Figure 4.

Synthesis and activity of compound R derivatives. A, synthesis of compound R analogs. Structures of IT2-171 and IT3-70a are shown here. B, activity of analogs in ATPase assays (Hsp72, DnaJA2, and BAG2 at 0.5, 0.1, and 0.25 μm, respectively). Results are the average of three independent experiments, each performed in triplicate ± S.D. In addition, compounds were tested for membrane permeability using cell growth assays in MDA-MB-231 breast cancer cells and normal MEFs. EC₅₀ values in cell experiments are the result of two independent experiments, each in triplicate ± S.D. The selectivity index is the EC₅₀ in MDA-MB-231 cells divided by the EC₅₀ in MEF cells.