Adenosine: Synthetic Methods of Its Derivatives and Antitumor Activity

Abstract

Since 1929, several researchers have conducted studies in relation to the nucleoside of adenosine (1) mainly distribution identifying, characterizing their biological importance and synthetic chemistry to which this type of molecule has been subjected to obtain multiple of its derivatives. The receptors that interact with adenosine and its derivatives, called purinergic receptors, are classified as A1, A2A, A2B and A3. In the presence of agonists and antagonists, these receptors are involved in various physiological processes and diseases. This review describes and compares some of the synthetic methods that have been developed over the last 30 years for obtaining some adenosine derivatives, classified according to substitution processes, complexation, mating and conjugation. Finally, we mention that although the concentrations of these nucleosides are low in normal tissues, they can increase rapidly in pathophysiological conditions such as hypoxia, ischemia, inflammation, trauma and cancer. In particular, the evaluation of adenosine derivatives as adjunctive therapy promises to have a significant impact on the treatment of certain cancers, although the transfer of these results to clinical practice requires a deeper understanding of how adenosine regulates the process of tumorigenesis.

The Goldilocks Zone of Healing An unexploited resource for advanced healing

“…The activated Nrf2 then binds to a region of antioxidant response elements (ARE) of numerous antioxidant genes, enhancing their expression and restoring redox homeostasis. Molecules secreted at this stage will be dominated by growth factors and factors that limit inflammatory cell transformation, such as adenosine acting through purinergic P1 receptors(A1, A2A, A2B, and A3) (Valdés, Luna, & Arévalo ;Borea, Gessi, & Merighi 2018). Many of these factors act through G-proteins and the insulin-dependent class I PI3K/Akt2/mTOR pathway, associated with growth and anabolism.…”

Regiospecific route to N9-alkylated thioxanthines

“…Analogues of natural nucleosides are a privileged group of heterocycles in medicinal chemistry, as they form a wide array of biologically active compounds and marketed drug molecules. Heterocycles of this class are primarily considered as antivirals [1][2][3] and antimetabolites, [4][5][6][7] but certain antifungal 8,9 and antibiotic [10][11][12] characteristics have also been described. The purine scaffold is a major part of the unnatural nucleoside class [13][14][15] as several molecules with an N9-acyclic pseudoriboside moiety have been registered as antiviral drugs.…”