Discovery of a novel class of triazolones as Checkpoint Kinase inhibitors - Hit to lead exploration

Vibha Oza; Susan Ashwell; Patrick Brassil; Jason Breed; Chun Deng; Jay Ezhuthachan; Heather Haye; Candice Horn; James Janetka; Paul Lyne; Nicholas Newcombe; Ludo Otterbien; Martin Pass; Jon Read; Sian Roswell; Mei Su; Dorin Toader; Dingwei Yu; Yan Yu; Anna Valentine; Peter Webborn; Ann White; Sonya Zabludoff; Xiaolan Zheng

doi:10.1016/j.bmcl.2010.07.015

Discovery of a novel class of triazolones as Checkpoint Kinase inhibitors - Hit to lead exploration

Vibha Oza
, Susan Ashwell
, Patrick Brassil
, Jason Breed
, Chun Deng
, Jay Ezhuthachan
, Heather Haye
, Candice Horn
, James Janetka
, Paul Lyne
, Nicholas Newcombe
, Ludo Otterbien
, Martin Pass
, Jon Read
, Sian Roswell
, Mei Su
, Dorin Toader
, Dingwei Yu
, Yan Yu
, Anna Valentine

Peter Webborn, Ann White, Sonya Zabludoff, Xiaolan Zheng

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

18 Scopus citations

Abstract

Checkpoint Kinase-1 (Chk1, CHK1, CHEK1) is a Ser/Thr protein kinase that mediates cellular responses to DNA-damage. A novel class of Chk1 inhibitors, triazoloquinolones/triazolones (TZ's) was identified by high throughput screening. The optimization of these hits to provide a lead series is described.

Original language	English
Pages (from-to)	5133-5138
Number of pages	6
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	20
Issue number	17
DOIs	https://doi.org/10.1016/j.bmcl.2010.07.015
State	Published - Sep 1 2010

Keywords

CHK1
Checkpoint Kinase inhibitors
Triazolones

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10.1016/j.bmcl.2010.07.015

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Oza, V., Ashwell, S., Brassil, P., Breed, J., Deng, C., Ezhuthachan, J., Haye, H., Horn, C., Janetka, J., Lyne, P., Newcombe, N., Otterbien, L., Pass, M., Read, J., Roswell, S., Su, M., Toader, D., Yu, D., Yu, Y., ... Zheng, X. (2010). Discovery of a novel class of triazolones as Checkpoint Kinase inhibitors - Hit to lead exploration. Bioorganic and Medicinal Chemistry Letters, 20(17), 5133-5138. https://doi.org/10.1016/j.bmcl.2010.07.015

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title = "Discovery of a novel class of triazolones as Checkpoint Kinase inhibitors - Hit to lead exploration",

abstract = "Checkpoint Kinase-1 (Chk1, CHK1, CHEK1) is a Ser/Thr protein kinase that mediates cellular responses to DNA-damage. A novel class of Chk1 inhibitors, triazoloquinolones/triazolones (TZ's) was identified by high throughput screening. The optimization of these hits to provide a lead series is described.",

keywords = "CHK1, Checkpoint Kinase inhibitors, Triazolones",

author = "Vibha Oza and Susan Ashwell and Patrick Brassil and Jason Breed and Chun Deng and Jay Ezhuthachan and Heather Haye and Candice Horn and James Janetka and Paul Lyne and Nicholas Newcombe and Ludo Otterbien and Martin Pass and Jon Read and Sian Roswell and Mei Su and Dorin Toader and Dingwei Yu and Yan Yu and Anna Valentine and Peter Webborn and Ann White and Sonya Zabludoff and Xiaolan Zheng",

year = "2010",

month = sep,

day = "1",

doi = "10.1016/j.bmcl.2010.07.015",

language = "English",

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journal = "Bioorganic and Medicinal Chemistry Letters",

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Oza, V, Ashwell, S, Brassil, P, Breed, J, Deng, C, Ezhuthachan, J, Haye, H, Horn, C, Janetka, J, Lyne, P, Newcombe, N, Otterbien, L, Pass, M, Read, J, Roswell, S, Su, M, Toader, D, Yu, D, Yu, Y, Valentine, A, Webborn, P, White, A, Zabludoff, S & Zheng, X 2010, 'Discovery of a novel class of triazolones as Checkpoint Kinase inhibitors - Hit to lead exploration', Bioorganic and Medicinal Chemistry Letters, vol. 20, no. 17, pp. 5133-5138. https://doi.org/10.1016/j.bmcl.2010.07.015

TY - JOUR

T1 - Discovery of a novel class of triazolones as Checkpoint Kinase inhibitors - Hit to lead exploration

AU - Oza, Vibha

AU - Ashwell, Susan

AU - Brassil, Patrick

AU - Breed, Jason

AU - Deng, Chun

AU - Ezhuthachan, Jay

AU - Haye, Heather

AU - Horn, Candice

AU - Janetka, James

AU - Lyne, Paul

AU - Newcombe, Nicholas

AU - Otterbien, Ludo

AU - Pass, Martin

AU - Read, Jon

AU - Roswell, Sian

AU - Su, Mei

AU - Toader, Dorin

AU - Yu, Dingwei

AU - Yu, Yan

AU - Valentine, Anna

AU - Webborn, Peter

AU - White, Ann

AU - Zabludoff, Sonya

AU - Zheng, Xiaolan

PY - 2010/9/1

Y1 - 2010/9/1

N2 - Checkpoint Kinase-1 (Chk1, CHK1, CHEK1) is a Ser/Thr protein kinase that mediates cellular responses to DNA-damage. A novel class of Chk1 inhibitors, triazoloquinolones/triazolones (TZ's) was identified by high throughput screening. The optimization of these hits to provide a lead series is described.

AB - Checkpoint Kinase-1 (Chk1, CHK1, CHEK1) is a Ser/Thr protein kinase that mediates cellular responses to DNA-damage. A novel class of Chk1 inhibitors, triazoloquinolones/triazolones (TZ's) was identified by high throughput screening. The optimization of these hits to provide a lead series is described.

KW - CHK1

KW - Checkpoint Kinase inhibitors

KW - Triazolones

UR - https://www.scopus.com/pages/publications/77955653997

U2 - 10.1016/j.bmcl.2010.07.015

DO - 10.1016/j.bmcl.2010.07.015

M3 - Article

C2 - 20673630

AN - SCOPUS:77955653997

SN - 0960-894X

VL - 20

SP - 5133

EP - 5138

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 17

ER -

Discovery of a novel class of triazolones as Checkpoint Kinase inhibitors - Hit to lead exploration

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