Discovery of substituted 6-pheny-3H-pyridazin-3-one derivatives as novel c-Met kinase inhibitors

Seung Tae Kang; Eun Young Kim; Raghavendra Archary; Heejung Jung; Chi Hoon Park; Chang Soo Yun; Jong Yeon Hwang; Sang Un Choi; Chonghak Chae; Chong Ock Lee; Hyoung Rae Kim; Jae Du Ha; Dohyun Ryu; Sung Yun Cho

doi:10.1016/j.bmcl.2014.08.067

Discovery of substituted 6-pheny-3H-pyridazin-3-one derivatives as novel c-Met kinase inhibitors

Seung Tae Kang
, Eun Young Kim
, Raghavendra Archary
, Heejung Jung
, Chi Hoon Park
, Chang Soo Yun
, Jong Yeon Hwang
, Sang Un Choi
, Chonghak Chae
, Chong Ock Lee
, Hyoung Rae Kim
, Jae Du Ha
, Dohyun Ryu
, Sung Yun Cho

Department of Chemistry

Sungkyunkwan University
University of Science and Technology UST
Korea Research Institute of Chemical Technology

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

14 Scopus citations

Abstract

We report a series of phenyl substituted pyridazin-3-ones substituted with morpholino-pyrimidines. The SAR of the phenyl was explored and their c-Met kinase and cell-based inhibitory activity toward c-Met driven cell lines were evaluated. Described herein is a potent c-Met inhibitor by structural modification of the parent morpholino-pyridazinone scaffold, with particular focus on the phenyl and pyrimidine substituents.

Original language	English
Pages (from-to)	5093-5097
Number of pages	5
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	24
Issue number	21
DOIs	https://doi.org/10.1016/j.bmcl.2014.08.067
State	Published - 1 Nov 2014

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

SDG 3 Good Health and Well-being

Keywords

c-Met inhibitor
Cancer
Pyridazin-3-one

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10.1016/j.bmcl.2014.08.067

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Kang, S. T., Kim, E. Y., Archary, R., Jung, H., Park, C. H., Yun, C. S., Hwang, J. Y., Choi, S. U., Chae, C., Lee, C. O., Kim, H. R., Ha, J. D., Ryu, D., & Cho, S. Y. (2014). Discovery of substituted 6-pheny-3H-pyridazin-3-one derivatives as novel c-Met kinase inhibitors. Bioorganic and Medicinal Chemistry Letters, 24(21), 5093-5097. https://doi.org/10.1016/j.bmcl.2014.08.067

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title = "Discovery of substituted 6-pheny-3H-pyridazin-3-one derivatives as novel c-Met kinase inhibitors",

abstract = "We report a series of phenyl substituted pyridazin-3-ones substituted with morpholino-pyrimidines. The SAR of the phenyl was explored and their c-Met kinase and cell-based inhibitory activity toward c-Met driven cell lines were evaluated. Described herein is a potent c-Met inhibitor by structural modification of the parent morpholino-pyridazinone scaffold, with particular focus on the phenyl and pyrimidine substituents.",

keywords = "c-Met inhibitor, Cancer, Pyridazin-3-one",

author = "Kang, \{Seung Tae\} and Kim, \{Eun Young\} and Raghavendra Archary and Heejung Jung and Park, \{Chi Hoon\} and Yun, \{Chang Soo\} and Hwang, \{Jong Yeon\} and Choi, \{Sang Un\} and Chonghak Chae and Lee, \{Chong Ock\} and Kim, \{Hyoung Rae\} and Ha, \{Jae Du\} and Dohyun Ryu and Cho, \{Sung Yun\}",

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doi = "10.1016/j.bmcl.2014.08.067",

language = "English",

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journal = "Bioorganic and Medicinal Chemistry Letters",

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T1 - Discovery of substituted 6-pheny-3H-pyridazin-3-one derivatives as novel c-Met kinase inhibitors

AU - Kang, Seung Tae

AU - Kim, Eun Young

AU - Archary, Raghavendra

AU - Jung, Heejung

AU - Park, Chi Hoon

AU - Yun, Chang Soo

AU - Hwang, Jong Yeon

AU - Choi, Sang Un

AU - Chae, Chonghak

AU - Lee, Chong Ock

AU - Kim, Hyoung Rae

AU - Ha, Jae Du

AU - Ryu, Dohyun

AU - Cho, Sung Yun

PY - 2014/11/1

Y1 - 2014/11/1

N2 - We report a series of phenyl substituted pyridazin-3-ones substituted with morpholino-pyrimidines. The SAR of the phenyl was explored and their c-Met kinase and cell-based inhibitory activity toward c-Met driven cell lines were evaluated. Described herein is a potent c-Met inhibitor by structural modification of the parent morpholino-pyridazinone scaffold, with particular focus on the phenyl and pyrimidine substituents.

AB - We report a series of phenyl substituted pyridazin-3-ones substituted with morpholino-pyrimidines. The SAR of the phenyl was explored and their c-Met kinase and cell-based inhibitory activity toward c-Met driven cell lines were evaluated. Described herein is a potent c-Met inhibitor by structural modification of the parent morpholino-pyridazinone scaffold, with particular focus on the phenyl and pyrimidine substituents.

KW - c-Met inhibitor

KW - Cancer

KW - Pyridazin-3-one

UR - https://www.scopus.com/pages/publications/84907993439

U2 - 10.1016/j.bmcl.2014.08.067

DO - 10.1016/j.bmcl.2014.08.067

M3 - Article

C2 - 25282552

AN - SCOPUS:84907993439

SN - 0960-894X

VL - 24

SP - 5093

EP - 5097

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 21

ER -

Discovery of substituted 6-pheny-3H-pyridazin-3-one derivatives as novel c-Met kinase inhibitors

Abstract

UN SDGs

Keywords

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