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

Chemistry

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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10.1016/S0968-0896(00)00051-1

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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",

month = may,

doi = "10.1016/S0968-0896(00)00051-1",

language = "English (US)",

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journal = "Bioorganic and Medicinal Chemistry",

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T1 - Conformationally restricted analogues designed for selective inhibition of GAR Tfase versus thymidylate synthase or dihydrofolate reductase

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.

PY - 2000/5

Y1 - 2000/5

N2 - 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.

AB - 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.

UR - https://www.scopus.com/pages/publications/0034110646

UR - https://www.scopus.com/pages/publications/0034110646#tab=citedBy

U2 - 10.1016/S0968-0896(00)00051-1

DO - 10.1016/S0968-0896(00)00051-1

M3 - Article

C2 - 10882019

AN - SCOPUS:0034110646

SN - 0968-0896

VL - 8

SP - 1075

EP - 1086

JO - Bioorganic and Medicinal Chemistry

JF - Bioorganic and Medicinal Chemistry

IS - 5

ER -

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

Abstract

All Science Journal Classification (ASJC) codes

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