Conformationally restricted analogues designed for selective inhibition of GAR Tfase versus thymidylate synthase or dihydrofolate reductase

Dale L. Boger; Marc A. Labroli; Thomas H. Marsilje; Qing Jin; Michael P. Hedrick; Stephen J. Baker; Jae Hoon Shim; Stephen J. Benkovic

doi:10.1016/S0968-0896(00)00051-1

Conformationally restricted analogues designed for selective inhibition of GAR Tfase versus thymidylate synthase or dihydrofolate reductase

Dale L. Boger, Marc A. Labroli, Thomas H. Marsilje, Qing Jin, Michael P. Hedrick, Stephen J. Baker, Jae Hoon Shim, Stephen J. Benkovic

Research output: Contribution to journal › Article › peer-review

17 Scopus citations

Abstract

The synthesis and evaluation of a series of conformationally restricted analogues of 10-formyl-tetrahydrofolate as potential inhibitors of glycinamide ribonucleotide transformylase (GAR Tfase) or aminoimidazole carboxamide transformylase (AICAR Tfase) are reported. (C) 2000 Elsevier Science Ltd.

Original language	English (US)
Pages (from-to)	1075-1086
Number of pages	12
Journal	Bioorganic and Medicinal Chemistry
Volume	8
Issue number	5
DOIs	https://doi.org/10.1016/S0968-0896(00)00051-1
State	Published - May 2000

All Science Journal Classification (ASJC) codes

Biochemistry
Molecular Medicine
Molecular Biology
Pharmaceutical Science
Drug Discovery
Clinical Biochemistry
Organic Chemistry

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@article{76288d356deb41e8832c1bdaa66bbb97,

title = "Conformationally restricted analogues designed for selective inhibition of GAR Tfase versus thymidylate synthase or dihydrofolate reductase",

abstract = "The synthesis and evaluation of a series of conformationally restricted analogues of 10-formyl-tetrahydrofolate as potential inhibitors of glycinamide ribonucleotide transformylase (GAR Tfase) or aminoimidazole carboxamide transformylase (AICAR Tfase) are reported. (C) 2000 Elsevier Science Ltd.",

author = "Boger, {Dale L.} and Labroli, {Marc A.} and Marsilje, {Thomas H.} and Qing Jin and Hedrick, {Michael P.} and Baker, {Stephen J.} and Shim, {Jae Hoon} and Benkovic, {Stephen J.}",

note = "Funding Information: We gratefully acknowledge the financial support of the National Institutes of Health (CA 63536) and the Skaggs Institute for Chemical Biology.",

year = "2000",

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journal = "Bioorganic and Medicinal Chemistry",

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Conformationally restricted analogues designed for selective inhibition of GAR Tfase versus thymidylate synthase or dihydrofolate reductase. / Boger, Dale L.; Labroli, Marc A.; Marsilje, Thomas H.; Jin, Qing; Hedrick, Michael P.; Baker, Stephen J.; Shim, Jae Hoon; Benkovic, Stephen J.

In: Bioorganic and Medicinal Chemistry, Vol. 8, No. 5, 05.2000, p. 1075-1086.

Research output: Contribution to journal › Article › peer-review

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AU - Boger, Dale L.

AU - Labroli, Marc A.

AU - Marsilje, Thomas H.

AU - Jin, Qing

AU - Hedrick, Michael P.

AU - Baker, Stephen J.

AU - Shim, Jae Hoon

AU - Benkovic, Stephen J.

N1 - Funding Information: We gratefully acknowledge the financial support of the National Institutes of Health (CA 63536) and the Skaggs Institute for Chemical Biology.

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