5-Fluorocytosine derivatives as inhibitors of deoxycytidine kinase

James E. Tarver; Theodore C. Jessop; Marianne Carlsen; David J. Augeri; Qinghong Fu; Jason P. Healy; Alexander Heim-Riether; Amy Xu; Jerry A. Taylor; Min Shen; Philip E. Keyes; S. David Kimball; Xuan Chuan Yu; Maricar Miranda; Qingyun Liu; Jonathan C. Swaffield; Amr Nouraldeen; Alan G.E. Wilson; Rick Finch; Kanchan Jhaver; Ann Marie Di George Foushee; Steve Anderson; Tamas Oravecz; Kenneth G. Carson

doi:10.1016/j.bmcl.2009.09.082

5-Fluorocytosine derivatives as inhibitors of deoxycytidine kinase

James E. Tarver, Theodore C. Jessop, Marianne Carlsen, David J. Augeri, Qinghong Fu, Jason P. Healy, Alexander Heim-Riether, Amy Xu, Jerry A. Taylor, Min Shen, Philip E. Keyes, S. David Kimball, Xuan Chuan Yu, Maricar Miranda, Qingyun Liu, Jonathan C. Swaffield, Amr Nouraldeen, Alan G.E. Wilson, Rick Finch, Kanchan JhaverAnn Marie Di George Foushee, Steve Anderson, Tamas Oravecz, Kenneth G. Carson

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

4 Scopus citations

Abstract

A series of potent piperidine-linked cytosine derivatives were prepared as inhibitors of deoxycytidine kinase (dCK). Compound 9h was discovered to be a potent inhibitor of dCK and shows a good combination of cellular potency and pharmacokinetic parameters. Compound 9h blocks the incorporation of radiolabeled cytosine into mouse T-cells in vitro, as well as in vivo in mice following a T-cell challenge.

Original language	English (US)
Pages (from-to)	6780-6783
Number of pages	4
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	19
Issue number	23
DOIs	https://doi.org/10.1016/j.bmcl.2009.09.082
State	Published - Dec 1 2009
Externally published	Yes

Keywords

Cancer
Deoxycytidine kinase
Immunology
Pharmacokinetics
Virology

ASJC Scopus subject areas

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

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10.1016/j.bmcl.2009.09.082

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Tarver, J. E., Jessop, T. C., Carlsen, M., Augeri, D. J., Fu, Q., Healy, J. P., Heim-Riether, A., Xu, A., Taylor, J. A., Shen, M., Keyes, P. E., David Kimball, S., Yu, X. C., Miranda, M., Liu, Q., Swaffield, J. C., Nouraldeen, A., Wilson, A. G. E., Finch, R., ... Carson, K. G. (2009). 5-Fluorocytosine derivatives as inhibitors of deoxycytidine kinase. Bioorganic and Medicinal Chemistry Letters, 19(23), 6780-6783. https://doi.org/10.1016/j.bmcl.2009.09.082

Tarver, JE, Jessop, TC, Carlsen, M, Augeri, DJ, Fu, Q, Healy, JP, Heim-Riether, A, Xu, A, Taylor, JA, Shen, M, Keyes, PE, David Kimball, S, Yu, XC, Miranda, M, Liu, Q, Swaffield, JC, Nouraldeen, A, Wilson, AGE, Finch, R, Jhaver, K, Foushee, AMDG, Anderson, S, Oravecz, T & Carson, KG 2009, '5-Fluorocytosine derivatives as inhibitors of deoxycytidine kinase', Bioorganic and Medicinal Chemistry Letters, vol. 19, no. 23, pp. 6780-6783. https://doi.org/10.1016/j.bmcl.2009.09.082

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title = "5-Fluorocytosine derivatives as inhibitors of deoxycytidine kinase",

abstract = "A series of potent piperidine-linked cytosine derivatives were prepared as inhibitors of deoxycytidine kinase (dCK). Compound 9h was discovered to be a potent inhibitor of dCK and shows a good combination of cellular potency and pharmacokinetic parameters. Compound 9h blocks the incorporation of radiolabeled cytosine into mouse T-cells in vitro, as well as in vivo in mice following a T-cell challenge.",

keywords = "Cancer, Deoxycytidine kinase, Immunology, Pharmacokinetics, Virology",

author = "Tarver, {James E.} and Jessop, {Theodore C.} and Marianne Carlsen and Augeri, {David J.} and Qinghong Fu and Healy, {Jason P.} and Alexander Heim-Riether and Amy Xu and Taylor, {Jerry A.} and Min Shen and Keyes, {Philip E.} and {David Kimball}, S. and Yu, {Xuan Chuan} and Maricar Miranda and Qingyun Liu and Swaffield, {Jonathan C.} and Amr Nouraldeen and Wilson, {Alan G.E.} and Rick Finch and Kanchan Jhaver and Foushee, {Ann Marie Di George} and Steve Anderson and Tamas Oravecz and Carson, {Kenneth G.}",

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doi = "10.1016/j.bmcl.2009.09.082",

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AU - Tarver, James E.

AU - Jessop, Theodore C.

AU - Carlsen, Marianne

AU - Augeri, David J.

AU - Fu, Qinghong

AU - Healy, Jason P.

AU - Heim-Riether, Alexander

AU - Xu, Amy

AU - Taylor, Jerry A.

AU - Shen, Min

AU - Keyes, Philip E.

AU - David Kimball, S.

AU - Yu, Xuan Chuan

AU - Miranda, Maricar

AU - Liu, Qingyun

AU - Swaffield, Jonathan C.

AU - Nouraldeen, Amr

AU - Wilson, Alan G.E.

AU - Finch, Rick

AU - Jhaver, Kanchan

AU - Foushee, Ann Marie Di George

AU - Anderson, Steve

AU - Oravecz, Tamas

AU - Carson, Kenneth G.

PY - 2009/12/1

Y1 - 2009/12/1

N2 - A series of potent piperidine-linked cytosine derivatives were prepared as inhibitors of deoxycytidine kinase (dCK). Compound 9h was discovered to be a potent inhibitor of dCK and shows a good combination of cellular potency and pharmacokinetic parameters. Compound 9h blocks the incorporation of radiolabeled cytosine into mouse T-cells in vitro, as well as in vivo in mice following a T-cell challenge.

AB - A series of potent piperidine-linked cytosine derivatives were prepared as inhibitors of deoxycytidine kinase (dCK). Compound 9h was discovered to be a potent inhibitor of dCK and shows a good combination of cellular potency and pharmacokinetic parameters. Compound 9h blocks the incorporation of radiolabeled cytosine into mouse T-cells in vitro, as well as in vivo in mice following a T-cell challenge.

KW - Cancer

KW - Deoxycytidine kinase

KW - Immunology

KW - Pharmacokinetics

KW - Virology

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AN - SCOPUS:71749114511

SN - 0960-894X

VL - 19

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EP - 6783

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 23

ER -

5-Fluorocytosine derivatives as inhibitors of deoxycytidine kinase

Abstract

Keywords

ASJC Scopus subject areas

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