Effects of alpha-substitutions on structure and biological activity of anticancer chalcones.
Chalcones are known to exhibit antimitotic properties caused by inhibition of tubulin polymerisation. We describe here the effects of different alpha-substitutions, in particular alpha-fluorination, on the structure and biological activity of a series of chalcones.
Lawrence
Nicholas J
NJ
Drug Discovery Program, H. Lee Moffitt Cancer Center and Research Institute, Department of Interdisciplinary Oncology, University of South Florida, Tampa, FL 33612-9497, USA. Lawrennj@moffitt.usf.edu
Patterson
Richard P
RP
Ooi
Li-Ling
LL
Cook
Darren
D
Ducki
Sylvie
S
D050256:Antimitotic Agents / Q000138:chemical synthesis / Q000494:pharmacology*; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000494:pharmacology*; D002599:Chalcone / Q000031:analogs & derivatives / Q000138:chemical synthesis / Q000494:pharmacology*; D006801:Humans; D020014:K562 Cells; D013329:Structure-Activity Relationship; D014404:Tubulin / Q000378:metabolism*; D014407:Tumor Cells, Cultured / Q000187:drug effects*
D050256:Antimitotic Agents; D000970:Antineoplastic Agents; D014404:Tubulin; D002599:Chalcone