Purine analogues as kinase inhibitors: A review

Sahil Sharma, Samir Mehndiratta, Sunil Kumar, Jagjeet Singh, Preet M.S. Bedi, Kunal Nepali

Research output: Contribution to journalReview articlepeer-review

29 Citations (Scopus)


Protein kinases constitute one of the largest and most functionally diverse gene families that regulate key cell functions. In past several years, kinase inhibition has emerged as potential anti-cancer drug target. Purine is a priveleged heterocyclicnucleus which exists in the chemical architecture of various bioactive compounds. Numerous reports on the use of purine analogues in the treatment of acute leukemias (thiopurines, pentostatin), as antiviral (acyclovir, penciclovir, ganciclovir), as immunosuppressive (azathioprine), as antitumor (vidarabine), as bronchodilator (theophylline) have been revealed. In the past decade, purine analogues have emerged as significantly potent kinase inhibitors. A fair amount of research has been done and several patents have also been published highlighting the kinase inhibitory action of purines. Caffeine, 2- aminopurine, purvalanol-A, seleciclib, FSBA, adenosine thiol analogue possessing purine as the basic moiety fall under this category. In view of the use of purines for the inhibition of kinases, there is need for compilation of data specifying the prominence of purines in the treatment of cancer through this mechanism. The structure of the potent compounds, their IC50 values, models used and the enzymes/ receptors/ targets involved have been presented in this review. The present compilation covers the patents published entailing the purines as kinase inhibitors and the purine drugs employed in chemotherapy.

Original languageEnglish
Pages (from-to)308-341
Number of pages34
JournalRecent Patents on Anti-Cancer Drug Discovery
Issue number3
Publication statusPublished - Oct 1 2015
Externally publishedYes


  • Chemotherapy
  • Clinical trials
  • Patents
  • Potential inhibitors
  • Protein kinases
  • Purines

ASJC Scopus subject areas

  • Oncology
  • Drug Discovery
  • Cancer Research
  • Pharmacology (medical)


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