ANTICARCINOMA ACTIVITY OF A NOVEL DRUG, 3-ETHYL-3'-METHYLTHIATELLURACARBOCYANINE IODIDE (TE), A TELLURIUM-CONTAINING CYANINE TARGETED AT MITOCHONDRIA

Lipophilic cationic compounds such as rhodamine 123, AA1, and dequalin ium chloride have been reported to constitute a new class of anticarci noma agents based on their selective localization, accumulation, and r etention within the mitochondria of certain carcinoma cells, After scr eening more than 1000 lipophilic cationic compounds in clonogenic assa ys, we found that a tellurium-containing cyanine, 3-ethyl-3'-methyl-th iatelluracarbocyanine iodide (Te), exhibits significant anticarcinoma activity, In vitro testing showed that Te was 64-fold more toxic to th e carcinoma cell line CX-1 than to the normal epithelial cell line CV- 1, In vivo testing showed that Te significantly prolonged the survival of mice implanted with tumors, For C57BL x DBA/2 F-1, mice implanted with the mouse bladder carcinoma cell line MB49, the treated:control ( T:C) ratio ranged from 250 to 268%, For Swiss nu/nu mice implanted wit h the human melanoma cell line LOX, the T:C ratio ranged from 176 to 2 70%, For Swiss nu/nu mice implanted with the human ovarian tumor cell line OVCA-III, the T:C ratio was 344%, These anticarcinoma activities warrant further investigation of Te as a potential anticarcinoma agent .