Rank |
Title |
Journal |
Year |
PubWeight™‹?› |
1
|
Synthesis and anti-viral activity of a series of sesquiterpene lactones and analogues in the subgenomic HCV replicon system.
|
Bioorg Med Chem
|
2005
|
2.38
|
2
|
BPR0L075, a novel synthetic indole compound with antimitotic activity in human cancer cells, exerts effective antitumoral activity in vivo.
|
Cancer Res
|
2004
|
1.36
|
3
|
Aurintricarboxylic acid inhibits influenza virus neuraminidase.
|
Antiviral Res
|
2008
|
1.19
|
4
|
Aurora kinase inhibitors in preclinical and clinical testing.
|
Expert Opin Investig Drugs
|
2009
|
1.16
|
5
|
Bortezomib overcomes tumor necrosis factor-related apoptosis-inducing ligand resistance in hepatocellular carcinoma cells in part through the inhibition of the phosphatidylinositol 3-kinase/Akt pathway.
|
J Biol Chem
|
2009
|
1.15
|
6
|
Concise synthesis and structure-activity relationships of combretastatin A-4 analogues, 1-aroylindoles and 3-aroylindoles, as novel classes of potent antitubulin agents.
|
J Med Chem
|
2004
|
1.08
|
7
|
Inhibition of severe acute respiratory syndrome coronavirus replication by niclosamide.
|
Antimicrob Agents Chemother
|
2004
|
1.07
|
8
|
Synthesis and structure-activity relationship of 2-aminobenzophenone derivatives as antimitotic agents.
|
J Med Chem
|
2002
|
1.06
|
9
|
Shear stress inhibits smooth muscle cell-induced inflammatory gene expression in endothelial cells: role of NF-kappaB.
|
Arterioscler Thromb Vasc Biol
|
2005
|
1.01
|
10
|
Survivin counteracts the therapeutic effect of microtubule de-stabilizers by stabilizing tubulin polymers.
|
Mol Cancer
|
2009
|
1.01
|
11
|
Structure-based drug design of a novel family of PPARgamma partial agonists: virtual screening, X-ray crystallography, and in vitro/in vivo biological activities.
|
J Med Chem
|
2006
|
0.98
|
12
|
Aurora kinase inhibitor patents and agents in clinical testing: an update (2009-10).
|
Expert Opin Ther Pat
|
2011
|
0.96
|
13
|
Anti-influenza drug discovery: structure-activity relationship and mechanistic insight into novel angelicin derivatives.
|
J Med Chem
|
2010
|
0.96
|
14
|
Identification of BPR3P0128 as an inhibitor of cap-snatching activities of influenza virus.
|
Antimicrob Agents Chemother
|
2011
|
0.95
|
15
|
Bioassay-guided purification and identification of PPARalpha/gamma agonists from Chlorella sorokiniana.
|
Phytother Res
|
2008
|
0.95
|
16
|
Structure-based drug design of novel Aurora kinase A inhibitors: structural basis for potency and specificity.
|
J Med Chem
|
2009
|
0.95
|
17
|
Aurora kinase A inhibitors: identification, SAR exploration and molecular modeling of 6,7-dihydro-4H-pyrazolo-[1,5-a]pyrrolo[3,4-d]pyrimidine-5,8-dione scaffold.
|
Bioorg Med Chem Lett
|
2008
|
0.91
|
18
|
2-[3-[2-[(2S)-2-Cyano-1-pyrrolidinyl]-2-oxoethylamino]-3-methyl-1-oxobutyl]- 1,2,3,4-tetrahydroisoquinoline: a potent, selective, and orally bioavailable dipeptide-derived inhibitor of dipeptidyl peptidase IV.
|
J Med Chem
|
2006
|
0.90
|
19
|
4- and 5-aroylindoles as novel classes of potent antitubulin agents.
|
J Med Chem
|
2007
|
0.88
|
20
|
Small-molecule EGFR tyrosine kinase inhibitors for the treatment of cancer.
|
Expert Opin Investig Drugs
|
2014
|
0.87
|
21
|
Pyrazole compound BPR1P0034 with potent and selective anti-influenza virus activity.
|
J Biomed Sci
|
2010
|
0.87
|
22
|
Fast-forwarding hit to lead: aurora and epidermal growth factor receptor kinase inhibitor lead identification.
|
J Med Chem
|
2010
|
0.87
|
23
|
5-Amino-2-aroylquinolines as highly potent tubulin polymerization inhibitors.
|
J Med Chem
|
2010
|
0.86
|
24
|
Synthesis and biological evaluation of 1-methyl-2-(3',4',5'-trimethoxybenzoyl)-3-aminoindoles as a new class of antimitotic agents and tubulin inhibitors.
|
J Med Chem
|
2008
|
0.86
|
25
|
Tubulin-destabilizing agent BPR0L075 induces vascular-disruption in human breast cancer mammary fat pad xenografts.
|
PLoS One
|
2012
|
0.86
|
26
|
7-Aroyl-aminoindoline-1-sulfonamides as a novel class of potent antitubulin agents.
|
J Med Chem
|
2006
|
0.86
|
27
|
Discovery of 4-amino and 4-hydroxy-1-aroylindoles as potent tubulin polymerization inhibitors.
|
J Med Chem
|
2008
|
0.86
|
28
|
Synthesis and biological evaluation of 1-(4'-Indolyl and 6'-Quinolinyl) indoles as a new class of potent anticancer agents.
|
Eur J Med Chem
|
2011
|
0.85
|
29
|
Thiopurine analogues inhibit papain-like protease of severe acute respiratory syndrome coronavirus.
|
Biochem Pharmacol
|
2008
|
0.85
|
30
|
Novel indole-based peroxisome proliferator-activated receptor agonists: design, SAR, structural biology, and biological activities.
|
J Med Chem
|
2005
|
0.85
|
31
|
Cancer cells acquire mitotic drug resistance properties through beta I-tubulin mutations and alterations in the expression of beta-tubulin isotypes.
|
PLoS One
|
2010
|
0.85
|
32
|
Isocostunolide, a sesquiterpene lactone, induces mitochondrial membrane depolarization and caspase-dependent apoptosis in human melanoma cells.
|
Cancer Lett
|
2006
|
0.84
|
33
|
Evaluation of metal-conjugated compounds as inhibitors of 3CL protease of SARS-CoV.
|
FEBS Lett
|
2004
|
0.84
|
34
|
Structure-based drug design and structural biology study of novel nonpeptide inhibitors of severe acute respiratory syndrome coronavirus main protease.
|
J Med Chem
|
2006
|
0.84
|
35
|
Synthesis and evaluation of 3-aroylindoles as anticancer agents: metabolite approach.
|
J Med Chem
|
2009
|
0.84
|
36
|
Structural basis for the improved potency of peroxisome proliferator-activated receptor (PPAR) agonists.
|
ChemMedChem
|
2010
|
0.83
|
37
|
Identification, SAR studies, and X-ray co-crystallographic analysis of a novel furanopyrimidine aurora kinase A inhibitor.
|
ChemMedChem
|
2010
|
0.83
|
38
|
Protein kinase inhibitor design by targeting the Asp-Phe-Gly (DFG) motif: the role of the DFG motif in the design of epidermal growth factor receptor inhibitors.
|
J Med Chem
|
2013
|
0.83
|
39
|
Design and synthesis of alpha-ketoamides as cathepsin S inhibitors with potential applications against tumor invasion and angiogenesis.
|
J Med Chem
|
2010
|
0.83
|
40
|
BPR2-D2 targeting viral ribonucleoprotein complex-associated function inhibits oseltamivir-resistant influenza viruses.
|
J Antimicrob Chemother
|
2010
|
0.83
|
41
|
Identification of ligand efficient, fragment-like hits from an HTS library: structure-based virtual screening and docking investigations of 2H- and 3H-pyrazolo tautomers for Aurora kinase A selectivity.
|
J Comput Aided Mol Des
|
2014
|
0.83
|
42
|
Antiangiogenic activities and cisplatin-combined antitumor activities of BPR0L075.
|
Anticancer Res
|
2010
|
0.82
|
43
|
A high-throughput cell-based screening for L858R/T790M mutant epidermal growth factor receptor inhibitors.
|
Anticancer Res
|
2012
|
0.81
|
44
|
Design and synthesis of tetrahydropyridothieno[2,3-d]pyrimidine scaffold based epidermal growth factor receptor (EGFR) kinase inhibitors: the role of side chain chirality and Michael acceptor group for maximal potency.
|
J Med Chem
|
2010
|
0.81
|
45
|
Anti-HSV activity of digitoxin and its possible mechanisms.
|
Antiviral Res
|
2008
|
0.81
|
46
|
Design and structural analysis of novel pharmacophores for potent and selective peroxisome proliferator-activated receptor gamma agonists.
|
J Med Chem
|
2009
|
0.80
|
47
|
Indol-1-yl acetic acids as peroxisome proliferator-activated receptor agonists: design, synthesis, structural biology, and molecular docking studies.
|
J Med Chem
|
2006
|
0.80
|
48
|
Generation of ligand-based pharmacophore model and virtual screening for identification of novel tubulin inhibitors with potent anticancer activity.
|
J Med Chem
|
2009
|
0.80
|
49
|
Advances in Aurora kinase inhibitor patents.
|
Expert Opin Ther Pat
|
2009
|
0.80
|
50
|
Scaffold-hopping strategy: synthesis and biological evaluation of 5,6-fused bicyclic heteroaromatics to identify orally bioavailable anticancer agents.
|
J Med Chem
|
2011
|
0.80
|
51
|
Inhibition of HIV-1 Tat-mediated transcription by a coumarin derivative, BPRHIV001, through the Akt pathway.
|
J Virol
|
2011
|
0.80
|
52
|
BPR1K653, a novel Aurora kinase inhibitor, exhibits potent anti-proliferative activity in MDR1 (P-gp170)-mediated multidrug-resistant cancer cells.
|
PLoS One
|
2011
|
0.80
|
53
|
Aurora kinase inhibitors reveal mechanisms of HURP in nucleation of centrosomal and kinetochore microtubules.
|
Proc Natl Acad Sci U S A
|
2013
|
0.80
|
54
|
Structure-activity relationship studies of 3-aroylindoles as potent antimitotic agents.
|
ChemMedChem
|
2006
|
0.79
|
55
|
Parallel screening of wild-type and drug-resistant targets for anti-resistance neuraminidase inhibitors.
|
PLoS One
|
2013
|
0.79
|
56
|
Structural basis for the structure-activity relationships of peroxisome proliferator-activated receptor agonists.
|
J Med Chem
|
2006
|
0.79
|
57
|
A novel peroxisome proliferator-activated receptor alpha/gamma agonist, BPR1H0101, inhibits topoisomerase II catalytic activity in human cancer cells.
|
Anticancer Drugs
|
2008
|
0.79
|
58
|
Synthesis and structure-activity relationships of 1-benzyl-4,5,6-trimethoxyindoles as a novel class of potent antimitotic agents.
|
ChemMedChem
|
2009
|
0.78
|
59
|
CDKN1A-mediated responsiveness of MLL-AF4-positive acute lymphoblastic leukemia to Aurora kinase-A inhibitors.
|
Int J Cancer
|
2014
|
0.78
|
60
|
Synthesis and structure-activity relationships of 3-aminobenzophenones as antimitotic agents.
|
J Med Chem
|
2004
|
0.78
|
61
|
Pronounced induction of endoplasmic reticulum stress and tumor suppression by surfactant-free poly(lactic-co-glycolic acid) nanoparticles via modulation of the PI3K signaling pathway.
|
Int J Nanomedicine
|
2013
|
0.78
|
62
|
Antiviral drug discovery against SARS-CoV.
|
Curr Med Chem
|
2006
|
0.78
|
63
|
Facile identification of dual FLT3-Aurora A inhibitors: a computer-guided drug design approach.
|
ChemMedChem
|
2014
|
0.78
|
64
|
A cell-based high-throughput screen for epidermal growth factor receptor pathway inhibitors.
|
Anal Biochem
|
2008
|
0.78
|
65
|
A novel bis-benzylidenecyclopentanone derivative, BPR0Y007, inducing a rapid caspase activation involving upregulation of Fas (CD95/APO-1) and wild-type p53 in human oral epidermoid carcinoma cells.
|
Biochem Pharmacol
|
2004
|
0.78
|
66
|
A novel aurora-A inhibitor, BPR1K0609S1, sensitizes colorectal tumor cells to 5-fluorofracil (5-FU) treatment.
|
Int J Biol Sci
|
2013
|
0.77
|
67
|
An antimitotic and antivascular agent BPR0L075 overcomes multidrug resistance and induces mitotic catastrophe in paclitaxel-resistant ovarian cancer cells.
|
PLoS One
|
2013
|
0.77
|
68
|
3D-QSAR-assisted drug design: identification of a potent quinazoline-based Aurora kinase inhibitor.
|
ChemMedChem
|
2012
|
0.77
|
69
|
3-[2-((2S)-2-cyano-pyrrolidin-1-yl)-2-oxo-ethylamino]-3-methyl-butyramide analogues as selective DPP-IV inhibitors for the treatment of type-II diabetes.
|
Bioorg Med Chem Lett
|
2006
|
0.77
|
70
|
Dual inhibition of topoisomerase I and tubulin polymerization by BPR0Y007, a novel cytotoxic agent.
|
Biochem Pharmacol
|
2003
|
0.77
|
71
|
Optimization of ligand and lipophilic efficiency to identify an in vivo active furano-pyrimidine Aurora kinase inhibitor.
|
J Med Chem
|
2013
|
0.77
|
72
|
Discovery of a novel family of SARS-CoV protease inhibitors by virtual screening and 3D-QSAR studies.
|
J Med Chem
|
2006
|
0.76
|
73
|
Anti-influenza drug discovery: identification of an orally bioavailable quinoline derivative through activity- and property-guided lead optimization.
|
ChemMedChem
|
2012
|
0.76
|
74
|
First total syntheses of (+/-)-annuionone B and (+/-)-tanarifuranonol.
|
Org Lett
|
2008
|
0.75
|
75
|
Development and validation of a liquid chromatography-tandem mass spectrometry for the determination of BPR0L075, a novel antimicrotuble agent, in rat plasma: application to a pharmacokinetic study.
|
J Chromatogr B Analyt Technol Biomed Life Sci
|
2006
|
0.75
|
76
|
Synthesis and structure-activity relationships of 2-amino-1-aroylnaphthalene and 2-hydroxy-1-aroylnaphthalenes as potent antitubulin agents.
|
J Med Chem
|
2008
|
0.75
|
77
|
Biotransformation of 6-methoxy-3-(3',4',5'-trimethoxy-benzoyl)-1H-indole (BPR0L075), a novel antimicrotubule agent, by mouse, rat, dog, and human liver microsomes.
|
Drug Metab Dispos
|
2007
|
0.75
|
78
|
2-amino-3,4,5-trimethoxybenzophenones as potent tubulin polymerization inhibitors.
|
ChemMedChem
|
2011
|
0.75
|
79
|
Discovery of a Furanopyrimidine-Based Epidermal Growth Factor Receptor Inhibitor (DBPR112) as a Clinical Candidate for the Treatment of Non-Small Cell Lung Cancer.
|
J Med Chem
|
2019
|
0.75
|
80
|
Substituted pyrrolidine-2,4-dicarboxylic acid amides as potent dipeptidyl peptidase IV inhibitors.
|
Bioorg Med Chem Lett
|
2006
|
0.75
|