3-Acyl-2,6-diaminopyridines as cyclin-dependent kinase inhibitors: Synthesis and biological evaluation

Ronghui Lin; Yanhua Lu; Steven K. Wetter; Peter J. Connolly; Ignatius J. Turchi; William V. Murray; Stuart L. Emanuel; Robert H. Gruninger; Angel R. Fuentes-Pesquera; Mary Adams; Niranjan Pandey; Sandra Moreno-Mazza; Steven A. Middleton; Linda K. Jolliffe

doi:10.1016/j.bmcl.2005.03.024

3-Acyl-2,6-diaminopyridines as cyclin-dependent kinase inhibitors: Synthesis and biological evaluation

Ronghui Lin, Yanhua Lu, Steven K. Wetter, Peter J. Connolly, Ignatius J. Turchi, William V. Murray, Stuart L. Emanuel, Robert H. Gruninger, Angel R. Fuentes-Pesquera, Mary Adams, Niranjan Pandey, Sandra Moreno-Mazza, Steven A. Middleton, Linda K. Jolliffe

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

25 Scopus citations

Abstract

A novel series of 2,6-diamino-3-acylpyridines were designed and synthesized as cyclin-dependent kinase (CDK) inhibitors. The representative compounds 2r and 11 showed potent CDK1 and CDK2 inhibitory activities and inhibited cellular proliferation in HeLa, HCT116, and A375 tumor cells.

Original language	English (US)
Pages (from-to)	2221-2224
Number of pages	4
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	15
Issue number	9
DOIs	https://doi.org/10.1016/j.bmcl.2005.03.024
State	Published - May 2 2005
Externally published	Yes

Keywords

CDK inhibitor
Cell proliferation inhibitor
Cyclin-dependent kinase inhibitor
Synthesis

ASJC Scopus subject areas

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

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10.1016/j.bmcl.2005.03.024

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Lin, R., Lu, Y., Wetter, S. K., Connolly, P. J., Turchi, I. J., Murray, W. V., Emanuel, S. L., Gruninger, R. H., Fuentes-Pesquera, A. R., Adams, M., Pandey, N., Moreno-Mazza, S., Middleton, S. A., & Jolliffe, L. K. (2005). 3-Acyl-2,6-diaminopyridines as cyclin-dependent kinase inhibitors: Synthesis and biological evaluation. Bioorganic and Medicinal Chemistry Letters, 15(9), 2221-2224. https://doi.org/10.1016/j.bmcl.2005.03.024

Lin, R, Lu, Y, Wetter, SK, Connolly, PJ, Turchi, IJ, Murray, WV, Emanuel, SL, Gruninger, RH, Fuentes-Pesquera, AR, Adams, M, Pandey, N, Moreno-Mazza, S, Middleton, SA & Jolliffe, LK 2005, '3-Acyl-2,6-diaminopyridines as cyclin-dependent kinase inhibitors: Synthesis and biological evaluation', Bioorganic and Medicinal Chemistry Letters, vol. 15, no. 9, pp. 2221-2224. https://doi.org/10.1016/j.bmcl.2005.03.024

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title = "3-Acyl-2,6-diaminopyridines as cyclin-dependent kinase inhibitors: Synthesis and biological evaluation",

abstract = "A novel series of 2,6-diamino-3-acylpyridines were designed and synthesized as cyclin-dependent kinase (CDK) inhibitors. The representative compounds 2r and 11 showed potent CDK1 and CDK2 inhibitory activities and inhibited cellular proliferation in HeLa, HCT116, and A375 tumor cells.",

keywords = "CDK inhibitor, Cell proliferation inhibitor, Cyclin-dependent kinase inhibitor, Synthesis",

author = "Ronghui Lin and Yanhua Lu and Wetter, {Steven K.} and Connolly, {Peter J.} and Turchi, {Ignatius J.} and Murray, {William V.} and Emanuel, {Stuart L.} and Gruninger, {Robert H.} and Fuentes-Pesquera, {Angel R.} and Mary Adams and Niranjan Pandey and Sandra Moreno-Mazza and Middleton, {Steven A.} and Jolliffe, {Linda K.}",

year = "2005",

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doi = "10.1016/j.bmcl.2005.03.024",

language = "English (US)",

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T1 - 3-Acyl-2,6-diaminopyridines as cyclin-dependent kinase inhibitors

T2 - Synthesis and biological evaluation

AU - Lin, Ronghui

AU - Lu, Yanhua

AU - Wetter, Steven K.

AU - Connolly, Peter J.

AU - Turchi, Ignatius J.

AU - Murray, William V.

AU - Emanuel, Stuart L.

AU - Gruninger, Robert H.

AU - Fuentes-Pesquera, Angel R.

AU - Adams, Mary

AU - Pandey, Niranjan

AU - Moreno-Mazza, Sandra

AU - Middleton, Steven A.

AU - Jolliffe, Linda K.

PY - 2005/5/2

Y1 - 2005/5/2

N2 - A novel series of 2,6-diamino-3-acylpyridines were designed and synthesized as cyclin-dependent kinase (CDK) inhibitors. The representative compounds 2r and 11 showed potent CDK1 and CDK2 inhibitory activities and inhibited cellular proliferation in HeLa, HCT116, and A375 tumor cells.

AB - A novel series of 2,6-diamino-3-acylpyridines were designed and synthesized as cyclin-dependent kinase (CDK) inhibitors. The representative compounds 2r and 11 showed potent CDK1 and CDK2 inhibitory activities and inhibited cellular proliferation in HeLa, HCT116, and A375 tumor cells.

KW - CDK inhibitor

KW - Cell proliferation inhibitor

KW - Cyclin-dependent kinase inhibitor

KW - Synthesis

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JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

SN - 0960-894X

IS - 9

ER -

3-Acyl-2,6-diaminopyridines as cyclin-dependent kinase inhibitors: Synthesis and biological evaluation

Abstract

Keywords

ASJC Scopus subject areas

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