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Issue 19, 2012
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Exploiting conformationally restricted N,N′-dimethyl-N,N′-diarylureas as biologically active C[double bond, length as m-dash]C double bond analogues: synthesis and biological evaluation of combretastatin A-4 analogues

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Abstract

The biological efficacy of a number of suitably functionalised conformationally restricted N,N′-dimethyl-N,N′-diarylureas, which occupy a similar 3-dimensional space to combretastatin A-4 (CA4), has been evaluated for their ability to inhibit tubulin polymerisation and inhibit the growth of short term glioblastoma multiforme (GBM) cell cultures and an established GBM cell line (U251MG). The results show that the ureas most like CA4, with regards to benzene ring oxygenation and overall shape, are the most active.

Graphical abstract: Exploiting conformationally restricted N,N′-dimethyl-N,N′-diarylureas as biologically active C [[double bond, length as m-dash]] C double bond analogues: synthesis and biological evaluation of combretastatin A-4 analogues

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Supplementary files

Article information


Submitted
31 May 2012
Accepted
19 Jun 2012
First published
23 Jul 2012

RSC Adv., 2012,2, 7557-7560
Article type
Paper

Exploiting conformationally restricted N,N′-dimethyl-N,N′-diarylureas as biologically active C[double bond, length as m-dash]C double bond analogues: synthesis and biological evaluation of combretastatin A-4 analogues

T. J. Snape, K. Karakoula, F. Rowther and T. Warr, RSC Adv., 2012, 2, 7557
DOI: 10.1039/C2RA21096G

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