1
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Preclinical testing of the nitroimidazopyran PA-824 for activity against Mycobacterium tuberculosis in a series of in vitro and in vivo models.
|
Antimicrob Agents Chemother
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2005
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3.16
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2
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High-throughput screening for inhibitors of Mycobacterium tuberculosis H37Rv.
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Tuberculosis (Edinb)
|
2009
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2.58
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3
|
Synthesis and antimycobacterial activity of pyrazine and quinoxaline derivatives.
|
J Med Chem
|
2002
|
2.16
|
4
|
Antituberculosis activity of the molecular libraries screening center network library.
|
Tuberculosis (Edinb)
|
2009
|
1.94
|
5
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EthA, a common activator of thiocarbamide-containing drugs acting on different mycobacterial targets.
|
Antimicrob Agents Chemother
|
2007
|
1.58
|
6
|
A novel sulindac derivative that does not inhibit cyclooxygenases but potently inhibits colon tumor cell growth and induces apoptosis with antitumor activity.
|
Cancer Prev Res (Phila)
|
2009
|
1.51
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7
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Thiacetazone, an antitubercular drug that inhibits cyclopropanation of cell wall mycolic acids in mycobacteria.
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PLoS One
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2007
|
1.41
|
8
|
2-Alkoxycarbonylaminopyridines: inhibitors of Mycobacterium tuberculosis FtsZ.
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J Antimicrob Chemother
|
2002
|
1.39
|
9
|
The use of microarray analysis to determine the gene expression profiles of Mycobacterium tuberculosis in response to anti-bacterial compounds.
|
Tuberculosis (Edinb)
|
2004
|
1.33
|
10
|
Sulindac sulfide selectively inhibits growth and induces apoptosis of human breast tumor cells by phosphodiesterase 5 inhibition, elevation of cyclic GMP, and activation of protein kinase G.
|
Mol Cancer Ther
|
2009
|
1.31
|
11
|
Structure of Mycobacterium tuberculosis FtsZ reveals unexpected, G protein-like conformational switches.
|
J Mol Biol
|
2004
|
1.10
|
12
|
Bayesian models leveraging bioactivity and cytotoxicity information for drug discovery.
|
Chem Biol
|
2013
|
1.10
|
13
|
Enhancing hit identification in Mycobacterium tuberculosis drug discovery using validated dual-event Bayesian models.
|
PLoS One
|
2013
|
1.01
|
14
|
Combining computational methods for hit to lead optimization in Mycobacterium tuberculosis drug discovery.
|
Pharm Res
|
2013
|
0.99
|
15
|
Mycolic acid methyltransferase, MmaA4, is necessary for thiacetazone susceptibility in Mycobacterium tuberculosis.
|
Mol Microbiol
|
2009
|
0.99
|
16
|
Fractionation, structural studies, and immunological characterization of the semi-synthetic Quillaja saponins derivative GPI-0100.
|
Vaccine
|
2003
|
0.99
|
17
|
Synthesis and biological evaluation of trehalose analogs as potential inhibitors of mycobacterial cell wall biosynthesis.
|
Carbohydr Res
|
2002
|
0.97
|
18
|
Synthesis and preliminary in vitro evaluation of antimycobacterial activity of new pyrrolo[1,2-a] quinoxaline-carboxylic acid hydrazide derivatives.
|
J Enzyme Inhib Med Chem
|
2004
|
0.95
|
19
|
Novel pyridopyrazine and pyrimidothiazine derivatives as FtsZ inhibitors.
|
Bioorg Med Chem
|
2011
|
0.95
|
20
|
Symmetrical and unsymmetrical analogues of isoxyl; active agents against Mycobacterium tuberculosis.
|
Bioorg Med Chem Lett
|
2006
|
0.90
|
21
|
Identification of novel Mt-Guab2 inhibitor series active against M. tuberculosis.
|
PLoS One
|
2012
|
0.89
|
22
|
Identification of novel diphenyl urea inhibitors of Mt-GuaB2 active against Mycobacterium tuberculosis.
|
Microbiology
|
2010
|
0.89
|
23
|
Are bigger data sets better for machine learning? Fusing single-point and dual-event dose response data for Mycobacterium tuberculosis.
|
J Chem Inf Model
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2014
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0.88
|
24
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Looking back to the future: predicting in vivo efficacy of small molecules versus Mycobacterium tuberculosis.
|
J Chem Inf Model
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2014
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0.87
|
25
|
Silibinin inhibits Wnt/β-catenin signaling by suppressing Wnt co-receptor LRP6 expression in human prostate and breast cancer cells.
|
Cell Signal
|
2012
|
0.87
|
26
|
Fusing dual-event data sets for Mycobacterium tuberculosis machine learning models and their evaluation.
|
J Chem Inf Model
|
2013
|
0.85
|
27
|
A novel quinoline derivative that inhibits mycobacterial FtsZ.
|
Tuberculosis (Edinb)
|
2013
|
0.85
|
28
|
Antimycobacterial agents. 1. Thio analogues of purine.
|
J Med Chem
|
2004
|
0.85
|
29
|
Expression, purification and characterisation of soluble GlfT and the identification of a novel galactofuranosyltransferase Rv3782 involved in priming GlfT-mediated galactan polymerisation in Mycobacterium tuberculosis.
|
Protein Expr Purif
|
2007
|
0.84
|
30
|
Disaccharide analogs as probes for glycosyltransferases in Mycobacterium tuberculosis.
|
Bioorg Med Chem
|
2007
|
0.84
|
31
|
EmbR2, a structural homologue of EmbR, inhibits the Mycobacterium tuberculosis kinase/substrate pair PknH/EmbR.
|
Biochem J
|
2008
|
0.84
|
32
|
Synthesis of an arabinofuranosyl disaccharide photoaffinity probe for arabinosyltransferase activity in Mycobacterium tuberculosis.
|
Bioorg Med Chem Lett
|
2002
|
0.84
|
33
|
A novel sulindac derivative lacking cyclooxygenase-inhibitory activities suppresses carcinogenesis in the transgenic adenocarcinoma of mouse prostate model.
|
Cancer Prev Res (Phila)
|
2010
|
0.80
|
34
|
Studies on n-octyl-5-(alpha-D-arabinofuranosyl)-beta-D-galactofuranosides for mycobacterial glycosyltransferase activity.
|
Bioorg Med Chem
|
2002
|
0.79
|
35
|
Parallel solution-phase synthesis of an adenosine antibiotic analog library.
|
ACS Comb Sci
|
2013
|
0.79
|
36
|
Degradation of Quillaja saponaria Molina saponins: loss of the protective effects of a herpes simplex virus 1 subunit vaccine.
|
Int Immunopharmacol
|
2002
|
0.78
|
37
|
Binding mode analysis of 2,4-diamino-5-methyl-5-deaza-6-substituted pteridines with Mycobacterium tuberculosis and human dihydrofolate reductases.
|
J Biomol Struct Dyn
|
2008
|
0.78
|
38
|
Synthesis of novel peptidyl adenosine antibiotic analogs.
|
Nucleosides Nucleotides Nucleic Acids
|
2014
|
0.77
|
39
|
Parallel solution-phase synthesis and general biological activity of a uridine antibiotic analog library.
|
ACS Comb Sci
|
2014
|
0.77
|
40
|
Synthesis of mannopyranose disaccharides as photoaffinity probes for mannosyltransferases in Mycobacterium tuberculosis.
|
Carbohydr Res
|
2004
|
0.77
|
41
|
6-Oxo and 6-thio purine analogs as antimycobacterial agents.
|
Bioorg Med Chem
|
2013
|
0.77
|
42
|
5-Benzothiazole substituted pyrimidine derivatives as HCV replication (replicase) inhibitors.
|
Bioorg Med Chem Lett
|
2012
|
0.77
|
43
|
Synthesis of symmetrical C- and pseudo-symmetrical O-linked disaccharide analogs for arabinosyltransferase inhibitory activity in Mycobacterium tuberculosis.
|
Bioorg Med Chem Lett
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2007
|
0.76
|
44
|
Solution-phase parallel synthesis of acyclic nucleoside libraries of purine, pyrimidine, and triazole acetamides.
|
ACS Comb Sci
|
2014
|
0.75
|
45
|
Synthesis of deoxygenated alpha(1-->5)-linked arabinofuranose disaccharides as substrates and inhibitors of arabinosyltransferases of Mycobacterium tuberculosis.
|
Bioorg Med Chem
|
2008
|
0.75
|
46
|
Synthesis and SAR of pyridothiazole substituted pyrimidine derived HCV replication inhibitors.
|
Bioorg Med Chem Lett
|
2012
|
0.75
|
47
|
Synthesis and SAR of geminal substitutions at the C5' carbosugar position of pyrimidine-derived HCV inhibitors.
|
Bioorg Med Chem Lett
|
2012
|
0.75
|
48
|
Synthesis and general biological activity of a small adenosine-5'-(carboxamide and sulfanilamide) library.
|
Nucleosides Nucleotides Nucleic Acids
|
2014
|
0.75
|
49
|
Novel substituted pyrimidines as HCV replication (replicase) inhibitors.
|
Bioorg Med Chem Lett
|
2011
|
0.75
|
50
|
Pyridofuran substituted pyrimidine derivatives as HCV replication (replicase) inhibitors.
|
Bioorg Med Chem Lett
|
2012
|
0.75
|