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“Introduction Isothioureas are a class of amphiphilic compounds carrying a highly basic isothiourea function of pKa ≈ 10. Therefore, at physiological pH these compounds exist in a protonated (cationic)

form that may be important for their specific biological effects. In solid state they form salts of usually better water solubility then that of the substrates used for their synthesis. Reports on anticancer activity of isothioureas are very scarce. S-(10-undecen-1-yl)isothiouronium iodide was found to be effective against Walker carcinoma cells in rats (Carmona Monoiodotyrosine and Gonzalez-Cadavid, 1978; Gonzalez-Cadavid and Herrera Quijada, 1974), and bisisothiouronium derivatives of thiophene were reported to show activity against Yoshida sarcoma (Gogte et al., 1967). Recently, a report showing proapoptotic activity of a number of pentabromobenzylisothiourea derivatives with substantial cytotoxicity toward human glioblastoma cells has been published. The efficacy of the latter compounds was

higher than that of the well-known casein kinase 2 (CK2) inhibitor 4,5,6,7-tetrabromo-1H-benzotriazole (TBB), and was similar to that of 4,5,6,7-tetrabromo-1H-benzimidazole (TBI). Cell death induced in rat and human malignant glioma cells by the pentabromobenzylisothiourea derivatives was associated with a decrease in mitochondrial membrane potential and with activation of caspase-3 and caspase-7 followed by PARP cleavage (Kaminska et al., 2009). More attention was given to isothioureas as inhibitors of nitric oxide synthase (NOS) FK506 mouse isoforms. These enzymes play a significant and multifaceted role in both physiology and pathology; therefore, there is an ongoing search for their effective inhibitors (Garvey et al., 1994; Jin et al., 2009; Rairigh et al., 1998; Kalish et al., 2002).