Apoptosis-inducing effect of epolactaene derivatives on BALL-1 cells

Abstract

Epolactaene, a neuritogenic compound in human neuroblastoma SH-SY5Y, induces apoptosis in a human leukemia B-cell line, BALL-1. The apoptosis-inducing activities of 34 epolactaene derivatives, including those of the newly synthesized α-alkyl-α,β-epoxy-γ-lactam derivative and cyclopropane derivatives, were also tested. The structure–activity relationships of the epolactaene derivatives as an inducer of apoptosis are described. The α-acyl-α,β-epoxy-γ-lactam moiety as well as the hydrophobicity derived from the long alkyl side chain are both important for activity. Compound 1e displayed the strongest activity among all the synthesized compounds with an IC 50 value of 0.70 μM.