Synthesis and cell growth inhibitory properties of substituted ( E)-1-phenylbut-1-en-3-ones

A series of ( E)-1-phenylbut-1-en-3-ones, based on the naturally occurring ( E)-1-(4′-hydroxyphenyl)but-1-en-3-one [IC 50 (K562) 60 μM], was synthesised and screened for cytotoxic activity against the K562 human leukaemia cell line. ( E)-1-(Pentafluorophenyl)but-1-en-3-one [IC 50 (K562) 1.8 μM] was...

Full description

Saved in:
Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 1997-12, Vol.7 (24), p.3091-3094
Main Authors: Ducki, Sylvie, Hadfield, John A., Hepworth, Lucy A., Lawrence, Nicholas J., Liu, Ching-Ying, McGown, Alan T.
Format: Article
Language:English
Subjects:
Antineoplastic agents
Biological and medical sciences
General aspects
Medical sciences
Pharmacology. Drug treatments
Citations: Items that this one cites
Items that cite this one
Online Access:Get full text
Tags: Add Tag
No Tags, Be the first to tag this record!
Description
Summary:A series of ( E)-1-phenylbut-1-en-3-ones, based on the naturally occurring ( E)-1-(4′-hydroxyphenyl)but-1-en-3-one [IC 50 (K562) 60 μM], was synthesised and screened for cytotoxic activity against the K562 human leukaemia cell line. ( E)-1-(Pentafluorophenyl)but-1-en-3-one [IC 50 (K562) 1.8 μM] was found to be over 30-fold more active than 1. A series of E-1-phenylbut-1-en-3-ones, based on the naturally occurring E-1-(4′-hydroxyphenyl)but-1-en-3-one 1 [IC 50 (K562) 60 μM], was synthesised and screened for cell growth inhibition. E-1-(pentafluorophenyl)but-1-en-3-one 4a [IC 50 (K562) 1.8 μM] was found to be over 30-fold more active than 1.
ISSN:0960-894X
1464-3405
DOI:10.1016/S0960-894X(97)10147-0