Discovery of 2-(α-methylbenzylamino) pyrazines as potent Type II inhibitors of FMS

Christopher J Burns; Michael F. Harte; Xianyong Bu; Emmanuelle Fantino; Marilena Giarrusso; Max Joffe; Margarita Kurek; Fiona Sue Legge; Pasquale Razzino; Stephen Su; Herbert Treutlein; Soo San Wan; Jun Zeng; Andrew F. Wilks

doi:10.1016/j.bmcl.2008.12.073

Discovery of 2-(α-methylbenzylamino) pyrazines as potent Type II inhibitors of FMS

Christopher J Burns, Michael F. Harte, Xianyong Bu, Emmanuelle Fantino, Marilena Giarrusso, Max Joffe, Margarita Kurek, Fiona Sue Legge, Pasquale Razzino, Stephen Su, Herbert Treutlein, Soo San Wan, Jun Zeng, Andrew F. Wilks

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

14 Citations (Scopus)

Abstract

A series of 2-(α-methylbenzylamino) pyrazines have shown to be potent inhibitors of the FMS tyrosine receptor kinase. Details of SAR studies, modeling and synthesis of compounds within this series are reported.

Original language	English
Pages (from-to)	1206-1209
Number of pages	4
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	19
Issue number	4
DOIs	https://doi.org/10.1016/j.bmcl.2008.12.073
Publication status	Published - 15 Feb 2009
Externally published	Yes

Keywords

CSF-1
CSF-1R
FMS
Kinase inhibitor
M-CSF-1
Macrophage

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10.1016/j.bmcl.2008.12.073

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Burns, C. J., Harte, M. F., Bu, X., Fantino, E., Giarrusso, M., Joffe, M., Kurek, M., Legge, F. S., Razzino, P., Su, S., Treutlein, H., Wan, S. S., Zeng, J., & Wilks, A. F. (2009). Discovery of 2-(α-methylbenzylamino) pyrazines as potent Type II inhibitors of FMS. Bioorganic and Medicinal Chemistry Letters, 19(4), 1206-1209. https://doi.org/10.1016/j.bmcl.2008.12.073

Burns, Christopher J ; Harte, Michael F. ; Bu, Xianyong ; Fantino, Emmanuelle ; Giarrusso, Marilena ; Joffe, Max ; Kurek, Margarita ; Legge, Fiona Sue ; Razzino, Pasquale ; Su, Stephen ; Treutlein, Herbert ; Wan, Soo San ; Zeng, Jun ; Wilks, Andrew F. / Discovery of 2-(α-methylbenzylamino) pyrazines as potent Type II inhibitors of FMS. In: Bioorganic and Medicinal Chemistry Letters. 2009 ; Vol. 19, No. 4. pp. 1206-1209.

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abstract = "A series of 2-(α-methylbenzylamino) pyrazines have shown to be potent inhibitors of the FMS tyrosine receptor kinase. Details of SAR studies, modeling and synthesis of compounds within this series are reported.",

keywords = "CSF-1, CSF-1R, FMS, Kinase inhibitor, M-CSF-1, Macrophage",

author = "Burns, {Christopher J} and Harte, {Michael F.} and Xianyong Bu and Emmanuelle Fantino and Marilena Giarrusso and Max Joffe and Margarita Kurek and Legge, {Fiona Sue} and Pasquale Razzino and Stephen Su and Herbert Treutlein and Wan, {Soo San} and Jun Zeng and Wilks, {Andrew F.}",

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Discovery of 2-(α-methylbenzylamino) pyrazines as potent Type II inhibitors of FMS. / Burns, Christopher J; Harte, Michael F.; Bu, Xianyong; Fantino, Emmanuelle; Giarrusso, Marilena; Joffe, Max; Kurek, Margarita; Legge, Fiona Sue; Razzino, Pasquale; Su, Stephen; Treutlein, Herbert; Wan, Soo San; Zeng, Jun; Wilks, Andrew F.

In: Bioorganic and Medicinal Chemistry Letters, Vol. 19, No. 4, 15.02.2009, p. 1206-1209.

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

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T1 - Discovery of 2-(α-methylbenzylamino) pyrazines as potent Type II inhibitors of FMS

AU - Burns, Christopher J

AU - Harte, Michael F.

AU - Bu, Xianyong

AU - Fantino, Emmanuelle

AU - Giarrusso, Marilena

AU - Joffe, Max

AU - Kurek, Margarita

AU - Legge, Fiona Sue

AU - Razzino, Pasquale

AU - Su, Stephen

AU - Treutlein, Herbert

AU - Wan, Soo San

AU - Zeng, Jun

AU - Wilks, Andrew F.

PY - 2009/2/15

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AB - A series of 2-(α-methylbenzylamino) pyrazines have shown to be potent inhibitors of the FMS tyrosine receptor kinase. Details of SAR studies, modeling and synthesis of compounds within this series are reported.

KW - CSF-1

KW - CSF-1R

KW - FMS

KW - Kinase inhibitor

KW - M-CSF-1

KW - Macrophage

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JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

SN - 0960-894X

IS - 4

ER -

Discovery of 2-(α-methylbenzylamino) pyrazines as potent Type II inhibitors of FMS

Abstract

Keywords

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