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Nos livres ou articles en couvertures

Sequential One-Pot Synthesis of 3-Arylbenzofurans from N-Tosylhydrazones and Bromophenol Derivatives

The cover art (from CoSMIT team) shows an efficient one-pot sequence, allowing direct access to 3-arylbenzofuran derivatives starting from N-tosylhydrazones and bromophenols. This transformation, which involves a palladium/copper catalysis, enabled the synthesis of 3-arylated benzofurans bearing various substituents with good to excellent yields.

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Asian J. Org. Chem. 11/2017

Metal-Catalyzed Synthesis of 1,1-Diarylethylene

Timothée Naret, Olivier Provot, Mouad Alami*, Abdallah Hamze*

The cover picture, provided by Abdallah Hamze and co-workers summarizes the principal methodological studies concerning the synthesis of 1,1-diarylethylene compounds using metal catalysis, mainly focusing on palladium, nickel, copper, iron and gold catalyzed processes. More information can be found in the Focus Review :

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Advanced Synthesis Catalyst 11/2016

N -Tosylhydrazones in Action

Adv. Synth. Catal. 200000, 00, 1 – 2

Timothée Naret, Pascal Retailleau, Jérôme Bignon, Jean-Daniel Brion, Mouad Alami,* Abdallah Hamze*

The cover picture, provided by Abdallah Hamze and co-workers, reports an efficient one-pot metal-catalyzed process between N-tosyl- hydrazones, N-(dihalophenyl)-imidates, and amines. During this trans- formation, one C C bond and two C N bonds were created by a single palladium-catalyzed reaction leading to a library of 5-(1-aryl- vinyl)-1H-benzimidazoles. Imidates were found to be an ideal partner for the cross-coupling with hydrazones in comparison with acet- amides. Among several derivatives evaluated, one compound exhibits excellent antiproliferative activity in the nanomolar concentration range. Details can be found in the full paper on pages xxxx–xxxx (T. Naret, P. Retailleau, J. Bignon, J.-D. Brion, M. Alami, A. Hamze, Adv. Synth. Catal. 2016, 358, xxxx–xxxx ; DOI : 10.1002/ adsc.201600173).

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Organic & Biomolecular Chemistry 01/2013

Scientists in France and Lebanon had previously synthesised and evaluated the biological properties of a series of 1,1-diarylethylene analogues of isocombretastatin A-4, which is related to the natural combretastatin A-4, an antitumour agent. Now, they have studied the effects of structural modifications on the linker between the two aromatic rings of the isocombretastatin A-4 to better understand the structure-activity relationships associated with this series of 1,1-diarylethylene tubulin polymerisation inhibitors. The new compounds exhibit potent cytotoxicity against cancer cell lines.

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