Multi-targeted anti-leukemic drug design with the incorporation of silicon into Nelarabine: How silicon increases bioactivity

Eryilmaz, Esma

doi:10.1016/j.ejps.2019.04.008

Cited by 9 publications

(3 citation statements)

References 34 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…A triazolopyrazine derivative containing silicon that was chosen as the OSM project had not previously investigated any silyl analogues. While silicon-based drugs are rare, some examples of drug-like candidates containing silicon, which are bioavailable via an oral route of administration, are known [16]. Compound 5 was produced using the previously described method, except that the reaction time was increased to 3 h (Scheme 3).…”

Section: Synthesis Of Osm-based Scaffolds Via Coupling Of Primary Alcohols With Chloro-heterocyclesmentioning

confidence: 99%

See 1 more Smart Citation

Synthesis of New Triazolopyrazine Antimalarial Compounds

et al. 2021

View full text Add to dashboard Cite

A radical approach to late-stage functionalization using photoredox and Diversinate™ chemistry on the Open Source Malaria (OSM) triazolopyrazine scaffold (Series 4) resulted in the synthesis of 12 new analogues, which were characterized by NMR, UV, and MS data analysis. The structures of four triazolopyrazines were confirmed by X-ray crystal structure analysis. Several minor and unexpected side products were generated during these studies, including two resulting from a possible disproportionation reaction. All compounds were tested for their ability to inhibit the growth of the malaria parasite Plasmodium falciparum (3D7 and Dd2 strains) and for cytotoxicity against a human embryonic kidney (HEK293) cell line. Moderate antimalarial activity was observed for some of the compounds, with IC50 values ranging from 0.3 to >20 µM; none of the compounds displayed any toxicity against HEK293 at 80 µM.

show abstract

Section: Synthesis Of Osm-based Scaffolds Via Coupling Of Primary Alcohols With Chloro-heterocyclesmentioning

confidence: 99%

“… Synthesis of 8 , 10, and 11 via photoredox-catalyzed methylation (for structure of the iridium catalyst, see Ref. [ 16 ]). …”

Section: Figures Schemes and Tablesmentioning

confidence: 99%

Synthesis of New Triazolopyrazine Antimalarial Compounds

et al. 2021

View full text Add to dashboard Cite

show abstract

“…In their study, they found that the C19 compound they designed fulfilled all the Lipinski rules. They also highlighted that the C19 compound had higher GPCR, ion CM and protease activity compared to nelarabine, and that it had the potential to be a good anti-leukaemic drug [41]. We compared our fludarabine derivatives with fludarabine in terms of their bioactivity performance.…”

Section: Calculation Of Pharmacokinetic Parametersmentioning

confidence: 99%

Identifying highly effective fludarabine-based novel target cancer therapy agents by in silico studies

Yucel,

Azak

2024

j-ebr

View full text Add to dashboard Cite

To develop an alternative drug molecule design to fludarabine which is commonly used in chronic lymphocytic leukemia. Methods: The molecular properties and biological activities of the drug molecules were determined using Molinspiration software. We investigated the biological activity and drug properties of fludarabine by changing the positions of bioisosteres on the molecular structure. Results: In our studies of derivatives of the fludarabine drug molecule, we obtained data by adding different structures to the Y part without changing the X structure (F) of fludarabine. We have used the abbreviation 'M' to refer to the molecules in these experiments. We predict that the M6 derivative of fludarabine will have higher ion channel modulator, kinase and protease activity compared to fludarabine. We predict that the M15 derivative of fludarabine will have higher G-protein coupled receptors, ion channel modulator, kinase, and protease and enzyme inhibition activity compared to fludarabine. In our experiments with fludarabine derivatives, we have experimented by binding different molecules to both the X and Y structures of fludarabine at the same time. We have used the abbreviation 'C' to refer to the molecules in these experiments. In these experiments, we did not achieve higher biological activity than fludarabine. Conclusions:The results suggest that this newly designed M15 derivative of fludarabine molecule may be a better antileukemic drug molecules in the future and may be useful for further drug molecule development research in medical biochemistry, chemistry and pharmacology.

show abstract

Higher Carbon Analogues of 1,4‐Dihydropyridines as Potent TGFβ/Smad Inhibitors

et al. 2019

View full text Add to dashboard Cite

The C to Si and Ge exchange in bioactive compounds has often led to positive changes in the molecular properties, whereby Ge analogues are underrepresented. This is only possible at tetrahedral positions, and it is necessary for the analogue building blocks to withstand the synthetic conditions. Here, we present the synthesis of Si and Ge analogues of a TGF inhibiting 1,4-dihydropyridine, which has a tetrahedral carbon in an important position for its activity. The molecular [a]

show abstract

Multi-targeted anti-leukemic drug design with the incorporation of silicon into Nelarabine: How silicon increases bioactivity

Cited by 9 publications

References 34 publications

Synthesis of New Triazolopyrazine Antimalarial Compounds

Synthesis of New Triazolopyrazine Antimalarial Compounds

Identifying highly effective fludarabine-based novel target cancer therapy agents by in silico studies

Higher Carbon Analogues of 1,4‐Dihydropyridines as Potent TGFβ/Smad Inhibitors

Contact Info

Product

Resources

About