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

Kouji Kuramochi, Rie Matsui, Yasuaki Matsubara, Junko Nakai, Takashi Sunoki, Satoshi Arai, Seigo Nagata, Yukitoshi Nagahara, Yoshiyuki Mizushina, Masahiko Ikekita, Susumu Kobayashi

Frontier Research Center for Genome and Drug Discovery, Tokyo University of Science, 2641 Yamazaki, Noda, Chiba 278-8510, Japan.

Bioorganic & medicinal chemistry 2006 Apr 1

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Epolactaene, a neuritogenic compound in human neuroblastoma SH-SY5Y, induces apoptosis in a human leukemia B-ce ll 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.

Citation

Kouji Kuramochi, Rie Matsui, Yasuaki Matsubara, Junko Nakai, Takashi Sunoki, Satoshi Arai, Seigo Nagata, Yukitoshi Nagahara, Yoshiyuki Mizushina, Masahiko Ikekita, Susumu Kobayashi. Apoptosis-inducing effect of epolactaene derivatives on BALL-1 cells. Bioorganic & medicinal chemistry. 2006 Apr 1;14(7):2151-61