Discovery, synthesis and characterization of a series of 7-aryl-imidazo[1,2-a]pyridine-3-ylquinolines as activin-like kinase (ALK) inhibitors

Darren W. Engers; Sean R. Bollinger; Andrew S. Felts; Anish K. Vadukoot; Charles H. Williams; Anna L. Blobaum; Craig W. Lindsley; Charles C. Hong; Corey R. Hopkins

doi:10.1016/j.bmcl.2020.127418

Discovery, synthesis and characterization of a series of 7-aryl-imidazo[1,2-a]pyridine-3-ylquinolines as activin-like kinase (ALK) inhibitors

Darren W. Engers, Sean R. Bollinger, Andrew S. Felts, Anish K. Vadukoot, Charles H. Williams, Anna L. Blobaum, Craig W. Lindsley, Charles C. Hong, Corey R. Hopkins

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

7 Scopus citations

Abstract

The activin-like kinases are a family of kinases that play important roles in a variety of disease states. Of this class of kinases, ALK2, has been shown by a gain-of-function to be the primary driver of the childhood skeletal disease fibrodysplasia ossificans progressiva (FOP) and more recently the pediatric cancer diffuse intrinsic pontine glioma (DIPG). Herein, we report our efforts to identify a novel imidazo[1,2-a]pyridine scaffold as potent inhibitors of ALK2 with good in vivo pharmacokinetic properties suitable for future animal studies.

Original language	English (US)
Article number	127418
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	30
Issue number	18
DOIs	https://doi.org/10.1016/j.bmcl.2020.127418
State	Published - Sep 15 2020

Keywords

ALK2
ALK3
Activin-like kinase inhibitors
BMP inhibitors

ASJC Scopus subject areas

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

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Engers, D. W., Bollinger, S. R., Felts, A. S., Vadukoot, A. K., Williams, C. H., Blobaum, A. L., Lindsley, C. W., Hong, C. C., & Hopkins, C. R. (2020). Discovery, synthesis and characterization of a series of 7-aryl-imidazo[1,2-a]pyridine-3-ylquinolines as activin-like kinase (ALK) inhibitors. Bioorganic and Medicinal Chemistry Letters, 30(18), Article 127418. https://doi.org/10.1016/j.bmcl.2020.127418

Engers, DW, Bollinger, SR, Felts, AS, Vadukoot, AK, Williams, CH, Blobaum, AL, Lindsley, CW, Hong, CC & Hopkins, CR 2020, 'Discovery, synthesis and characterization of a series of 7-aryl-imidazo[1,2-a]pyridine-3-ylquinolines as activin-like kinase (ALK) inhibitors', Bioorganic and Medicinal Chemistry Letters, vol. 30, no. 18, 127418. https://doi.org/10.1016/j.bmcl.2020.127418

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abstract = "The activin-like kinases are a family of kinases that play important roles in a variety of disease states. Of this class of kinases, ALK2, has been shown by a gain-of-function to be the primary driver of the childhood skeletal disease fibrodysplasia ossificans progressiva (FOP) and more recently the pediatric cancer diffuse intrinsic pontine glioma (DIPG). Herein, we report our efforts to identify a novel imidazo[1,2-a]pyridine scaffold as potent inhibitors of ALK2 with good in vivo pharmacokinetic properties suitable for future animal studies.",

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AU - Bollinger, Sean R.

AU - Felts, Andrew S.

AU - Vadukoot, Anish K.

AU - Williams, Charles H.

AU - Blobaum, Anna L.

AU - Lindsley, Craig W.

AU - Hong, Charles C.

AU - Hopkins, Corey R.

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Discovery, synthesis and characterization of a series of 7-aryl-imidazo[1,2-a]pyridine-3-ylquinolines as activin-like kinase (ALK) inhibitors

Abstract

Keywords

ASJC Scopus subject areas

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