Discovery of a dihydropyrimidine series of molecules that selectively mimic the biological actions of calcitonin

Jay M. Matthews; Fina Liotta; William Hageman; Ralph A. Rivero; Lori Westover; Maria Yang; Jun Xu; Keith Demarest

doi:10.1016/j.bmcl.2003.12.071

Discovery of a dihydropyrimidine series of molecules that selectively mimic the biological actions of calcitonin

Jay M. Matthews, Fina Liotta, William Hageman, Ralph A. Rivero, Lori Westover, Maria Yang, Jun Xu, Keith Demarest

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

16 Scopus citations

Abstract

The use of a multiplex mimetic assay led us to identify 1,4-dihydropyrimidines with potent and selective calcitonin receptor mimetic activity. Subsequent modification of the dihydropyrimidine scaffold led to a series of molecules that were efficacious in a neonatal mouse calvaria in vitro model. Dihydropyrimidine 5h, in particular, was identified as a calcitonin mimetic (EC₅₀=6 μM), active in-vivo in the Weanling rat model when administered subcutaneously.

Original language	English (US)
Pages (from-to)	1155-1159
Number of pages	5
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	14
Issue number	5
DOIs	https://doi.org/10.1016/j.bmcl.2003.12.071
State	Published - Mar 8 2004
Externally published	Yes

All Science Journal Classification (ASJC) codes

Biochemistry
Molecular Medicine
Molecular Biology
Pharmaceutical Science
Drug Discovery
Clinical Biochemistry
Organic Chemistry

Keywords

Calcitonin
Dihydropyrimidine
GPCR

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10.1016/j.bmcl.2003.12.071

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title = "Discovery of a dihydropyrimidine series of molecules that selectively mimic the biological actions of calcitonin",

abstract = "The use of a multiplex mimetic assay led us to identify 1,4-dihydropyrimidines with potent and selective calcitonin receptor mimetic activity. Subsequent modification of the dihydropyrimidine scaffold led to a series of molecules that were efficacious in a neonatal mouse calvaria in vitro model. Dihydropyrimidine 5h, in particular, was identified as a calcitonin mimetic (EC50=6 μM), active in-vivo in the Weanling rat model when administered subcutaneously.",

keywords = "Calcitonin, Dihydropyrimidine, GPCR",

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doi = "10.1016/j.bmcl.2003.12.071",

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T1 - Discovery of a dihydropyrimidine series of molecules that selectively mimic the biological actions of calcitonin

AU - Matthews, Jay M.

AU - Liotta, Fina

AU - Hageman, William

AU - Rivero, Ralph A.

AU - Westover, Lori

AU - Yang, Maria

AU - Xu, Jun

AU - Demarest, Keith

PY - 2004/3/8

Y1 - 2004/3/8

N2 - The use of a multiplex mimetic assay led us to identify 1,4-dihydropyrimidines with potent and selective calcitonin receptor mimetic activity. Subsequent modification of the dihydropyrimidine scaffold led to a series of molecules that were efficacious in a neonatal mouse calvaria in vitro model. Dihydropyrimidine 5h, in particular, was identified as a calcitonin mimetic (EC50=6 μM), active in-vivo in the Weanling rat model when administered subcutaneously.

AB - The use of a multiplex mimetic assay led us to identify 1,4-dihydropyrimidines with potent and selective calcitonin receptor mimetic activity. Subsequent modification of the dihydropyrimidine scaffold led to a series of molecules that were efficacious in a neonatal mouse calvaria in vitro model. Dihydropyrimidine 5h, in particular, was identified as a calcitonin mimetic (EC50=6 μM), active in-vivo in the Weanling rat model when administered subcutaneously.

KW - Calcitonin

KW - Dihydropyrimidine

KW - GPCR

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M3 - Article

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AN - SCOPUS:1242316923

SN - 0960-894X

VL - 14

SP - 1155

EP - 1159

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 5

ER -

Discovery of a dihydropyrimidine series of molecules that selectively mimic the biological actions of calcitonin

Abstract

All Science Journal Classification (ASJC) codes

Keywords

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