Synthesis and biological evaluation of N-cyclopropylbenzamide-benzophenone hybrids as novel and selective p38 mitogen activated protein kinase (MAPK) inhibitors

Jinyuk Heo; Hanbo Shin; Jun Lee; Taelim Kim; Kyung Soo Inn; Nam Jung Kim

doi:10.1016/j.bmcl.2015.06.036

Synthesis and biological evaluation of N-cyclopropylbenzamide-benzophenone hybrids as novel and selective p38 mitogen activated protein kinase (MAPK) inhibitors

Jinyuk Heo, Hanbo Shin, Jun Lee, Taelim Kim, Kyung Soo Inn, Nam Jung Kim

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

22 Citations (Scopus)

Abstract

A series of hybrid molecules consisting of benzophenones and N-cyclopropyl-3-methylbenzamides were synthesized and biologically evaluated as novel p38 mitogen activated protein kinase (MAPK) inhibitors. In particular, we found that compound 10g displayed potent p38α MAPK inhibitory activity (IC₅₀ = 0.027 μM), high kinase selectivity, and significant anti-inflammatory activity in THP-1 monocyte cells.

Original language	English
Pages (from-to)	3694-3698
Number of pages	5
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	25
Issue number	17
DOIs	https://doi.org/10.1016/j.bmcl.2015.06.036
Publication status	Published - 3 Aug 2015

Bibliographical note

Publisher Copyright:
© 2015 Elsevier Ltd.

Keywords

Benzophenone
Hybrid
Kinase selectivity
N-Cyclopropylbenzamide
P38 mitogen activated protein kinase inhibitor

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10.1016/j.bmcl.2015.06.036

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title = "Synthesis and biological evaluation of N-cyclopropylbenzamide-benzophenone hybrids as novel and selective p38 mitogen activated protein kinase (MAPK) inhibitors",

abstract = "A series of hybrid molecules consisting of benzophenones and N-cyclopropyl-3-methylbenzamides were synthesized and biologically evaluated as novel p38 mitogen activated protein kinase (MAPK) inhibitors. In particular, we found that compound 10g displayed potent p38α MAPK inhibitory activity (IC50 = 0.027 μM), high kinase selectivity, and significant anti-inflammatory activity in THP-1 monocyte cells.",

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author = "Jinyuk Heo and Hanbo Shin and Jun Lee and Taelim Kim and Inn, {Kyung Soo} and Kim, {Nam Jung}",

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doi = "10.1016/j.bmcl.2015.06.036",

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T1 - Synthesis and biological evaluation of N-cyclopropylbenzamide-benzophenone hybrids as novel and selective p38 mitogen activated protein kinase (MAPK) inhibitors

AU - Heo, Jinyuk

AU - Shin, Hanbo

AU - Lee, Jun

AU - Kim, Taelim

AU - Inn, Kyung Soo

AU - Kim, Nam Jung

PY - 2015/8/3

Y1 - 2015/8/3

N2 - A series of hybrid molecules consisting of benzophenones and N-cyclopropyl-3-methylbenzamides were synthesized and biologically evaluated as novel p38 mitogen activated protein kinase (MAPK) inhibitors. In particular, we found that compound 10g displayed potent p38α MAPK inhibitory activity (IC50 = 0.027 μM), high kinase selectivity, and significant anti-inflammatory activity in THP-1 monocyte cells.

AB - A series of hybrid molecules consisting of benzophenones and N-cyclopropyl-3-methylbenzamides were synthesized and biologically evaluated as novel p38 mitogen activated protein kinase (MAPK) inhibitors. In particular, we found that compound 10g displayed potent p38α MAPK inhibitory activity (IC50 = 0.027 μM), high kinase selectivity, and significant anti-inflammatory activity in THP-1 monocyte cells.

KW - Benzophenone

KW - Hybrid

KW - Kinase selectivity

KW - N-Cyclopropylbenzamide

KW - P38 mitogen activated protein kinase inhibitor

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DO - 10.1016/j.bmcl.2015.06.036

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SN - 0960-894X

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EP - 3698

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 17

ER -

Synthesis and biological evaluation of N-cyclopropylbenzamide-benzophenone hybrids as novel and selective p38 mitogen activated protein kinase (MAPK) inhibitors

Abstract

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Keywords

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