Novel diazine derived hydrazones as potential ribonucleotide reductase inhibitors

1995 ◽  
Vol 121 (S1) ◽  
pp. S38-S38
Author(s):  
J. Easmon ◽  
H. Frunicke ◽  
G. Heinisch ◽  
J. Hofmann ◽  
G. Pürstinger
Keyword(s):  
Ribonucleotide Reductase ◽  
Reductase Inhibitors ◽  
Ribonucleotide Reductase Inhibitors

scholarly journals Ribonucleotide reductase inhibitors suppress SAMHD 1 ara‐ CTP ase activity enhancing cytarabine efficacy

2020 ◽  
Vol 12 (3) ◽  
Author(s):  
Sean G Rudd ◽  
Nikolaos Tsesmetzis ◽  
Kumar Sanjiv ◽  
Cynthia BJ Paulin ◽  
Lakshmi Sandhow ◽  
...  
Keyword(s):  
Ribonucleotide Reductase ◽  
Reductase Inhibitors ◽  
Ribonucleotide Reductase Inhibitors

Design, Synthesis and biological evaluation of diazeno-thiazole derivatives as ribonucleotide reductase inhibitors

2017 ◽  
Vol 4 (2) ◽  
pp. 20-24 ◽  
Author(s):  
Mohd Usman Mohd Siddique ◽  
Surender Singh Jadav ◽  
Geraldine Graser ◽  
Philipp Saiko ◽  
Thomas Szekeres ◽  
...  
Keyword(s):  
Dna Synthesis ◽  
Ribonucleotide Reductase ◽  
Biological Evaluation ◽  
Thiazole Derivatives ◽  
Design Synthesis ◽  
Reductase Inhibitors ◽  
Good Target ◽  
Cell Synthesis ◽  
Ribonucleotide Reductase Inhibitors ◽  
Sar Study

Ribonucleotide reductase(RNR) is a metalloenzyme that catalyses the rate limiting step in DNA synthesis and repair. It causes the reduction of ribonucleotide to 2’-deoxyribonuclotides which are used as precursors for DNA synthesis, thus offering a good target for inhibition of cell synthesis. Experimental results have been proven that RNR inhibitors can be used as antiviral, anticancer or antibacterial agents. Here we report the synthesis of a novel class of diazeno-thiazole derivatives as potent RNR inhibitors. A series of forty molecules were synthesized and evaluated for their RNR inhibitory properties. All compounds were found to be good inhibitors of the RNR. Compound 3iwas found to be most active showing an IC50 value of 0.8 µm. The established SAR study indicated the presence of a polar bridge with an adjacent flexible aromatic ringprerequisite for RNR inhibitory activity. Moreover, compounds having an additional 4-chloro phenyl ring were found to be most potent.

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