PMID- 11814858
OWN - NLM
STAT- MEDLINE
DCOM- 20030501
LR  - 20190901
IS  - 0968-0896 (Print)
IS  - 0968-0896 (Linking)
VI  - 10
IP  - 3
DP  - 2002 Mar
TI  - Synthesis and biological activities of fluorinated chalcone derivatives.
PG  - 699-706
AB  - We have designed and synthesized new 5-lipoxygenase inhibitors, fluorinated 
      3,4-dihydroxychalcones, and evaluated their biological activities with respect to 
      antiperoxidation activity and in vitro antitumor activities. All fluorinated 
      chalcones tested showed 5-lipoxygenase inhibition on rat basophilic leukemia-1 
      (RBL-1) cells and inhibitory action on Fe(3+)-ADP induced NADPH-dependent lipid 
      peroxidation in rat liver microsomes. The potencies were comparable or better to 
      that of the lead 3,4-dihydroxychalcone. 6-Fluoro-3,4-dihydroxy-2',4'-dimethoxy 
      chalcone (7) was the most effective compound in the in vitro assay using a human 
      cancer cell line panel (HCC panel) consisting of 39 systems.
FAU - Nakamura, Chika
AU  - Nakamura C
AD  - Faculty of Pharmaceutical Sciences, Tokushima Bunri University, Tokushima 
      770-8514, Japan.
FAU - Kawasaki, Nobuhide
AU  - Kawasaki N
FAU - Miyataka, Hideki
AU  - Miyataka H
FAU - Jayachandran, Ezhuthachan
AU  - Jayachandran E
FAU - Kim, In Ho
AU  - Kim IH
FAU - Kirk, Kenneth L
AU  - Kirk KL
FAU - Taguchi, Takeo
AU  - Taguchi T
FAU - Takeuchi, Yoshio
AU  - Takeuchi Y
FAU - Hori, Hitoshi
AU  - Hori H
FAU - Satoh, Toshio
AU  - Satoh T
LA  - eng
PT  - Journal Article
PT  - Research Support, Non-U.S. Gov't
PL  - England
TA  - Bioorg Med Chem
JT  - Bioorganic & medicinal chemistry
JID - 9413298
RN  - 0 (Antineoplastic Agents)
RN  - 0 (Enzyme Inhibitors)
RN  - 0 (Hydrocarbons, Fluorinated)
RN  - 0 (Lipoxygenase Inhibitors)
RN  - 5S5A2Q39HX (Chalcone)
SB  - IM
MH  - Animals
MH  - Antineoplastic Agents/*chemical synthesis/pharmacology
MH  - Cell Division/drug effects
MH  - Chalcone/*analogs & derivatives/chemical synthesis/pharmacology
MH  - Drug Design
MH  - Drug Screening Assays, Antitumor
MH  - Enzyme Inhibitors/chemical synthesis/pharmacology
MH  - Humans
MH  - Hydrocarbons, Fluorinated/chemical synthesis/pharmacology
MH  - Inhibitory Concentration 50
MH  - Lipid Peroxidation/drug effects
MH  - *Lipoxygenase Inhibitors
MH  - Male
MH  - Microsomes, Liver/enzymology
MH  - Organ Specificity
MH  - Rats
MH  - Rats, Wistar
MH  - Tumor Cells, Cultured
EDAT- 2002/01/30 10:00
MHDA- 2003/05/02 05:00
CRDT- 2002/01/30 10:00
PHST- 2002/01/30 10:00 [pubmed]
PHST- 2003/05/02 05:00 [medline]
PHST- 2002/01/30 10:00 [entrez]
AID - S0968089601003194 [pii]
AID - 10.1016/s0968-0896(01)00319-4 [doi]
PST - ppublish
SO  - Bioorg Med Chem. 2002 Mar;10(3):699-706. doi: 10.1016/s0968-0896(01)00319-4.