Exploiting conformationally restricted N,N′-dimethyl-N,N′-diarylureas as biologically active CC double bond analogues: synthesis and biological evaluation of combretastatin A-4 analogues

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.