Design strategies, structure activity relationship and mechanistic insights for purines as kinase inhibitors

Sahil Sharma, Jagjeet Singh, Ritu Ojha, Harbinder Singh, Manpreet Kaur, P. M.S. Bedi, Kunal Nepali

Research output: Contribution to journalReview articlepeer-review

52 Citations (Scopus)


Kinases control a diverse set of cellular processes comprising of reversible phosphorylation of proteins. Protein kinases play a pivotal role in human tumor cell proliferation, migration and survival of neoplasia. In the recent past, purine based molecules have emerged as significantly potent kinase inhibitors. In view of their promising potential for the inhibition of kinases, this review article focuses on purines which have progressed as kinase inhibitors during the last five years. A detailed account of the design strategies employed for the synthesis of purine analogs exerting inhibitory effects on diverse kinases has been presented. Apart from presenting the design strategies, the article also highlights the structure activity relationship along with mechanistic insights revealed during the biological evaluation of the purine analogs for kinase inhibition. The interactions with the amino acid residues responsible for kinase inhibitory potential of purine based molecules have also been discussed. In this assemblage, purine based protein kinase inhibitors patented in the past have also been summarized in the tabular form. This compilation will be of great interest for the researchers working in the area of protein kinase inhibitors.

Original languageEnglish
Pages (from-to)298-346
Number of pages49
JournalEuropean Journal of Medicinal Chemistry
Publication statusPublished - Apr 13 2016
Externally publishedYes


  • Cancer
  • Cell lines
  • Design strategies
  • Kinases
  • Purine
  • Structure activity relationship

ASJC Scopus subject areas

  • Pharmacology
  • Drug Discovery
  • Organic Chemistry


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