Synthesis and Biological Activity of a Series of Methylene-Expanded Oxetanocin Nucleoside Analogues

2002 ◽  
Vol 133 (4) ◽  
pp. 499-520 ◽  
Author(s):  
Michael E. Jung ◽  
Akemi Toyota ◽  
Erik de Clercq ◽  
Jan Balzarini
Molecules ◽  
2018 ◽  
Vol 23 (8) ◽  
pp. 2017 ◽  
Author(s):  
Roman Komor ◽  
Gabriela Pastuch-Gawolek ◽  
Ewelina Krol ◽  
Wieslaw Szeja

Herein we present the methodology for obtaining glycosyltransferase inhibitors, analogues of natural enzyme substrates of donor-type: UDP-glucose and UDP-galactose. The synthesis concerned glycoconjugates, nucleoside analogues containing an acyclic ribose mimetic linked to a uracil moiety in their structure. The biological activity of the synthesised compounds was determined on the basis of their ability to inhibit the model enzyme action of β-1,4-galactosyltransferase from bovine milk. The obtained results allowed to expand and supplement the existing library of synthetic compounds that are able to regulate the biological activity of enzymes from the GT class.


Molecules ◽  
2019 ◽  
Vol 24 (19) ◽  
pp. 3433 ◽  
Author(s):  
Anastasia Khandazhinskaya ◽  
Elena Matyugina ◽  
Pavel Solyev ◽  
Maggie Wilkinson ◽  
Karen Buckheit ◽  
...  

Carbocyclic nucleosides have long played a role in antiviral, antiparasitic, and antibacterial therapies. Recent results from our laboratories from two structurally related scaffolds have shown promising activity against both Mycobacterium tuberculosis and several parasitic strains. As a result, a small structure activity relationship study was designed to further probe their activity and potential. Their synthesis and the results of the subsequent biological activity are reported herein.


ChemInform ◽  
2010 ◽  
Vol 33 (32) ◽  
pp. no-no
Author(s):  
Michael E. Jung ◽  
Akemi Toyota ◽  
Erik de Clercq ◽  
Jan Balzarini

ARKIVOC ◽  
2014 ◽  
Vol 2014 (4) ◽  
pp. 170-182 ◽  
Author(s):  
P. Venkat Reddy ◽  
Mohammad Saquib ◽  
Nripendra N. Mishra ◽  
Praveen K. Shukla ◽  
Arun K. Shaw

2016 ◽  
Vol 13 (3) ◽  
pp. 531-546
Author(s):  
Thanaa Al-Mouamin ◽  
◽  
Suror Mahdi ◽  
Omar Mohammed ◽  
Yasmeen Muhamad ◽  
...  

ChemInform ◽  
2012 ◽  
Vol 43 (20) ◽  
pp. no-no
Author(s):  
Oleksandr S. Kanishchev ◽  
Ganna P. Gudz ◽  
Yuriy G. Shermolovich ◽  
Nadezhda V. Nesterova ◽  
Svetlana D. Zagorodnya ◽  
...  

1994 ◽  
Vol 1 (1) ◽  
pp. 65-72 ◽  
Author(s):  
E. Lukevics ◽  
L. Ignatovich ◽  
N. Shilina ◽  
A. Kemme ◽  
N. Sjakste

Direct lithiation of 1-(2-tetrahydrofuryl)-5-fluorouracil (Ftorafur) has been investigated. The treatment of ftorafur with lithium diisopropylamide (LDA)at –70℃ in ether-hexane, followed by the reaction with various electrophiles afforded the corresponding 6-substituted silicon, germanium and tin derivatives of ftorafur. The results of biological investigation indicate the ability of germanium–modified nucleoside analogues to interfere with transcription and replication processes.


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