Inhibitors of the tyrosine kinase EphB4: part 1: structure-based design and optimization of a series of 2,4-bis-anilinopyrimidines

Catherine Bardelle; Darren Cross; Sara Davenport; Jason G. Kettle; Eun Jung Ko; Andrew G. Leach; Andrew Mortlock; Jon Read; Nicola J. Roberts; Peter Robins; Emma J. Williams

doi:10.1016/j.bmcl.2008.04.015

Inhibitors of the tyrosine kinase EphB4: part 1: structure-based design and optimization of a series of 2,4-bis-anilinopyrimidines

Catherine Bardelle, Darren Cross, Sara Davenport, Jason G. Kettle, Eun Jung Ko, Andrew G. Leach, Andrew Mortlock, Jon Read, Nicola J. Roberts, Peter Robins, Emma J. Williams

Pharmacy

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

Abstract

A series of bis-anilinopyrimidines have been identified as potent inhibitors of the tyrosine kinase EphB4. Structural information from two alternative series identified from screening efforts was combined to identify the initial leads.5

Original language	English
Pages (from-to)	2776-2780
Number of pages	5
Journal	Bioorganic & medicinal chemistry letters
Volume	18
Issue number	9
DOIs	https://doi.org/10.1016/j.bmcl.2008.04.015
Publication status	Published - 1 May 2008

Keywords

kinase
EphB4
structure-based design
lead identification

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

Access to Document

10.1016/j.bmcl.2008.04.015

Cite this

Bardelle, C., Cross, D., Davenport, S., Kettle, J. G., Ko, E. J., Leach, A. G., Mortlock, A., Read, J., Roberts, N. J., Robins, P., & Williams, E. J. (2008). Inhibitors of the tyrosine kinase EphB4: part 1: structure-based design and optimization of a series of 2,4-bis-anilinopyrimidines. Bioorganic & medicinal chemistry letters, 18(9), 2776-2780. https://doi.org/10.1016/j.bmcl.2008.04.015

@article{3ea7b09d19ab46a3aecf8187a3a612d7,

title = "Inhibitors of the tyrosine kinase EphB4: part 1: structure-based design and optimization of a series of 2,4-bis-anilinopyrimidines",

abstract = "A series of bis-anilinopyrimidines have been identified as potent inhibitors of the tyrosine kinase EphB4. Structural information from two alternative series identified from screening efforts was combined to identify the initial leads.5",

keywords = "kinase, EphB4, structure-based design, lead identification",

author = "Catherine Bardelle and Darren Cross and Sara Davenport and Kettle, {Jason G.} and Ko, {Eun Jung} and Leach, {Andrew G.} and Andrew Mortlock and Jon Read and Roberts, {Nicola J.} and Peter Robins and Williams, {Emma J.}",

year = "2008",

month = may,

day = "1",

doi = "10.1016/j.bmcl.2008.04.015",

language = "English",

volume = "18",

pages = "2776--2780",

journal = "Bioorganic & medicinal chemistry letters",

issn = "0960-894X",

publisher = "Elsevier BV",

number = "9",

}

Bardelle, C, Cross, D, Davenport, S, Kettle, JG, Ko, EJ, Leach, AG, Mortlock, A, Read, J, Roberts, NJ, Robins, P & Williams, EJ 2008, 'Inhibitors of the tyrosine kinase EphB4: part 1: structure-based design and optimization of a series of 2,4-bis-anilinopyrimidines', Bioorganic & medicinal chemistry letters, vol. 18, no. 9, pp. 2776-2780. https://doi.org/10.1016/j.bmcl.2008.04.015

TY - JOUR

T1 - Inhibitors of the tyrosine kinase EphB4

T2 - part 1: structure-based design and optimization of a series of 2,4-bis-anilinopyrimidines

AU - Bardelle, Catherine

AU - Cross, Darren

AU - Davenport, Sara

AU - Kettle, Jason G.

AU - Ko, Eun Jung

AU - Leach, Andrew G.

AU - Mortlock, Andrew

AU - Read, Jon

AU - Roberts, Nicola J.

AU - Robins, Peter

AU - Williams, Emma J.

PY - 2008/5/1

Y1 - 2008/5/1

N2 - A series of bis-anilinopyrimidines have been identified as potent inhibitors of the tyrosine kinase EphB4. Structural information from two alternative series identified from screening efforts was combined to identify the initial leads.5

AB - A series of bis-anilinopyrimidines have been identified as potent inhibitors of the tyrosine kinase EphB4. Structural information from two alternative series identified from screening efforts was combined to identify the initial leads.5

KW - kinase

KW - EphB4

KW - structure-based design

KW - lead identification

U2 - 10.1016/j.bmcl.2008.04.015

DO - 10.1016/j.bmcl.2008.04.015

M3 - Article

SN - 0960-894X

VL - 18

SP - 2776

EP - 2780

JO - Bioorganic & medicinal chemistry letters

JF - Bioorganic & medicinal chemistry letters

IS - 9

ER -

Inhibitors of the tyrosine kinase EphB4: part 1: structure-based design and optimization of a series of 2,4-bis-anilinopyrimidines

Abstract

Keywords

UN SDGs

Access to Document

Fingerprint

Cite this