Kuramochi Kouji, Matsui Rie, Matsubara Yasuaki, Nakai Junko, Sunoki Takashi, Arai Satoshi, Nagata Seigo, Nagahara Yukitoshi, Mizushina Yoshiyuki, Ikekita Masahiko, Kobayashi Susumu
Frontier Research Center for Genome and Drug Discovery, Tokyo University of Science, 2641 Yamazaki, Noda, Chiba 278-8510, Japan.
Bioorg Med Chem. 2006 Apr 1;14(7):2151-61. doi: 10.1016/j.bmc.2005.10.057. Epub 2005 Nov 18.
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.
埃波拉他汀，一种人神经母细胞瘤SH-SY5Y中的促神经突生长化合物，可诱导人白血病B细胞系BALL-1凋亡。还测试了34种埃波拉他汀衍生物的凋亡诱导活性，包括新合成的α-烷基-α,β-环氧-γ-内酰胺衍生物和环丙烷衍生物。描述了埃波拉他汀衍生物作为凋亡诱导剂的构效关系。α-酰基-α,β-环氧-γ-内酰胺部分以及长烷基侧链产生的疏水性对活性都很重要。化合物1e在所有合成化合物中表现出最强的活性，IC50值为0.70微摩尔。
