Both organelle-specific and receptor-mediated drug delivery systems have proven to be promising tools in anticancer therapy. We have previously shown the efficacy of tri-and pentamethine cyanine dyes in selectively delivering different cargos to the mitochondria of human cancer cell lines. Many cancer cells overexpress the folate receptor α, enabling the use of folate for targeting cancer cells, especially those derived from ovarian, breast and lung carcinomas. With these premises, we sought to improve the efficacy of existing proapoptotic peptides via conjugation with either cyanine dyes (compounds 6-9) or folate (10-12). We also attempted to combine the subcellular and receptor mediated delivery strategies by labelling those sequences with both cyanine dye 1 and folate (13-15).