Synthesis of highly substituted dibenzo[b,f]azocines and their evaluation as protein kinase inhibitors

Leggy A. Arnold; R. Kiplin Guy

doi:10.1016/j.bmcl.2006.07.078

Synthesis of highly substituted dibenzo[b,f]azocines and their evaluation as protein kinase inhibitors

Leggy A. Arnold
, R. Kiplin Guy

Producción científica: Article › revisión exhaustiva

18 Citas (Scopus)

Resumen

Synthetic routes towards highly substituted eight membered ring heterocycles fused to aryl rings such as the dibenzo[b,f]azocine system are still lacking. Herein, we present a convenient convergent synthetic route towards this heterocyclic class of compounds with possible variations at positions 4, 7, and 11. One member of a library of dibenzo[b,f]azocines with different substituents at position 11 was identified to inhibit protein kinase A activity (IC₅₀ = 122 μM) but not protein kinase C.

Idioma original	English
Páginas (desde-hasta)	5360-5363
Número de páginas	4
Publicación	Bioorganic and Medicinal Chemistry Letters
Volumen	16
N.º	20
DOI	https://doi.org/10.1016/j.bmcl.2006.07.078
Estado	Published - oct 15 2006

Nota bibliográfica

Funding Information:
This work was supported by the HHMI Research Resources Program Grant No. 76296-549901, the NIH (R01 No. DK58080), and the Sandler Research Foundation.

Financiación

This work was supported by the HHMI Research Resources Program Grant No. 76296-549901, the NIH (R01 No. DK58080), and the Sandler Research Foundation.

Financiadores	Número del financiador
Sandler Research Foundation
National Institutes of Health (NIH)
Howard Hughes Medical Institute	76296-549901
National Institute of Diabetes and Digestive and Kidney Diseases	R01DK058080

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.2006.07.078

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title = "Synthesis of highly substituted dibenzo[b,f]azocines and their evaluation as protein kinase inhibitors",

abstract = "Synthetic routes towards highly substituted eight membered ring heterocycles fused to aryl rings such as the dibenzo[b,f]azocine system are still lacking. Herein, we present a convenient convergent synthetic route towards this heterocyclic class of compounds with possible variations at positions 4, 7, and 11. One member of a library of dibenzo[b,f]azocines with different substituents at position 11 was identified to inhibit protein kinase A activity (IC50 = 122 μM) but not protein kinase C.",

keywords = "Dibenzo[b,f]azocine, Kinase inhibitor",

author = "Arnold, \{Leggy A.\} and \{Kiplin Guy\}, R.",

note = "Funding Information: This work was supported by the HHMI Research Resources Program Grant No. 76296-549901, the NIH (R01 No. DK58080), and the Sandler Research Foundation.",

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AU - Arnold, Leggy A.

AU - Kiplin Guy, R.

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PY - 2006/10/15

Y1 - 2006/10/15

N2 - Synthetic routes towards highly substituted eight membered ring heterocycles fused to aryl rings such as the dibenzo[b,f]azocine system are still lacking. Herein, we present a convenient convergent synthetic route towards this heterocyclic class of compounds with possible variations at positions 4, 7, and 11. One member of a library of dibenzo[b,f]azocines with different substituents at position 11 was identified to inhibit protein kinase A activity (IC50 = 122 μM) but not protein kinase C.

AB - Synthetic routes towards highly substituted eight membered ring heterocycles fused to aryl rings such as the dibenzo[b,f]azocine system are still lacking. Herein, we present a convenient convergent synthetic route towards this heterocyclic class of compounds with possible variations at positions 4, 7, and 11. One member of a library of dibenzo[b,f]azocines with different substituents at position 11 was identified to inhibit protein kinase A activity (IC50 = 122 μM) but not protein kinase C.

KW - Dibenzo[b,f]azocine

KW - Kinase inhibitor

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JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

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Synthesis of highly substituted dibenzo[b,f]azocines and their evaluation as protein kinase inhibitors

Resumen

Nota bibliográfica

Financiación

ASJC Scopus subject areas

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