Design of Cytotoxic Conjugates of Indole-3-glyoxylamides and 3,5-Bis(benzylidene)piperidin-4-ones by Click Chemistry Using Molecular Hybridization Strategy

The reaction of indole-3-glyoxylyl chloride with α,ω-azidoalkanols and α,ω-azidoalkylamines afforded azide analogues of indibulin. The latter were reacted with acetylene derivatives of 3,5-bis(benzylidene)piperidin-4-ones using click chemistry approaches. The resulting conjugates were tested for antiproliferative activity.