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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 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.

journal_name

Bioorg Med Chem

journal_title

Bioorganic & medicinal chemistry

authors

Kuramochi K,Matsui R,Matsubara Y,Nakai J,Sunoki T,Arai S,Nagata S,Nagahara Y,Mizushina Y,Ikekita M,Kobayashi S

doi

10.1016/j.bmc.2005.10.057

subject

Has Abstract

pub_date

2006-04-01 00:00:00

pages

2151-61

issue

7

eissn

0968-0896

issn

1464-3391

pii

S0968-0896(05)01055-2

journal_volume

14

pub_type

杂志文章

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