| RRC ID |
42492
|
| Author |
Kuramochi K, Matsui R, Matsubara Y, Nakai J, Sunoki T, Arai S, Nagata S, Nagahara Y, Mizushina Y, Ikekita M, Kobayashi S.
|
| Title |
Apoptosis-inducing effect of epolactaene derivatives on BALL-1 cells.
|
| Journal |
Bioorg Med Chem
|
| 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.
|
| Volume |
14(7)
|
| Pages |
2151-61
|
| Published |
2006-4-1
|
| DOI |
10.1016/j.bmc.2005.10.057
|
| PII |
S0968-0896(05)01055-2
|
| PMID |
16298530
|
| MeSH |
Apoptosis / drug effects*
Cell Line, Tumor
Cell Survival / drug effects
Drug Screening Assays, Antitumor
Epoxy Compounds / chemical synthesis
Epoxy Compounds / chemistry
Epoxy Compounds / pharmacology
Humans
Hydrolysis
Leukemia, B-Cell / drug therapy*
Molecular Structure
Polyenes / chemical synthesis
Polyenes / chemistry
Polyenes / pharmacology
Stereoisomerism
Structure-Activity Relationship
|
| IF |
3.073
|
| Times Cited |
22
|
|
WOS Category
|
CHEMISTRY, ORGANIC
CHEMISTRY, MEDICINAL
BIOCHEMISTRY & MOLECULAR BIOLOGY
|
| Resource |
| Human and Animal Cells |
BALL-1 |
