We report herein the synthesis and the in vitro antileishmanial evaluation of a series of 6-substituted purines. The most active compounds against Leishmania amazonensis promastigotes were 6-(3'-chloropropylthio)purine 2 [11,12] [corrected] 6-(3'-(thioethylamine)propylthio)purine 5, 6-(alpha-aceticacidthio)purine 7 and 6-(6'-deoxy-1'-O-methyl-beta-D-ribofuranose)purine 14 with an IC(50)=50, 50, 39 and 29 microM, respectively.
Download full-text PDF |
Source |
---|---|
http://dx.doi.org/10.1016/j.ejmech.2006.10.014 | DOI Listing |
Dokl Biochem Biophys
January 2025
Engelhardt Institute of Molecular Biology, Russian Academy of Sciences, Moscow, Russia.
In this work, two new compounds, N-(4,5-dimethoxyphenyl)adenine and N-(3,5-di-trifluoromethylphenyl)adenine, with a broad range of antiviral activity against RNA viruses were identified. We showed that these compounds exhibit pronounced antiviral activity against human poliovirus types 1, 2, and 3, belonging to enterovirus C species. Both compounds also demonstrated pronounced antiviral activity against Coxsackie viruses B3, B5, and B6, belonging to enterovirus B species.
View Article and Find Full Text PDFComput Struct Biotechnol J
December 2024
National Institute of Chemistry, Hajdrihova 19, SI 1000 Ljubljana, Slovenia.
The 4,6-substituted-1,3,5-triazin-2(1)-ones are promising inhibitors of human DNA topoisomerase IIα. To further develop this chemical class targeting the enzyme´s ATP binding site, the triazin-2(1)-one substitution position 6 was optimized. Inspired by binding of preclinical substituted 9-purine derivative, bicyclic substituents were incorporated at position 6 and the utility of this modification was validated by a combination of molecular simulations, dynamic pharmacophores, and free energy calculations.
View Article and Find Full Text PDFViruses
May 2024
Department of Biology, Trent University, 1600 West Bank Drive, Peterborough, ON K9J 0G2, Canada.
Cytokinins (CKs) are a group of N-substituted signaling molecules whose biosynthesis and metabolism have been documented in all kingdoms of life, including vertebrates. While their biological relevance in vertebrate systems continues to be elucidated, they have broadly been documented with therapeutic effects in exogenous applications. In this study, we evaluated the virostatic potential of four types of CKs including, -isopentenyladenine (iP), -isopentenyladenosine (iPR), -isopentenyladenosine-5'monophosphate (iPMP), and 2-methylthiol--isopentenyladenosine (2MeSiPR) against the ranavirus type species, frog virus 3 (FV3).
View Article and Find Full Text PDFBioorg Med Chem Lett
July 2024
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Ankara University, 06560, Ankara, Turkey. Electronic address:
A series of novel 6-(substituted phenyl piperazine)-8-(4-substituted phenyl)-9-cyclopentyl purines, 10-51, were synthesized by a four-step synthesis, achieving an overall yield of about 43 %. The reaction conditions were effectively optimized, and the final products were obtained with high purity and yield in all synthesis steps. The synthesized nucleobases were evaluated for their in vitro cytotoxic activities on selected human cancer cell lines (HUH7 (liver), HCT116 (colon), and MCF7 (breast)) using the Sulforhodamine B (SRB) assay.
View Article and Find Full Text PDFACS Omega
April 2024
Department of Organic Chemistry, Faculty of Science, Palacký University, 17. Listopadu 12, 771 46 Olomouc, Czech Republic.
A new direct regioselective method allowing the introduction of -alkyl groups into appropriate 6-substituted purine derivatives is developed. This method is based on a reaction of -trimethylsilylated purines with a -alkyl halide using SnCl as a catalyst. In this work, we study the structure and optimal reaction conditions leading to the isomer and in some cases also to the isomer.
View Article and Find Full Text PDFEnter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!