(-)-Epigallocatechin gallate (EGCG 1) is the most abundant catechin in green tea leaves and exhibits various biological activities, including anticancer and anti-allergic effects. The 67-kDa laminin receptor (67LR) has been identified as a receptor for EGCG, mediating its therapeutic actions. Studies on naturally occurring EGCG-related compounds have suggested that the gallate moiety (D ring) is a crucial pharmacophore for 67LR binding. Furthermore, a combinatorial synthesis and biological evaluation of methylated EGCG have demonstrated that methylation of the hydroxy group at the A and B rings does not significantly reduce biological activity. These results suggested that the A or B ring is a suitable position of EGCG for modification with functional groups, such as fluorescent dyes or reactive functional groups at the A and B rings without compromising the biological activity of EGCG. Indeed, the EGCG derivatives 3 and 4 possessing a fluorescent dye linked through the A ring were reported to be chemical probes for analysis and imaging of EGCG.