N-(5-Phenylpentan-1-yl)adenine-A New Non-competitive Receptor-Specific Anti-cytokinin.

For the first time, N-(5-phenylpentan-1-yl)adenine, a synthetic adenine derivative with a receptor-specific anticytokinin effect, was obtained. This compound exhibits a pronounced anticytokinin effect, reducing cytokinin-induced expression of the GUS reporter gene when interacting with the cytokinin receptor CRE1/AHK4 of the model plant Arabidopsis thaliana. This effect manifests itself much weaker with the related AHK2 receptor and is not observed at all with the AHK3 receptor.

Nucleoside Analog 2',3'-Isopropylidene-5-Iodouridine as Novel Efficient Inhibitor of HIV-1.

Nucleoside reverse transcriptase inhibitors are the first class of drugs to be approved by the FDA for the suppression of HIV-1 and are widely used for this purpose in combination with drugs of other classes. Despite the progress in HIV-1 treatment, there is still the need to develop novel efficient antivirals. Here the efficiency of HIV-1 inhibition by a set of original 5-substituted uridine nucleosides was studied.

Purine Nucleosides and Analogues Bearing Chiral Substituents: Medicinal Chemistry and Therapeutic Perspective.

Adenosine and its analogues play an important role as bioregulators of metabolic processes in animal cells, affecting a variety of metabolic functions by acting through the purinergic signaling system. Synthesis and structure-activity relationship for some known purine nucleosides bearing chiral substituents are considered in this work. These compounds represent a promising potential as drug prototypes for targeted therapy of cancer, metabolic dysfunctions, and neuronal disorders due to their enhanced selectivity to receptors of the purinergic signaling system.

The Lipophilic Purine Nucleoside-Tdp1 Inhibitor-Enhances DNA Damage Induced by Topotecan In Vitro and Potentiates the Antitumor Effect of Topotecan In Vivo.

The use of cancer chemotherapy sensitizers is a promising approach to induce the effect of clinically used anticancer treatments. One of the interesting targets is Tyrosyl-DNA Phosphodiesterase 1 (Tdp1), a DNA-repair enzyme, that may prevent the action of clinical Topoisomerase 1 (Top1) inhibitors, such as topotecan (Tpc). Tdp1 eliminates covalent Top1-DNA (Top1c) complexes that appear under the action of topotecan and determines the cytotoxic effect of this drug.