Synthesis and biological evaluation of quinoxaline derivatives as specific c-Met kinase inhibitors

Bioorg Med Chem Lett. 2020 Jul 1;30(13):127189. doi: 10.1016/j.bmcl.2020.127189.

Seung Chan Kim ¹, Pulla Reddy Boggu ², Ha Na Yu ³, So Young Ki ³, Jun Min Jung ², Yeon Su Kim ², Gi Min Park ², Sang Ho Ma ², In Su Kim ², Young Hoon Jung ⁴

Affiliations

1 School of Pharmacy, Sungkyunkwan University, Suwon 16419, Republic of Korea; R&D Center, CJ HealthCare Corporation, Icheon 17389, Republic of Korea.
2 School of Pharmacy, Sungkyunkwan University, Suwon 16419, Republic of Korea.
3 R&D Center, CJ HealthCare Corporation, Icheon 17389, Republic of Korea.
4 School of Pharmacy, Sungkyunkwan University, Suwon 16419, Republic of Korea. Electronic address: [email protected].

PMID: 32371098 DOI: 10.1016/j.bmcl.2020.127189

Abstract

A series of novel quinoxaline derivatives were synthesized and evaluated for their inhibitory activity against c-Met kinase enzyme. Most of the tested compounds exhibited potent inhibitory activity. All the synthesized quinoxaline compounds were further examined against c-Met overexpressed human gastric Cancer cell line (MKN-45), which showed good inhibitory activity. Among the synthesized compounds, compound 4 exhibited better tumor growth inhibition in the animal model study; we also confirmed its acceptable drug property and highly selective target activity.

Keywords

Quinoxaline; Synthesis; c-Met inhibitors; c-Met kinase.

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