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

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

Keywords

c-Met inhibitor
Cancer
Pyridazin-3-one

UN SDGs

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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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TY - JOUR

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

Keywords

UN SDGs

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