Novel and potent transforming growth factor beta type I receptor kinase domain inhibitor: 7-Amino 4-(2-pyridin-2-yl-5,6-dihydro-4H-pyrrolo[1,2-b] pyrazol-3-yl)-quinolines

Hong Yu Li; Yan Wang; Lei Yan; Robert M. Campbell; Bryan D. Anderson; Jill R. Wagner; Jonathan M. Yingling

doi:10.1016/j.bmcl.2004.04.065

Novel and potent transforming growth factor beta type I receptor kinase domain inhibitor: 7-Amino 4-(2-pyridin-2-yl-5,6-dihydro-4H-pyrrolo[1,2-b] pyrazol-3-yl)-quinolines

Hong Yu Li
, Yan Wang
, Lei Yan
, Robert M. Campbell
, Bryan D. Anderson
, Jill R. Wagner
, Jonathan M. Yingling

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

30 Scopus citations

Abstract

A novel series of 7-amino 4-(2-pyridin-2-yl-5,6-dihydro-4H-pyrrolo[1,2-b] pyrazol-3-yl)-quinolines was synthesized and their TβR-1 inhibitory, p38 MAPK inhibitory, and TβR-1-dependent cellular activity were evaluated. Compound 5a was found to be a highly potent in the enzyme assay and TβR-1-dependent cellular assays. In addition, dimer (4g), with a urea linker, shows a similar enzyme and cellular activity despite a bulky substitution.

Original language	English (US)
Pages (from-to)	3585-3588
Number of pages	4
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	14
Issue number	13
DOIs	https://doi.org/10.1016/j.bmcl.2004.04.065
State	Published - Jul 5 2004
Externally published	Yes

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.2004.04.065

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Li, H. Y., Wang, Y., Yan, L., Campbell, R. M., Anderson, B. D., Wagner, J. R., & Yingling, J. M. (2004). Novel and potent transforming growth factor beta type I receptor kinase domain inhibitor: 7-Amino 4-(2-pyridin-2-yl-5,6-dihydro-4H-pyrrolo[1,2-b] pyrazol-3-yl)-quinolines. Bioorganic and Medicinal Chemistry Letters, 14(13), 3585-3588. https://doi.org/10.1016/j.bmcl.2004.04.065

Novel and potent transforming growth factor beta type I receptor kinase domain inhibitor: 7-Amino 4-(2-pyridin-2-yl-5,6-dihydro-4H-pyrrolo[1,2-b] pyrazol-3-yl)-quinolines. / Li, Hong Yu; Wang, Yan; Yan, Lei et al.
In: Bioorganic and Medicinal Chemistry Letters, Vol. 14, No. 13, 05.07.2004, p. 3585-3588.

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

Li, HY, Wang, Y, Yan, L, Campbell, RM, Anderson, BD, Wagner, JR & Yingling, JM 2004, 'Novel and potent transforming growth factor beta type I receptor kinase domain inhibitor: 7-Amino 4-(2-pyridin-2-yl-5,6-dihydro-4H-pyrrolo[1,2-b] pyrazol-3-yl)-quinolines', Bioorganic and Medicinal Chemistry Letters, vol. 14, no. 13, pp. 3585-3588. https://doi.org/10.1016/j.bmcl.2004.04.065

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title = "Novel and potent transforming growth factor beta type I receptor kinase domain inhibitor: 7-Amino 4-(2-pyridin-2-yl-5,6-dihydro-4H-pyrrolo[1,2-b] pyrazol-3-yl)-quinolines",

abstract = "A novel series of 7-amino 4-(2-pyridin-2-yl-5,6-dihydro-4H-pyrrolo[1,2-b] pyrazol-3-yl)-quinolines was synthesized and their TβR-1 inhibitory, p38 MAPK inhibitory, and TβR-1-dependent cellular activity were evaluated. Compound 5a was found to be a highly potent in the enzyme assay and TβR-1-dependent cellular assays. In addition, dimer (4g), with a urea linker, shows a similar enzyme and cellular activity despite a bulky substitution.",

author = "Li, \{Hong Yu\} and Yan Wang and Lei Yan and Campbell, \{Robert M.\} and Anderson, \{Bryan D.\} and Wagner, \{Jill R.\} and Yingling, \{Jonathan M.\}",

year = "2004",

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doi = "10.1016/j.bmcl.2004.04.065",

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AU - Yan, Lei

AU - Campbell, Robert M.

AU - Anderson, Bryan D.

AU - Wagner, Jill R.

AU - Yingling, Jonathan M.

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Novel and potent transforming growth factor beta type I receptor kinase domain inhibitor: 7-Amino 4-(2-pyridin-2-yl-5,6-dihydro-4H-pyrrolo[1,2-b] pyrazol-3-yl)-quinolines

Abstract

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