scholarly journals Preparation of Phosphonic Acid Analogues of Proline and Proline Analogues and Their Biological Evaluation as δ1-Pyrroline-5-carboxylate Reductase Inhibitors

ACS Omega ◽  
2018 ◽  
Vol 3 (4) ◽  
pp. 4441-4452 ◽  
Author(s):  
Renzhe Qian ◽  
Thomas Kalina ◽  
Jeannie Horak ◽  
Samuele Giberti ◽  
Giuseppe Forlani ◽  
...  
Keyword(s):  
Phosphonic Acid ◽  
Biological Evaluation ◽  
Reductase Inhibitors ◽  
Carboxylate Reductase

Heterocyclichydrazonesasribonucleotide reductase inhibitors: Synthesis and biological evaluation

1997 ◽  
Vol 30 (3) ◽  
pp. 260
Author(s):  
G. Pürstinger ◽  
J. Easmon ◽  
G. Heinisch ◽  
H. Grunicke ◽  
J. Hofmann
Keyword(s):  
Biological Evaluation ◽  
Reductase Inhibitors ◽  
Synthesis And Biological Evaluation

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.

scholarly journals Structure-Based Virtual Screening and Biological Evaluation ofMycobacterium tuberculosisAdenosine 5′-Phosphosulfate Reductase Inhibitors

2008 ◽  
Vol 51 (21) ◽  
pp. 6627-6630 ◽  
Author(s):  
Sandro Cosconati ◽  
Jiyoung A. Hong ◽  
Ettore Novellino ◽  
Kate S. Carroll ◽  
David S. Goodsell ◽  
...  
Keyword(s):  
Virtual Screening ◽  
Biological Evaluation ◽  
Reductase Inhibitors
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