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Published on: September 3, 2016
Apoptosis-inducing effect of epolactaene derivatives on BALL-1 cells
Kouji Kuramochi1, Rie Matsui, Yasuaki Matsubara
1Frontier Research Center for Genome and Drug Discovery, Tokyo University of Science, 2641 Yamazaki, Noda, Chiba 278-8510, Japan.
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 alpha-alkyl-alpha,beta-epoxy-gamma-lactam derivative and cyclopropane derivatives, were also tested. The structure-activity relationships of the epolactaene derivatives as an inducer of apoptosis are described. The alpha-acyl-alpha,beta-epoxy-gamma-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 IC50 value of 0.70 microM.
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