1070195-62-8Relevant articles and documents
Toward a Greener Barluenga-Valdés Cross-Coupling: Microwave-Promoted C-C Bond Formation with a Pd/PEG/H2O Recyclable Catalytic System
Lamaa, Diana,Messe, Estelle,Gandon, Vincent,Alami, Mouad,Hamze, Abdallah
, p. 8708 - 8712 (2019/11/03)
A green Barluenga-Valdés cross-coupling reaction for the synthesis of 1,1-diarylethylenes using palladium catalysis has been developed. The new catalytic system based on Pd/Xphos-SO3Na or Pd/MeDavephos-CF3SO3 in PEG/H2O under microwave irradiation was found to be the best conditions for this transformation. The recyclability of the palladium catalyst system was also studied, and it was found to be active over nine runs without significant loss in its activity.
Synthesis, biological evaluation, and structure-activity relationships of tri- and tetrasubstituted olefins related to isocombretastatin A-4 as new tubulin inhibitors
Aziz, Jessy,Brachet, Etienne,Hamze, Abdallah,Peyrat, Jean-Fran?ois,Bernadat, Guillaume,Morvan, Estelle,Bignon, Jér?me,Wdzieczak-Bakala, Joanna,Desravines, Déborah,Dubois, Joelle,Tueni, Marie,Yassine, Ahmad,Brion, Jean-Daniel,Alami, Mouad
, p. 430 - 442 (2013/02/23)
The synthesis and structure-activity relationships associated with a series of 1,1-diarylethylene tubulin polymerization inhibitors 3 and 4 are described. The key step for their preparation involves a palladium-catalyzed coupling of N-arylsulfonylhydrazon
Discovery of Isoerianin Analogues as Promising Anticancer Agents
Messaoudi, Samir,Hamze, Abdallah,Provot, Olivier,Treguier, Bret,RodrigoDeLosada, Jordi,Bignon, Jerome,Liu, Jian-Miao,Wdzieczak-Bakala, Joanna,Thoret, Sylviane,Dubois, Joelle,Brion, Jean-Daniel,Alami, Mouad
scheme or table, p. 488 - 497 (2011/12/22)
The cytotoxic activity of a series of 23 new isoerianin derivatives with modifications on both the A and B rings was studied. Several compounds exhibited excellent antiproliferative activity at nanomolar concentrations against a panel of human cancer cell lines. The most cytotoxic compound, isoerianin (3), strongly inhibits tubulin polymerization in the micromolar range. Moreover, isoerianin leads to G2/M phase cell-cycle arrest in H1299 and K562 cancer cells, and strongly induces apoptosis. Isoerianin also disrupts the vessel-like structures formed by human umbilical vein endothelial cells (HUVECs) invitro, suggesting that this compound may act as a vascular disrupting agent. It clearly appears that in this compound series, the 1,1-ethane bridge encountered in isoerianin derivatives can replace the 1,2-ethane bridge of natural erianin with no loss of activity. This reinforces the bioisosteric replacement approach in the combretastatin series previously reported by our research group.