Ribonucleotide reductase (RR), an established cancer target, is usually inhibited by antimetabolites, which display multiple cross-reactive effects. Recently, we discovered a naphthyl salicyl acyl hydrazone-based inhibitor (<b>NSAH</b> or <i>E</i>-<b>3a</b>) of human RR (hRR) binding at the catalytic site (C-site) and inhibiting hRR reversibly. We herein report the synthesis and biochemical characterization of 25 distinct analogs. We designed each analog through docking to the C-site of hRR based on our 2.7 Å X-ray crystal structure (PDB ID: 5TUS). Broad tolerance to minor structural variations preserving inhibitory potency is observed. <i>E</i>-<b>3f</b> (82% yield) displayed an <i>in vitro</i> IC<sub>50</sub> of 5.3 ± 1.8 μM against hRR, ...
Sufficient pools of deoxyribonucleotide triphophates (dNTPs) are essential for the high fidelity rep...
Cancer is continuing to be a major health issue and despite the recent improvements in the chemother...
Ribonucleotide reductase (RNR) is a key enzyme in the de novo biosynthesis and homeostatic maintenan...
Ribonucleotide reductase (RR) catalyses the rate-limiting step of dNTP synthesis, establishing it as...
Ribonucleotide reductase (RR) catalyzes the rate-limiting step of dNTP synthesis and is an establish...
Ribonucleotide reductase (RR) is a key enzyme that converts ribonucleotides (NDP) to deoxyribonucleo...
Ribonucleotide reductase (RR) is an essential multi-subunit enzyme found in all living organisms; it...
Human ribonucleotide reductase (hRR) is the key enzyme involved in de novo dNTP synthesis and thus r...
Ribonucleotide reductase (RR) is a crucial enzyme in de novo DNA synthesis, where it catalyses the r...
Human ribonucleotide reductase (hRR) is the key enzyme involved in de novo dNTP synthesis and thus r...
© 2020 Annual Reviews Inc.. All rights reserved. Ribonucleotide reductases (RNRs) catalyze the de no...
We synthesized a series of serum-stable covalently linked drugs derived from 3'-C-methyladenosine (...
Screening a library of 5,292 hydrazone/hydrazine compounds for inhibition of HIV reverse transcripta...
Mammalian ribonucleotide reductase, a chemotherapeutic target, has two subunits, mR1 and mR2, and is...
We synthesized a series of serum-stable covalently linked drugs derived from 3′-C-methyladenosine (3...
Sufficient pools of deoxyribonucleotide triphophates (dNTPs) are essential for the high fidelity rep...
Cancer is continuing to be a major health issue and despite the recent improvements in the chemother...
Ribonucleotide reductase (RNR) is a key enzyme in the de novo biosynthesis and homeostatic maintenan...
Ribonucleotide reductase (RR) catalyses the rate-limiting step of dNTP synthesis, establishing it as...
Ribonucleotide reductase (RR) catalyzes the rate-limiting step of dNTP synthesis and is an establish...
Ribonucleotide reductase (RR) is a key enzyme that converts ribonucleotides (NDP) to deoxyribonucleo...
Ribonucleotide reductase (RR) is an essential multi-subunit enzyme found in all living organisms; it...
Human ribonucleotide reductase (hRR) is the key enzyme involved in de novo dNTP synthesis and thus r...
Ribonucleotide reductase (RR) is a crucial enzyme in de novo DNA synthesis, where it catalyses the r...
Human ribonucleotide reductase (hRR) is the key enzyme involved in de novo dNTP synthesis and thus r...
© 2020 Annual Reviews Inc.. All rights reserved. Ribonucleotide reductases (RNRs) catalyze the de no...
We synthesized a series of serum-stable covalently linked drugs derived from 3'-C-methyladenosine (...
Screening a library of 5,292 hydrazone/hydrazine compounds for inhibition of HIV reverse transcripta...
Mammalian ribonucleotide reductase, a chemotherapeutic target, has two subunits, mR1 and mR2, and is...
We synthesized a series of serum-stable covalently linked drugs derived from 3′-C-methyladenosine (3...
Sufficient pools of deoxyribonucleotide triphophates (dNTPs) are essential for the high fidelity rep...
Cancer is continuing to be a major health issue and despite the recent improvements in the chemother...
Ribonucleotide reductase (RNR) is a key enzyme in the de novo biosynthesis and homeostatic maintenan...