In:
ChemMedChem, Wiley, Vol. 4, No. 4 ( 2009-04-17), p. 588-593
Abstract:
Combretastatin A‐4 derivatives : A series of combretastatin A‐4‐derived 1‐benzyl‐4,5,6‐trimethoxyindoles was designed and prepared as a novel class of potent antimitotic agents acting through the colchicine binding site on the microtubule. magnified image A series of 1‐benzyl‐4,5,6‐trimethoxyindoles was designed and prepared as a novel class of potent antimitotic agents acting through the colchicine binding site of tubulin. Compounds 10 and 11 showed excellent antiproliferative activity with mean IC 50 values of 26 and 27 n M , respectively, in a diverse set of human cancer lines from different organs, including a MDR+ line. They also displayed substantial antitubulin efficacy with IC 50 values of 3.5 and 2.6 μ M , respectively, representing an improvement over colchicine (IC 50 =4.3 μ M ).
Type of Medium:
Online Resource
ISSN:
1860-7179
,
1860-7187
DOI:
10.1002/cmdc.200800405
Language:
English
Publisher:
Wiley
Publication Date:
2009
detail.hit.zdb_id:
2209649-8
SSG:
15,3
