title: Purine Analogues as Kinase Inhibitors: A Review.
abstract: 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 heterocyclic nucleus 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.
authors.forename: Sahil
authors.initials: S
authors.lastname: Sharma
authors.forename: Samir
authors.initials: S
authors.lastname: Mehndiratta
authors.forename: Sunil
authors.initials: S
authors.lastname: Kumar
authors.forename: Jagjeet
authors.initials: J
authors.lastname: Singh
authors.forename: Preet M S
authors.initials: PM
authors.lastname: Bedi
authors.affiliation: Department of Pharmaceutical Chemistry, ISF College of Pharmacy, Moga, Punjab -142001, India. kunal_8855@rediffmail.com.
authors.forename: Kunal
authors.initials: K
authors.lastname: Nepali
mesh_terms: D000970:Antineoplastic Agents / Q000494:pharmacology / Q000627:therapeutic use*; D006801:Humans; D007938:Leukemia / Q000188:drug therapy; D047428:Protein Kinase Inhibitors / Q000494:pharmacology / Q000627:therapeutic use*; D011687:Purines / Q000494:pharmacology / Q000627:therapeutic use*; D013329:Structure-Activity Relationship
chemical_list: D000970:Antineoplastic Agents; D047428:Protein Kinase Inhibitors; D011687:Purines