Pyrrolo[2,3‐d]pyrimidine (7‐deazapurine) as a privileged scaffold in design of antitumor and antiviral nucleosides

P Perlíková, M Hocek - Medicinal Research Reviews, 2017 - Wiley Online Library
Deazapurine (pyrrolo [2, 3‐d] pyrimidine) nucleosides are important analogues of biogenic
purine nucleosides with diverse biological activities. Replacement of the N7 atom with a …

SQM/COSMO Scoring Function: Reliable Quantum‐Mechanical Tool for Sampling and Ranking in Structure‐Based Drug Design

A Pecina, SM Eyrilmez, C Köprülüoğlu… - …, 2020 - Wiley Online Library
Quantum mechanical (QM) methods have been gaining importance in structure‐based drug
design where a reliable description of protein‐ligand interactions is of utmost significance …

Design, synthesis, and biochemical and biological evaluation of novel 7-deazapurine cyclic dinucleotide analogues as STING receptor agonists

Z Vavrina, P Perlíková, N Milisavljevic… - Journal of Medicinal …, 2022 - ACS Publications
Cyclic dinucleotides (CDNs) are second messengers that activate stimulator of interferon
genes (STING). The cGAS-STING pathway plays a promising role in cancer immunotherapy …

Antiviral activity of 7-substituted 7-deazapurine ribonucleosides, monophosphate prodrugs, and triphoshates against emerging RNA viruses

N Milisavljevic, E Konkolova, J Kozak… - ACS Infectious …, 2021 - ACS Publications
A series of 7-deazaadenine ribonucleosides bearing alkyl, alkenyl, alkynyl, aryl, or hetaryl
groups at position 7 as well as their 5′-O-triphosphates and two types of monophosphate …

Revisiting tubercidin against kinetoplastid parasites: aromatic substitutions at position 7 improve activity and reduce toxicity

F Hulpia, GD Campagnaro, M Scortichini… - European Journal of …, 2019 - Elsevier
The nucleoside antibiotic tubercidin displays strong activity against different target
organisms, but it is notoriously toxic to mammalian cells. The effects of tubercidin against T …

Synthesis and cytotoxic and antiviral profiling of pyrrolo-and furo-fused 7-deazapurine ribonucleosides

A Tokarenko, B Lišková, S Smoleń… - Journal of Medicinal …, 2018 - ACS Publications
Three series of isomeric pyrrolo-and furo-fused 7-deazapurine ribonucleosides were
synthesized and screened for cytostatic and antiviral activity. The synthesis was based on …

Synthesis and cytostatic and antiviral profiling of thieno-fused 7-deazapurine ribonucleosides

M Tichy, S Smoleń, E Tloušt'ová, R Pohl… - Journal of Medicinal …, 2017 - ACS Publications
Two isomeric series of new thieno-fused 7-deazapurine ribonucleosides (derived from 4-
substituted thieno [2′, 3′: 4, 5] pyrrolo [2, 3-d] pyrimidines and thieno [3′, 2′: 4, 5] …

South (S)-and North (N)-methanocarba-7-deazaadenosine analogues as inhibitors of human adenosine kinase

KS Toti, D Osborne, A Ciancetta, D Boison… - Journal of medicinal …, 2016 - ACS Publications
Adenosine kinase (AdK) inhibitors raise endogenous adenosine levels, particularly in
disease states, and have potential for treatment of seizures, neurodegeneration, and …

Deazapurine Nucleoside Analogues for the Treatment of Trichomonas vaginalis

MJ Natto, F Hulpia, ER Kalkman, S Baillie… - ACS infectious …, 2021 - ACS Publications
Trichomoniasis is the most common nonviral sexually transmitted disease in humans, but
treatment options are limited. Here, we report a resorufin-based drug sensitivity assay for …

7-(2-Thienyl)-7-deazaadenosine (AB61), a new potent nucleoside cytostatic with a complex mode of action

P Perlíková, G Rylová, P Nauš, T Elbert… - Molecular Cancer …, 2016 - AACR
(2-Thienyl)-7-deazaadenosine (AB61) showed nanomolar cytotoxic activities against
various cancer cell lines but only mild (micromolar) activities against normal fibroblasts. The …