Antiproliferative Activity of the Cyclization Products of 1-(2-Oxocyclohexyl)Ethane-1,1,2,2-Tetracarbonitrile and α,β-Unsaturated Aldehydes

Abstract

The antiproliferative activity of previously obtained 3-R-6-imino-2,7-dioxabicyclo[3.2.1.]octane-4,4,5-tricarbonitriles was tested on 59 cell lines obtained from human lung, colon, brain, ovary, kidney, prostate, and breast tumors and leukemia and melanoma. The most pronounced effect was observed against blood cancer cell lines of leukemia. The strength of the activity and specificity of the compounds on certain types of cells were related directly to the nature of the 3-substituent on the 2,7-dioxabicyclo[3.2.1]octane core. Compounds with multiple bonds and alkyl radicals exhibited more pronounced cytotoxic activity. A compound with a coumarin moiety showed high activity exceeding those of reference drugs (dacarbazine, cisplatin) with respect to kidney cancer cell lines.