The effects of substituted anthraquinones on intestinal motility were evaluated in-vitro using rabbit small intestinal strips. This structure-activity relationship study revealed the critical requirement of a hydroxy group at R2 position. The intestinal motility was inhibited 50% (IC50) by emodine (8 microM), 2-hydroxy anthraquinone (20 microM), 2,6-dihydroxy anthraquinone (25 microM), 2,7-dihydroxy anthraquinone (10 microM), 1,2,4-trihydroxy anthraquinone (80 microM) and 1,2,5,8-tetra-hydroxyanthraquinone (9 microM). The presence of other polar groups at R2 position such as an amino, aldehyde and carboxylic acid group significantly reduced the activity (IC50 360-400 microM). The presence of a methyl group and esterification of the carboxylic acid at R2 position was found to abolish the activity. These data are useful for the future development of anthraquinones as laxative agents.