggressive lymphoid malignancies, including multiple myeloma (MM), mantle cell lymphoma (MCL), and diffuse large B-cell lymphoma (DLBCL). Non-canonical NF-kB signaling involves NIK-dependent activation of IKK

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::feb3cdad510f1cd0028dfe83b41470b9
https://doi.org/10.1158/1538-7445.am2017-4199

Palladium catalyzed one-pot sequential Suzuki cross-coupling-direct C-H functionalization of imidazo[1,2-a]pyrazines

Autor: Philippe Jubault, Jean‐Francois Bonfanti, Christophe Hoarau, Vincent Gembus, Olivier Querolle, Vincent Levacher

Publikováno v: Organic Letters
Organic Letters, American Chemical Society, 2012, 14 (23), pp.6012-6015. ⟨10.1021/ol3029059⟩

An efficient “one-pot” selective functionalization at C3/C6 of imidazo[1,2-a]pyrazines has been developed via a palladium-catalyzed sequential Suzuki–Miyaura cross-coupling/direct C–H arylation, vinylation, and benzylation. The procedure rema

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fd4c52efa0dd37f4d79cf056e26a0dc7
https://pubmed.ncbi.nlm.nih.gov/23151283