PMID- 13129585
OWN - NLM
STAT- MEDLINE
DCOM- 20040601
LR  - 20190901
IS  - 0968-0896 (Print)
IS  - 0968-0896 (Linking)
VI  - 11
IP  - 20
DP  - 2003 Oct 1
TI  - Design, synthesis, and biological evaluation of simplified alpha-keto 
      heterocycle, trifluoromethyl ketone, and formyl substituted folate analogues as 
      potential inhibitors of GAR transformylase and AICAR transformylase.
PG  - 4487-501
AB  - A series of simplified alpha-keto heterocycle, trifluoromethyl ketone, and formyl 
      substituted folate analogues lacking the benzoylglutamate subunit were prepared 
      and examined as potential inhibitors of glycinamide ribonucleotide transformylase 
      (GAR Tfase) and aminoimidazole carboxamide transformylase (AICAR Tfase).
FAU - Marsilje, Thomas H
AU  - Marsilje TH
AD  - Department of Chemistry, The Scripps Research Institute, 10550 North Torrey Pines 
      Road, La Jolla, CA 92037, USA.
FAU - Hedrick, Michael P
AU  - Hedrick MP
FAU - Desharnais, Joel
AU  - Desharnais J
FAU - Tavassoli, Ali
AU  - Tavassoli A
FAU - Zhang, Yan
AU  - Zhang Y
FAU - Wilson, Ian A
AU  - Wilson IA
FAU - Benkovic, Stephen J
AU  - Benkovic SJ
FAU - Boger, Dale L
AU  - Boger DL
LA  - eng
GR  - CA 63536/CA/NCI NIH HHS/United States
PT  - Journal Article
PT  - Research Support, Non-U.S. Gov't
PT  - Research Support, U.S. Gov't, P.H.S.
PL  - England
TA  - Bioorg Med Chem
JT  - Bioorganic & medicinal chemistry
JID - 9413298
RN  - 0 (Enzyme Inhibitors)
RN  - 0 (Ketones)
RN  - 935E97BOY8 (Folic Acid)
RN  - EC 2.1.2.- (Hydroxymethyl and Formyl Transferases)
RN  - EC 2.1.2.2 (Phosphoribosylglycinamide Formyltransferase)
RN  - EC 2.1.2.3 (Phosphoribosylaminoimidazolecarboxamide Formyltransferase)
SB  - IM
MH  - Cell Line, Tumor
MH  - Cell Survival/drug effects
MH  - Drug Design
MH  - Enzyme Inhibitors/chemical synthesis/pharmacology
MH  - Folic Acid/*analogs & derivatives/chemical synthesis/pharmacology
MH  - Humans
MH  - Hydroxymethyl and Formyl Transferases/*antagonists & inhibitors
MH  - Inhibitory Concentration 50
MH  - Ketones
MH  - Phosphoribosylaminoimidazolecarboxamide Formyltransferase
MH  - Phosphoribosylglycinamide Formyltransferase
MH  - Structure-Activity Relationship
EDAT- 2003/09/18 05:00
MHDA- 2004/06/02 05:00
CRDT- 2003/09/18 05:00
PHST- 2003/09/18 05:00 [pubmed]
PHST- 2004/06/02 05:00 [medline]
PHST- 2003/09/18 05:00 [entrez]
AID - S0968089603004565 [pii]
AID - 10.1016/s0968-0896(03)00456-5 [doi]
PST - ppublish
SO  - Bioorg Med Chem. 2003 Oct 1;11(20):4487-501. doi: 10.1016/s0968-0896(03)00456-5.