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<p>Cancer is one of the major causes of human mortality worldwide. The available cancer therapy is associated with significant adverse effects. Targeted therapies represent a promising approach in drug discovery, focusing on specific pathways involved in cancer growth. Pim kinases play an important role in cancer signal transduction, promoting cell proliferation and inhibiting apoptosis, particularly in prostate and breast cancers. Pim-kinase inhibitors have emerged as an effective targeted therapy to treat cancer. Nitrogen-containing heterocyclic compounds have been reported to bind selectively with a specific Pim kinase enzyme. Various interesting compounds of nitrogen-containing heterocyclic rings, such as pyridine, pyrimidine, thiazole, quinoline, pyrazole, and indole, etc., have shown promising Pim kinase inhibitory potential. This review discusses the design strategies, molecular docking studies, and structure-activity relationships (SAR), including the importance of nitrogen heterocyclic derivatives in the drug discovery of anticancer agents. These developments can further improve the targeted therapy and could help in mitigating the adverse drug effects in cancer treatment. Recent advancements in the development of Pim kinase inhibitors as anti-neoplastic agents could pave the way for the discovery and development of more novel and clinically useful Pim kinase inhibitors for future cancer therapies.</p> Graphical abstract <p><i>N</i>-heterocyclic derivatives are promising as Pim kinase inhibitors in treating cancer including pyridine, pyrimidine, thiazole, quinoline, pyrazole and indole.</p> <p></p>

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Unlocking the therapeutic potential of N-heterocyclic derivatives as Pim kinase inhibitors

  • 期刊论文

  • 发表日期：

    2025年12月4日

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  • Rajarshi Nath,
  • Arka Chakraborty,
  • Lakshminarayan Das,
  • Anhic Chakraborty,
  • Sumel Asique,
  • Sumit Maji,
  • Sayan Bhattacharjee,
  • Shah Alam Khan,
  • Biplab Debnath,
  • Md Jawaid Akhtar

摘要

Cancer is one of the major causes of human mortality worldwide. The available cancer therapy is associated with significant adverse effects. Targeted therapies represent a promising approach in drug discovery, focusing on specific pathways involved in cancer growth. Pim kinases play an important role in cancer signal transduction, promoting cell proliferation and inhibiting apoptosis, particularly in prostate and breast cancers. Pim-kinase inhibitors have emerged as an effective targeted therapy to treat cancer. Nitrogen-containing heterocyclic compounds have been reported to bind selectively with a specific Pim kinase enzyme. Various interesting compounds of nitrogen-containing heterocyclic rings, such as pyridine, pyrimidine, thiazole, quinoline, pyrazole, and indole, etc., have shown promising Pim kinase inhibitory potential. This review discusses the design strategies, molecular docking studies, and structure-activity relationships (SAR), including the importance of nitrogen heterocyclic derivatives in the drug discovery of anticancer agents. These developments can further improve the targeted therapy and could help in mitigating the adverse drug effects in cancer treatment. Recent advancements in the development of Pim kinase inhibitors as anti-neoplastic agents could pave the way for the discovery and development of more novel and clinically useful Pim kinase inhibitors for future cancer therapies.

Graphical abstract

N-heterocyclic derivatives are promising as Pim kinase inhibitors in treating cancer including pyridine, pyrimidine, thiazole, quinoline, pyrazole and indole.