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diaminoquinazoline

 
National Institutes of Health

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2019
2019
Diaminoquinazoline MMV675968 from Pathogen Box inhibits Acinetobacter baumannii growth through targeting of dihydrofolate reductase
Antibiotic resistance in Acinetobacter baumannii is a major global health threat. New drugs with novel chemical structures are… Expand
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2018
2018
Activation of 2,4-Diaminoquinazoline in Mycobacterium tuberculosis by Rv3161c, a Putative Dioxygenase
The diaminoquinazoline series has good potency against Mycobacterium tuberculosis Resistant isolates have mutations in Rv3161c, a… Expand
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2018
2018
Development of a Photo-Cross-Linkable Diaminoquinazoline Inhibitor for Target Identification in Plasmodium falciparum.
Diaminoquinazolines represent a privileged scaffold for antimalarial discovery, including use as putative Plasmodium histone… Expand
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2017
2017
Histone lysine methyltransferase structure activity relationships that allow for segregation of G9a inhibition and anti-Plasmodium activity† †The authors declare no competing interests. ‡ ‡Electronic…
Plasmodium falciparum HKMTs (PfHKMTs) play a key role in controlling Plasmodium gene expression and represent exciting new anti… Expand
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2015
2015
Rational targeting of active-site tyrosine residues using sulfonyl fluoride probes.
This work describes the first rational targeting of tyrosine residues in a protein binding site by small-molecule covalent probes… Expand
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2014
2014
Structure-based design of new dihydrofolate reductase antibacterial agents: 7-(benzimidazol-1-yl)-2,4-diaminoquinazolines.
A new series of dihydrofolate reductase (DHFR) inhibitors, the 7-(benzimidazol-1-yl)-2,4-diaminoquinazolines, were designed and… Expand
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2014
2014
Development of diaminoquinazoline histone lysine methyltransferase inhibitors as potent blood-stage antimalarial compounds.
Modulating epigenetic mechanisms in malarial parasites is an emerging avenue for the discovery of novel antimalarial drugs… Expand
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2012
2012
Design, synthesis, and biological evaluation of new diaminoquinazolines as β-catenin/Tcf4 pathway inhibitors.
More than 50 new diaminoquinazoline derivatives have been synthesized and evaluated in a colon carcinoma cell growth inhibition… Expand
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1998
1998
Computation of affinity and selectivity: Binding of 2,4-diaminopteridine and 2,4-diaminoquinazoline inhibitors to dihydrofolate reductases
Binding energy calculations for complexes of mutant and wild-type human dihydrofolate reductases with 2,4-diaminopteridine and 2… Expand
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1977
1977
Potent inhibitory activity of trimethoxyquine (tmq), "nonclassical" 2,4, diaminoquinazoline, on mammalian dna synthesis. Abstr.
 
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