Discovery of a novel class of 2-ureido thiophene carboxamide checkpoint kinase inhibitors

James W. Janetka; Lynsie Almeida; Susan Ashwell; Patrick J. Brassil; Kevin Daly; Chun Deng; Thomas Gero; Roberta E. Glynn; Candice L. Horn; Stephanos Ioannidis; Paul Lyne; Nicholas J. Newcombe; Vibha B. Oza; Martin Pass; Stephanie K. Springer; Mei Su; Dorin Toader; Melissa M. Vasbinder; Dingwei Yu; Yan Yu; Sonya D. Zabludoff

doi:10.1016/j.bmcl.2008.05.016

Discovery of a novel class of 2-ureido thiophene carboxamide checkpoint kinase inhibitors

James W. Janetka, Lynsie Almeida, Susan Ashwell, Patrick J. Brassil, Kevin Daly, Chun Deng, Thomas Gero, Roberta E. Glynn, Candice L. Horn, Stephanos Ioannidis, Paul Lyne, Nicholas J. Newcombe, Vibha B. Oza, Martin Pass, Stephanie K. Springer, Mei Su, Dorin Toader, Melissa M. Vasbinder, Dingwei Yu, Yan YuSonya D. Zabludoff

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

35 Scopus citations

Abstract

Checkpoint kinase-1 (Chk1, CHEK1) is a Ser/Thr protein kinase that mediates the cellular response to DNA-damage. A novel class of 2-ureido thiophene carboxamide urea (TCU) Chk1 inhibitors is described. Inhibitors in this chemotype were optimized for cellular potency and selectivity over Cdk1.

Original language	English
Pages (from-to)	4242-4248
Number of pages	7
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	18
Issue number	14
DOIs	https://doi.org/10.1016/j.bmcl.2008.05.016
State	Published - Jul 15 2008

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Janetka, J. W., Almeida, L., Ashwell, S., Brassil, P. J., Daly, K., Deng, C., Gero, T., Glynn, R. E., Horn, C. L., Ioannidis, S., Lyne, P., Newcombe, N. J., Oza, V. B., Pass, M., Springer, S. K., Su, M., Toader, D., Vasbinder, M. M., Yu, D., ... Zabludoff, S. D. (2008). Discovery of a novel class of 2-ureido thiophene carboxamide checkpoint kinase inhibitors. Bioorganic and Medicinal Chemistry Letters, 18(14), 4242-4248. https://doi.org/10.1016/j.bmcl.2008.05.016

@article{1804598b2b7249349aaba9a0d89ef87c,

title = "Discovery of a novel class of 2-ureido thiophene carboxamide checkpoint kinase inhibitors",

abstract = "Checkpoint kinase-1 (Chk1, CHEK1) is a Ser/Thr protein kinase that mediates the cellular response to DNA-damage. A novel class of 2-ureido thiophene carboxamide urea (TCU) Chk1 inhibitors is described. Inhibitors in this chemotype were optimized for cellular potency and selectivity over Cdk1.",

author = "Janetka, {James W.} and Lynsie Almeida and Susan Ashwell and Brassil, {Patrick J.} and Kevin Daly and Chun Deng and Thomas Gero and Glynn, {Roberta E.} and Horn, {Candice L.} and Stephanos Ioannidis and Paul Lyne and Newcombe, {Nicholas J.} and Oza, {Vibha B.} and Martin Pass and Springer, {Stephanie K.} and Mei Su and Dorin Toader and Vasbinder, {Melissa M.} and Dingwei Yu and Yan Yu and Zabludoff, {Sonya D.}",

year = "2008",

month = jul,

day = "15",

doi = "10.1016/j.bmcl.2008.05.016",

language = "English",

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Janetka, JW, Almeida, L, Ashwell, S, Brassil, PJ, Daly, K, Deng, C, Gero, T, Glynn, RE, Horn, CL, Ioannidis, S, Lyne, P, Newcombe, NJ, Oza, VB, Pass, M, Springer, SK, Su, M, Toader, D, Vasbinder, MM, Yu, D, Yu, Y & Zabludoff, SD 2008, 'Discovery of a novel class of 2-ureido thiophene carboxamide checkpoint kinase inhibitors', Bioorganic and Medicinal Chemistry Letters, vol. 18, no. 14, pp. 4242-4248. https://doi.org/10.1016/j.bmcl.2008.05.016

TY - JOUR

T1 - Discovery of a novel class of 2-ureido thiophene carboxamide checkpoint kinase inhibitors

AU - Janetka, James W.

AU - Almeida, Lynsie

AU - Ashwell, Susan

AU - Brassil, Patrick J.

AU - Daly, Kevin

AU - Deng, Chun

AU - Gero, Thomas

AU - Glynn, Roberta E.

AU - Horn, Candice L.

AU - Ioannidis, Stephanos

AU - Lyne, Paul

AU - Newcombe, Nicholas J.

AU - Oza, Vibha B.

AU - Pass, Martin

AU - Springer, Stephanie K.

AU - Su, Mei

AU - Toader, Dorin

AU - Vasbinder, Melissa M.

AU - Yu, Dingwei

AU - Yu, Yan

AU - Zabludoff, Sonya D.

PY - 2008/7/15

Y1 - 2008/7/15

N2 - Checkpoint kinase-1 (Chk1, CHEK1) is a Ser/Thr protein kinase that mediates the cellular response to DNA-damage. A novel class of 2-ureido thiophene carboxamide urea (TCU) Chk1 inhibitors is described. Inhibitors in this chemotype were optimized for cellular potency and selectivity over Cdk1.

AB - Checkpoint kinase-1 (Chk1, CHEK1) is a Ser/Thr protein kinase that mediates the cellular response to DNA-damage. A novel class of 2-ureido thiophene carboxamide urea (TCU) Chk1 inhibitors is described. Inhibitors in this chemotype were optimized for cellular potency and selectivity over Cdk1.

UR - http://www.scopus.com/inward/record.url?scp=47149091445&partnerID=8YFLogxK

U2 - 10.1016/j.bmcl.2008.05.016

DO - 10.1016/j.bmcl.2008.05.016

M3 - Article

C2 - 18547806

AN - SCOPUS:47149091445

SN - 0960-894X

VL - 18

SP - 4242

EP - 4248

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 14

ER -

Discovery of a novel class of 2-ureido thiophene carboxamide checkpoint kinase inhibitors

Abstract

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