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
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
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).
cell line, tumor
cell survival/drug effects
drug design
enzyme inhibitors/chemical synthesis/pharmacology
folic acid, analogs & derivatives/chemical synthesis/pharmacology
humans
hydroxymethyl and formyl transferases, antagonists & inhibitors
inhibitory concentration 50
ketones
phosphoribosylaminoimidazolecarboxamide formyltransferase
phosphoribosylglycinamide formyltransferase
structure-activity relationship
4487-4501
Marsilje, Thomas H.
2d64bf3a-143b-4a00-8b9c-825beceb810e
Hedrick, Michael P.
ba690321-bfda-496d-98de-c3d383497035
Desharnais, Joel
f4d5b1db-e99b-4487-b37a-f64f24c7914a
Tavassoli, Ali
d561cf8f-2669-46b5-b6e1-2016c85d63b2
Zhang, Yan
8552a39d-0c4d-4712-8ad8-d0d5cc9d1779
Wilson, Ian A.
7865d500-d638-4a67-ad6d-fefad0ae83bb
Benkovic, Stephen J.
f85498a5-27fc-4a22-9069-ff61a4297520
Boger, Dale L.
d81e0270-0561-47df-8904-85718bd462ff
2003
Marsilje, Thomas H.
2d64bf3a-143b-4a00-8b9c-825beceb810e
Hedrick, Michael P.
ba690321-bfda-496d-98de-c3d383497035
Desharnais, Joel
f4d5b1db-e99b-4487-b37a-f64f24c7914a
Tavassoli, Ali
d561cf8f-2669-46b5-b6e1-2016c85d63b2
Zhang, Yan
8552a39d-0c4d-4712-8ad8-d0d5cc9d1779
Wilson, Ian A.
7865d500-d638-4a67-ad6d-fefad0ae83bb
Benkovic, Stephen J.
f85498a5-27fc-4a22-9069-ff61a4297520
Boger, Dale L.
d81e0270-0561-47df-8904-85718bd462ff
Marsilje, Thomas H., Hedrick, Michael P., Desharnais, Joel, Tavassoli, Ali, Zhang, Yan, Wilson, Ian A., Benkovic, Stephen J. and Boger, Dale L.
(2003)
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.
Bioorganic & Medicinal Chemistry, 11 (20), .
(doi:10.1016/S0968-0896(03)00456-5).
Abstract
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).
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More information
Published date: 2003
Keywords:
cell line, tumor
cell survival/drug effects
drug design
enzyme inhibitors/chemical synthesis/pharmacology
folic acid, analogs & derivatives/chemical synthesis/pharmacology
humans
hydroxymethyl and formyl transferases, antagonists & inhibitors
inhibitory concentration 50
ketones
phosphoribosylaminoimidazolecarboxamide formyltransferase
phosphoribosylglycinamide formyltransferase
structure-activity relationship
Identifiers
Local EPrints ID: 45311
URI: http://eprints.soton.ac.uk/id/eprint/45311
ISSN: 0968-0896
PURE UUID: 05e5c061-f258-47e4-a9d6-a31dd9985386
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Date deposited: 20 Mar 2007
Last modified: 16 Mar 2024 03:51
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Contributors
Author:
Thomas H. Marsilje
Author:
Michael P. Hedrick
Author:
Joel Desharnais
Author:
Yan Zhang
Author:
Ian A. Wilson
Author:
Stephen J. Benkovic
Author:
Dale L. Boger
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