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

Authors: Moreau, EmmanuelFortin, SébastienDesjardins, MichelRousseau, JeanPetitclerc, ÉricC. Gaudreault, René
Abstract: 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-ω-hydroxyalkyl or 4-ω-hydroxyalkyl or 3-ω-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 μM. 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.
Document Type: Article de recherche
Issue Date: 13 September 2005
Open Access Date: 25 April 2019
Document version: AM
Permalink: http://hdl.handle.net/20.500.11794/34573
This document was published in: Bioorganic & Medicinal Chemistry, Vol. 13 (24), 6703–6712 (2005)
Oxford Pergamon
Alternative version: 10.1016/j.bmc.2005.07.048
Collection:Articles publiés dans des revues avec comité de lecture

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