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Design, synthesis and anti-breast cancer evaluation of biaryl pyridine analogues as potent RSK inhibitors.
Cui, Yi-Man; Li, Wei; Shen, Tian-Ze; Tao, Yong-Xing; Liu, Biao-Qi; Li, Xiao-Li; Zhang, Rui-Han; Jiang, De-Wei; Xiao, Wei-Lie.
Affiliation
  • Cui YM; Key Laboratory of Medicinal Chemistry for Natural Resource, Ministry of Education and Yunnan Province, School of Chemical Science and Technology, Yunnan University, Kunming 650091, China.
  • Li W; Key Laboratory of Animal Models and Human Disease Mechanisms of the Chinese Academy of Sciences, Kunming Institute of Zoology, Chinese Academy of Sciences, Kunming, Yunnan 650223, China; Kunming College of Life Sciences, The University of the Chinese Academy of Sciences, Kunming 650201, China.
  • Shen TZ; Key Laboratory of Medicinal Chemistry for Natural Resource, Ministry of Education and Yunnan Province, School of Chemical Science and Technology, Yunnan University, Kunming 650091, China.
  • Tao YX; Key Laboratory of Medicinal Chemistry for Natural Resource, Ministry of Education and Yunnan Province, School of Chemical Science and Technology, Yunnan University, Kunming 650091, China.
  • Liu BQ; Key Laboratory of Medicinal Chemistry for Natural Resource, Ministry of Education and Yunnan Province, School of Chemical Science and Technology, Yunnan University, Kunming 650091, China.
  • Li XL; Key Laboratory of Medicinal Chemistry for Natural Resource, Ministry of Education and Yunnan Province, School of Chemical Science and Technology, Yunnan University, Kunming 650091, China.
  • Zhang RH; Key Laboratory of Medicinal Chemistry for Natural Resource, Ministry of Education and Yunnan Province, School of Chemical Science and Technology, Yunnan University, Kunming 650091, China.
  • Jiang DW; Key Laboratory of Animal Models and Human Disease Mechanisms of the Chinese Academy of Sciences, Kunming Institute of Zoology, Chinese Academy of Sciences, Kunming, Yunnan 650223, China; Kunming College of Life Sciences, The University of the Chinese Academy of Sciences, Kunming 650201, China. Elect
  • Xiao WL; Key Laboratory of Medicinal Chemistry for Natural Resource, Ministry of Education and Yunnan Province, School of Chemical Science and Technology, Yunnan University, Kunming 650091, China. Electronic address: xiaoweilie@ynu.edu.cn.
Bioorg Med Chem Lett ; 59: 128565, 2022 03 01.
Article in En | MEDLINE | ID: mdl-35065234
In order to discover and develop the new RSK kinase inhibitor, 50 pyridyl biaryl derivatives were designed and synthesized with LJH685 as the lead compound and their anti-tumor ability was tested. The results showed that the ability of 7d compound to inhibit the phosphorylation of YB-1 was comparable to that of LJH685. Among them, after preliminary screening, compound 7d showed good activity in inhibiting cell proliferation. Therefore, we took 7d as an example and performed molecular docking analysis on it. Judging from the overlapping combination diagram with LJH685, the results have verified that compound 7d has a similar skeleton to LJH685 and has a similar docking effect with RSK. Therefore, compound 7d is in line with the RSK inhibitor we designed and could be developed to a promising anti-tumor drug in the future.
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Pyridines / Drug Design / Ribosomal Protein S6 Kinases, 90-kDa / Protein Kinase Inhibitors / Antineoplastic Agents Limits: Humans Language: En Journal: Bioorg Med Chem Lett Journal subject: BIOQUIMICA / QUIMICA Year: 2022 Type: Article Affiliation country: China
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Pyridines / Drug Design / Ribosomal Protein S6 Kinases, 90-kDa / Protein Kinase Inhibitors / Antineoplastic Agents Limits: Humans Language: En Journal: Bioorg Med Chem Lett Journal subject: BIOQUIMICA / QUIMICA Year: 2022 Type: Article Affiliation country: China