The identification and optimization of 2,4-diketobutyric acids as flap endonuclease 1 inhibitors

L. Nathan Tumey; Bayard Huck; Elizabeth Gleason; Jianmin Wang; Daniel Silver; Kurt Brunden; Sherry Boozer; Stephen Rundlett; Bruce Sherf; Steven Murphy; Andrew Bailey; Tom Dent; Christina Leventhal; John Harrington; Youssef L. Bennani

doi:10.1016/j.bmcl.2004.07.028

The identification and optimization of 2,4-diketobutyric acids as flap endonuclease 1 inhibitors

L. Nathan Tumey
, Bayard Huck
, Elizabeth Gleason
, Jianmin Wang
, Daniel Silver
, Kurt Brunden
, Sherry Boozer
, Stephen Rundlett
, Bruce Sherf
, Steven Murphy
, Andrew Bailey
, Tom Dent
, Christina Leventhal
, John Harrington
, Youssef L. Bennani

Pharmaceutical Sciences

Binghamton University

Athersys Ltd

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

24 Scopus citations

Abstract

Flap endonuclease 1 (FEN1) is a key enzyme involved in base excision repair (BER), a primary pathway utilized by mammalian cells to repair DNA damage. In this report, we describe the identification and SAR of a series of 2,4-diketobutyric acid FEN1 inhibitors that may be useful as chemopotentiators. There have been several recent reports of chemopotentiation via inhibition of DNA repair processes. Flap endonuclease 1 (FEN1) is a key enzyme involved in base excision repair (BER), a primary pathway utilized by mammalian cells to repair DNA damage. In this report, we describe the identification and SAR of a series of 2,4-diketobutyric acid FEN1 inhibitors.

Original language	English
Pages (from-to)	4915-4918
Number of pages	4
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	14
Issue number	19
DOIs	https://doi.org/10.1016/j.bmcl.2004.07.028
State	Published - Oct 4 2004

Keywords

Cancer
Endonuclease
FEN1

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10.1016/j.bmcl.2004.07.028

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Tumey, L. N., Huck, B., Gleason, E., Wang, J., Silver, D., Brunden, K., Boozer, S., Rundlett, S., Sherf, B., Murphy, S., Bailey, A., Dent, T., Leventhal, C., Harrington, J., & Bennani, Y. L. (2004). The identification and optimization of 2,4-diketobutyric acids as flap endonuclease 1 inhibitors. Bioorganic and Medicinal Chemistry Letters, 14(19), 4915-4918. https://doi.org/10.1016/j.bmcl.2004.07.028

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title = "The identification and optimization of 2,4-diketobutyric acids as flap endonuclease 1 inhibitors",

abstract = "Flap endonuclease 1 (FEN1) is a key enzyme involved in base excision repair (BER), a primary pathway utilized by mammalian cells to repair DNA damage. In this report, we describe the identification and SAR of a series of 2,4-diketobutyric acid FEN1 inhibitors that may be useful as chemopotentiators. There have been several recent reports of chemopotentiation via inhibition of DNA repair processes. Flap endonuclease 1 (FEN1) is a key enzyme involved in base excision repair (BER), a primary pathway utilized by mammalian cells to repair DNA damage. In this report, we describe the identification and SAR of a series of 2,4-diketobutyric acid FEN1 inhibitors.",

keywords = "Cancer, Endonuclease, FEN1",

author = "Tumey, \{L. Nathan\} and Bayard Huck and Elizabeth Gleason and Jianmin Wang and Daniel Silver and Kurt Brunden and Sherry Boozer and Stephen Rundlett and Bruce Sherf and Steven Murphy and Andrew Bailey and Tom Dent and Christina Leventhal and John Harrington and Bennani, \{Youssef L.\}",

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Tumey, LN, Huck, B, Gleason, E, Wang, J, Silver, D, Brunden, K, Boozer, S, Rundlett, S, Sherf, B, Murphy, S, Bailey, A, Dent, T, Leventhal, C, Harrington, J & Bennani, YL 2004, 'The identification and optimization of 2,4-diketobutyric acids as flap endonuclease 1 inhibitors', Bioorganic and Medicinal Chemistry Letters, vol. 14, no. 19, pp. 4915-4918. https://doi.org/10.1016/j.bmcl.2004.07.028

TY - JOUR

T1 - The identification and optimization of 2,4-diketobutyric acids as flap endonuclease 1 inhibitors

AU - Tumey, L. Nathan

AU - Huck, Bayard

AU - Gleason, Elizabeth

AU - Wang, Jianmin

AU - Silver, Daniel

AU - Brunden, Kurt

AU - Boozer, Sherry

AU - Rundlett, Stephen

AU - Sherf, Bruce

AU - Murphy, Steven

AU - Bailey, Andrew

AU - Dent, Tom

AU - Leventhal, Christina

AU - Harrington, John

AU - Bennani, Youssef L.

PY - 2004/10/4

Y1 - 2004/10/4

N2 - Flap endonuclease 1 (FEN1) is a key enzyme involved in base excision repair (BER), a primary pathway utilized by mammalian cells to repair DNA damage. In this report, we describe the identification and SAR of a series of 2,4-diketobutyric acid FEN1 inhibitors that may be useful as chemopotentiators. There have been several recent reports of chemopotentiation via inhibition of DNA repair processes. Flap endonuclease 1 (FEN1) is a key enzyme involved in base excision repair (BER), a primary pathway utilized by mammalian cells to repair DNA damage. In this report, we describe the identification and SAR of a series of 2,4-diketobutyric acid FEN1 inhibitors.

AB - Flap endonuclease 1 (FEN1) is a key enzyme involved in base excision repair (BER), a primary pathway utilized by mammalian cells to repair DNA damage. In this report, we describe the identification and SAR of a series of 2,4-diketobutyric acid FEN1 inhibitors that may be useful as chemopotentiators. There have been several recent reports of chemopotentiation via inhibition of DNA repair processes. Flap endonuclease 1 (FEN1) is a key enzyme involved in base excision repair (BER), a primary pathway utilized by mammalian cells to repair DNA damage. In this report, we describe the identification and SAR of a series of 2,4-diketobutyric acid FEN1 inhibitors.

KW - Cancer

KW - Endonuclease

KW - FEN1

UR - https://www.scopus.com/pages/publications/4444279071

U2 - 10.1016/j.bmcl.2004.07.028

DO - 10.1016/j.bmcl.2004.07.028

M3 - Article

C2 - 15341951

SN - 0960-894X

VL - 14

SP - 4915

EP - 4918

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 19

ER -

The identification and optimization of 2,4-diketobutyric acids as flap endonuclease 1 inhibitors

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Keywords

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