Syntheses and antiproliferative evaluation of oxyphenisatin derivatives.
Syntheses and structure-antiproliferative relationship for oxyphenisatin analogues are described. The cell proliferation data showed that the presence of substituents (especially F, Cl, Me, CF(3), and OMe) in the 6- and 7-position of oxyphenisatin markedly enhanced the potency in the MDA-468 cell line without affecting the MDA-231 cell line. The best compounds from this series showed low nanomolar antiproliferative activity towards the MDA-468 cell line and a 1000-fold selectivity over the MDA-231 cell line.
Uddin
Muhammed K
MK
Evotec(UK) Ltd, 111 Milton Park, Abingdon, Oxon OX14 4RX, UK.
Reignier
Serge G
SG
Coulter
Tom
T
Montalbetti
Christian
C
Grånäs
Charlotta
C
Butcher
Steven
S
Krog-Jensen
Christian
C
Felding
Jakob
J
D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D049109:Cell Proliferation / Q000187:drug effects*; D006801:Humans; D015394:Molecular Structure; D010114:Oxyphenisatin Acetate / Q000031:analogs & derivatives* / Q000138:chemical synthesis* / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D014407:Tumor Cells, Cultured
D000970:Antineoplastic Agents; C560641:Top001 compound; C560642:Top216 compound; D010114:Oxyphenisatin Acetate