Topical advances in PIM kinases and their inhibitors: Medicinal chemistry perspectives

Cytosolic PIM kinases are the members of serine/ threonine family play a crucial role in the cancer progression and development. Overexpression of PIM kinases is observed in various types of cancers including prostate, hematological, pancreatic, breast carcinoma and likewise. PIM kinases have now been considered as limelight target for the discovery of new molecules as novel anticancer agents as no drug is in the market targeting PIM kinases. In the last two decades, numerous PIM kinase inhibitors have been developed and few of them were in clinical trial phases but could not pass the pipeline of the clinical trials. The present comprehensive review intends to cover biological and the structural aspects of PIM kinases and also medicinal chemistry of PIM inhibitors developed in recent years. •PIM kinases considered as a new target for the discovery of new drug candidates against prostate and hematological cancers.•Structural insights of the PIM kinase X-Ray crystal structure.•Strategies to develop PIM kinase inhibitors based on the crystal structure of PIM kinases.•Detailed report of the PIM kinases inhibitors reported since two decades (2000–2021).•Mutations in the PIM kinase.