Optimized N-phenyl-N′-(2-chloroethyl)ureas as potential antineoplastic agents: Synthesis and growth inhibition activity - Université Clermont Auvergne Accéder directement au contenu
Article Dans Une Revue Bioorganic and Medicinal Chemistry Année : 2005

Optimized N-phenyl-N′-(2-chloroethyl)ureas as potential antineoplastic agents: Synthesis and growth inhibition activity

Jean L C Rousseau
  • Fonction : Auteur
Eric Petitclerc
  • Fonction : Auteur
René C-Gaudreault
  • Fonction : Auteur
Jean L.C. Rousseau
  • Fonction : Auteur
Éric Petitclerc
  • Fonction : Auteur
René C.-Gaudreault
  • Fonction : Auteur

Résumé

In our ongoing research program aimed at the optimization of microtubule-self-assembly disrupting agents, we have prepared three series of phenylurea analogues (CEU), derived from N-(3-omega-hydroxyalkyl or 4-omega-hydroxyalkyl or 3-omega-hydroxyalkynyl)-phenyl-N'-(2-chloroethyl)ureas. Most compounds exhibit potent growth inhibitory activity on human colon carcinoma HT-29, human skin melanoma M21, and human breast carcinoma MCF-7 tumor cell lines, with a GI50 ranging from 250 nM to 8 microM. Among these new molecules, three CEUs exhibit GI50 in the nanomolar range. They are more potent by approximately an order of magnitude than previously described CEU analogues. As such, they are attractive hit compounds for the development of potent new alkylating antitubulin drugs.

Dates et versions

hal-01677590 , version 1 (08-01-2018)

Identifiants

Citer

Emmanuel Moreau, Sébastien Fortin, Michel Desjardins, Jean L C Rousseau, Eric Petitclerc, et al.. Optimized N-phenyl-N′-(2-chloroethyl)ureas as potential antineoplastic agents: Synthesis and growth inhibition activity. Bioorganic and Medicinal Chemistry, 2005, 13 (24), pp.6703 - 6712. ⟨10.1016/j.bmc.2005.07.048⟩. ⟨hal-01677590⟩
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