PMID- 3599031
OWN - NLM
STAT- MEDLINE
DCOM- 19870807
LR  - 20190709
IS  - 0022-2623 (Print)
IS  - 0022-2623 (Linking)
VI  - 30
IP  - 7
DP  - 1987 Jul
TI  - N10-substituted 5,8-dideazafolate inhibitors of glycinamide ribonucleotide 
      transformylase.
PG  - 1254-6
AB  - A series of 5,8-dideazafolates bearing ethyl, isopropyl, cyclopropylmethyl, 
      propargyl, 3-cyanopropyl, carboxymethyl, 2-carboxyethyl, phenacyl, 
      3-fluorobenzyl, and 5-uracilylmethyl substituents at N10 were tested as 
      inhibitors of purified L5178Y glycinamide ribonucleotide transformylase (GAR 
      TFase), which requires 10-formyltetrahydrofolate as cofactor. All of these 
      cofactor analogues exhibited competitive inhibition against 
      N10-formyl-5,8-dideazafolate, with Ki's ranging from 2 to 32 microM.
FAU - Caperelli, C A
AU  - Caperelli CA
LA  - eng
GR  - CA43531/CA/NCI NIH HHS/United States
PT  - Journal Article
PT  - Research Support, U.S. Gov't, P.H.S.
PL  - United States
TA  - J Med Chem
JT  - Journal of medicinal chemistry
JID - 9716531
RN  - 935E97BOY8 (Folic Acid)
RN  - EC 2.1.2.- (Hydroxymethyl and Formyl Transferases)
RN  - EC 2.1.2.2 (Phosphoribosylglycinamide Formyltransferase)
RN  - EC 2.3.- (Acyltransferases)
SB  - IM
MH  - Acyltransferases/*antagonists & inhibitors
MH  - Folic Acid/*analogs & derivatives
MH  - *Hydroxymethyl and Formyl Transferases
MH  - Phosphoribosylglycinamide Formyltransferase
MH  - Structure-Activity Relationship
EDAT- 1987/07/01 00:00
MHDA- 1987/07/01 00:01
CRDT- 1987/07/01 00:00
PHST- 1987/07/01 00:00 [pubmed]
PHST- 1987/07/01 00:01 [medline]
PHST- 1987/07/01 00:00 [entrez]
AID - 10.1021/jm00390a024 [doi]
PST - ppublish
SO  - J Med Chem. 1987 Jul;30(7):1254-6. doi: 10.1021/jm00390a024.