Design, Synthesis, and Evaluation of Octahydropyranopyrrole-Based Inhibitors of Mammalian Ribonucleotide Reductase.

ChemInform ◽  
2006 ◽  
Vol 37 (9) ◽  
Author(s):  
Michael J. Fuertes ◽  
Jaskiran Kaur ◽  
Prasant Deb ◽  
Barry S. Cooperman ◽  
Amos B. III Smith
Keyword(s):  
Ribonucleotide Reductase ◽  
Design Synthesis

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.

Design, synthesis and evaluation of peptide inhibitors ofMycobacterium tuberculosis ribonucleotide reductase

2007 ◽  
Vol 13 (12) ◽  
pp. 822-832 ◽  
Author(s):  
Johanna Nurbo ◽  
Annette K. Roos ◽  
Daniel Muthas ◽  
Erik Wahlström ◽  
Daniel J. Ericsson ◽  
...  
Keyword(s):  
Ribonucleotide Reductase ◽  
Peptide Inhibitors ◽  
Design Synthesis ◽  
Ofmycobacterium Tuberculosis

Design, synthesis, and evaluation of octahydropyranopyrrole-based inhibitors of mammalian ribonucleotide reductase

2005 ◽  
Vol 15 (23) ◽  
pp. 5146-5149 ◽  
Author(s):  
Michael J. Fuertes ◽  
Jaskiran Kaur ◽  
Prasant Deb ◽  
Barry S. Cooperman ◽  
Amos B. Smith
Keyword(s):  
Ribonucleotide Reductase ◽  
Design Synthesis

Self-Assembly of Hydrogels From Elastin-Mimetic Block Copolymers

2002 ◽  
Vol 724 ◽  
Author(s):  
Elizabeth R. Wright ◽  
R. Andrew McMillan ◽  
Alan Cooper ◽  
Robert P. Apkarian ◽  
Vincent P. Conticello
Keyword(s):  
Block Copolymers ◽  
Self Assembly ◽  
Triblock Copolymers ◽  
Variable Temperature ◽  
Inverse Temperature ◽  
Temperature Transition ◽  
Scanning Calorimetry ◽  
Design Synthesis ◽  
Inverse Temperature Transition ◽  
Functional Biomaterials

AbstractTriblock copolymers have traditionally been synthesized with conventional organic components. However, triblock copolymers could be synthesized by the incorporation of two incompatible protein-based polymers. The polypeptides would differ in their hydrophobicity and confer unique physiochemical properties to the resultant materials. One protein-based polymer, based on a sequence of native elastin, that has been utilized in the synthesis of biomaterials is poly (Valine-Proline-Glycine-ValineGlycine) or poly(VPGVG) [1]. This polypeptide has been shown to have an inverse temperature transition that can be adjusted by non-conservative amino acid substitutions in the fourth position [2]. By combining polypeptide blocks with different inverse temperature transition values due to hydrophobicity differences, we expect to produce amphiphilic polypeptides capable of self-assembly into hydrogels. Our research examines the design, synthesis and characterization of elastin-mimetic block copolymers as functional biomaterials. The methods that are used for the characterization include variable temperature 1D and 2D High-Resolution-NMR, cryo-High Resolutions Scanning Electron Microscopy and Differential Scanning Calorimetry.

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