Synthesis, Reaction, and Cytotoxicity of Novel Propargylic Sulfones.

Abstract Propargylic sulfones 1 and 2 have been synthesized for their potent interactions with DNA. The crown ether conjugate 8 was also prepared from 1 under carefully established reaction conditions. The synthesized propargylic sulfones 2, 5, and 8 exhibited high reactivity toward sulfur-, nitrogen-, and oxygen-containing nucleophiles. Compound 1 showed an IC50 of 5.3×10−6 M against KB/P cancer cells comparable with that of the clinically used agent 5-FU.