2. Academic Validation
  3. Discovery of azaisoerianin derivatives as potential antitumors agents

Discovery of azaisoerianin derivatives as potential antitumors agents

  • Eur J Med Chem. 2014 May 6:78:178-89. doi: 10.1016/j.ejmech.2014.03.032.
Mohamed Ali Soussi 1,  Olivier Provot 1,  Guillaume Bernadat 1,  Jérome Bignon 2,  Joanna Wdzieczak-Bakala 2,  Déborah Desravines 2,  Joëlle Dubois 2,  Jean-Daniel Brion 1,  Samir Messaoudi 3,  Mouad Alami 4
Affiliations

Affiliations

  • 1 Univ Paris-Sud, CNRS, BioCIS-UMR 8076, Laboratoire de Chimie Thérapeutique, LabEx LERMIT, Equipe Labellisée Ligue Contre le Cancer, Faculté de Pharmacie, 5 rue J.-B. Clément, Châtenay-Malabry F-92296, France.
  • 2 Institut de Chimie des Substances Naturelles, UPR 2301, CNRS avenue de la terrasse, Gif sur Yvette F-91198, France.
  • 3 Univ Paris-Sud, CNRS, BioCIS-UMR 8076, Laboratoire de Chimie Thérapeutique, LabEx LERMIT, Equipe Labellisée Ligue Contre le Cancer, Faculté de Pharmacie, 5 rue J.-B. Clément, Châtenay-Malabry F-92296, France. Electronic address: samir.messaoudi@u-psud.fr.
  • 4 Univ Paris-Sud, CNRS, BioCIS-UMR 8076, Laboratoire de Chimie Thérapeutique, LabEx LERMIT, Equipe Labellisée Ligue Contre le Cancer, Faculté de Pharmacie, 5 rue J.-B. Clément, Châtenay-Malabry F-92296, France. Electronic address: mouad.alami@u-psud.fr.
PMID: 24681982 DOI: 10.1016/j.ejmech.2014.03.032
Abstract

A series of N-methyl-diarylamines 2 was designed and synthesized as a novel class of CA-4 and isoCA-4 analogues. Compounds 2b and 2m showed excellent antiproliferative activity with mean GI50 values at a nanomolar level in a diverse set of human Cancer cells. These compounds also inhibited tubulin assembly at a micromolar range, arrested the cellular cycle in the G2/M phase and induced Apoptosis at very low concentrations. Preliminary in vitro results revealed that 2b and 2m displayed substantial efficacy as potent antivascular agents. Docking studies indicates that these lead compounds showed a binding mode similar to those observed with isoCA-4 at the colchicine binding site of tubulin.

Keywords

Antimitotic; AzaisoCA-4; Combretastatin A-4; Cytotoxicity; IsoCA-4; Isoerianin; Tubulin.

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