Synthesis and structure-activity relationship of 3-phenyl-3H-quinazolin-4-one derivatives as CXCR3 chemokine receptor antagonists

S. Storelli; P.W. Verdijk; D. Verzijl; H. Timmerman; A. van de Stolpe; C.P. Tensen; M.J. Smit; I.J. De Esch; R. Leurs

doi:10.1016/j.bmcl.2005.03.070

Synthesis and structure-activity relationship of 3-phenyl-3H-quinazolin-4-one derivatives as CXCR3 chemokine receptor antagonists

S. Storelli
, P.W. Verdijk
, D. Verzijl
, H. Timmerman
, A. van de Stolpe
, C.P. Tensen
, M.J. Smit
, I.J. De Esch
, R. Leurs

Chemistry and Pharmaceutical Sciences

Research output: Contribution to Journal › Article › Academic › peer-review

Abstract

A series of 3-phenyl-3H-quinazolin-4-ones have been synthesized and tested for affinity and activity at the chemokine CXCR3 receptor. The most potent compound (1d) has been evaluated using radioligand binding and calcium mobilization assays and is considered a useful tool for further characterization of the CXCR3 receptor. © 2005 Elsevier Ltd. All rights reserved.

Original language	English
Pages (from-to)	2910-3
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	15
Issue number	11
DOIs	https://doi.org/10.1016/j.bmcl.2005.03.070
Publication status	Published - 2005

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10.1016/j.bmcl.2005.03.070

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Storelli, S., Verdijk, P. W., Verzijl, D., Timmerman, H., van de Stolpe, A., Tensen, C. P., Smit, M. J., De Esch, I. J., & Leurs, R. (2005). Synthesis and structure-activity relationship of 3-phenyl-3H-quinazolin-4-one derivatives as CXCR3 chemokine receptor antagonists. Bioorganic and Medicinal Chemistry Letters, 15(11), 2910-3. https://doi.org/10.1016/j.bmcl.2005.03.070

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abstract = "A series of 3-phenyl-3H-quinazolin-4-ones have been synthesized and tested for affinity and activity at the chemokine CXCR3 receptor. The most potent compound (1d) has been evaluated using radioligand binding and calcium mobilization assays and is considered a useful tool for further characterization of the CXCR3 receptor. {\textcopyright} 2005 Elsevier Ltd. All rights reserved.",

author = "S. Storelli and P.W. Verdijk and D. Verzijl and H. Timmerman and \{van de Stolpe\}, A. and C.P. Tensen and M.J. Smit and \{De Esch\}, I.J. and R. Leurs",

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doi = "10.1016/j.bmcl.2005.03.070",

language = "English",

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TY - JOUR

T1 - Synthesis and structure-activity relationship of 3-phenyl-3H-quinazolin-4-one derivatives as CXCR3 chemokine receptor antagonists

AU - Storelli, S.

AU - Verdijk, P.W.

AU - Verzijl, D.

AU - Timmerman, H.

AU - van de Stolpe, A.

AU - Tensen, C.P.

AU - Smit, M.J.

AU - De Esch, I.J.

AU - Leurs, R.

PY - 2005

Y1 - 2005

N2 - A series of 3-phenyl-3H-quinazolin-4-ones have been synthesized and tested for affinity and activity at the chemokine CXCR3 receptor. The most potent compound (1d) has been evaluated using radioligand binding and calcium mobilization assays and is considered a useful tool for further characterization of the CXCR3 receptor. © 2005 Elsevier Ltd. All rights reserved.

AB - A series of 3-phenyl-3H-quinazolin-4-ones have been synthesized and tested for affinity and activity at the chemokine CXCR3 receptor. The most potent compound (1d) has been evaluated using radioligand binding and calcium mobilization assays and is considered a useful tool for further characterization of the CXCR3 receptor. © 2005 Elsevier Ltd. All rights reserved.

U2 - 10.1016/j.bmcl.2005.03.070

DO - 10.1016/j.bmcl.2005.03.070

M3 - Article

SN - 0960-894X

VL - 15

SP - 2910

EP - 2913

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 11

ER -

Synthesis and structure-activity relationship of 3-phenyl-3H-quinazolin-4-one derivatives as CXCR3 chemokine receptor antagonists

Abstract

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