PubRank

Federico Da Settimo

Author PubWeight™ 42.63‹?›

Top papers

Rank Title Journal Year PubWeight™‹?›
1 Novel pyrazolopyrimidine derivatives as tyrosine kinase inhibitors with antitumoral activity in vitro and in vivo in papillary dedifferentiated thyroid cancer. J Clin Endocrinol Metab 2010 1.68
2 Pyrido[1,2-a]pyrimidin-4-one derivatives as a novel class of selective aldose reductase inhibitors exhibiting antioxidant activity. J Med Chem 2007 1.06
3 Sampling protein motion and solvent effect during ligand binding. Proc Natl Acad Sci U S A 2012 1.04
4 Inhibition of adenosine deaminase attenuates inflammation in experimental colitis. J Pharmacol Exp Ther 2007 1.01
5 Adenosine deaminase in the modulation of immune system and its potential as a novel target for treatment of inflammatory disorders. Curr Drug Targets 2012 1.01
6 The blockade of adenosine deaminase ameliorates chronic experimental colitis through the recruitment of adenosine A2A and A3 receptors. J Pharmacol Exp Ther 2010 0.93
7 N,N-dialkyl-2-phenylindol-3-ylglyoxylamides. A new class of potent and selective ligands at the peripheral benzodiazepine receptor. J Med Chem 2004 0.90
8 Progresses in the pursuit of aldose reductase inhibitors: the structure-based lead optimization step. Eur J Med Chem 2012 0.90
9 Benzofuroxane derivatives as multi-effective agents for the treatment of cardiovascular diabetic complications. Synthesis, functional evaluation, and molecular modeling studies. J Med Chem 2012 0.88
10 Novel N2-substituted pyrazolo[3,4-d]pyrimidine adenosine A3 receptor antagonists: inhibition of A3-mediated human glioblastoma cell proliferation. J Med Chem 2010 0.87
11 Identification of 5-arylidene-4-thiazolidinone derivatives endowed with dual activity as aldose reductase inhibitors and antioxidant agents for the treatment of diabetic complications. Eur J Med Chem 2011 0.87
12 Synthesis and biological evaluation of 4-phenylquinazoline-2-carboxamides designed as a novel class of potent ligands of the translocator protein. J Med Chem 2012 0.87
13 Computational studies of epidermal growth factor receptor: docking reliability, three-dimensional quantitative structure-activity relationship analysis, and virtual screening studies. J Med Chem 2009 0.86
14 Pursuing aldose reductase inhibitors through in situ cross-docking and similarity-based virtual screening. J Med Chem 2009 0.85
15 Genetic analysis of dTSPO, an outer mitochondrial membrane protein, reveals its functions in apoptosis, longevity, and Ab42-induced neurodegeneration. Aging Cell 2014 0.84
16 Exploiting the pyrazolo[3,4-d]pyrimidin-4-one ring system as a useful template to obtain potent adenosine deaminase inhibitors. J Med Chem 2009 0.84
17 Tricyclic sulfonamides incorporating benzothiopyrano[4,3-c]pyrazole and pyridothiopyrano[4,3-c]pyrazole effectively inhibit α- and β-carbonic anhydrase: X-ray crystallography and solution investigations on 15 isoforms. J Med Chem 2012 0.83
18 Novel irreversible fluorescent probes targeting the 18 kDa translocator protein: synthesis and biological characterization. J Med Chem 2010 0.83
19 CLM3, a multitarget tyrosine kinase inhibitor with antiangiogenic properties, is active against primary anaplastic thyroid cancer in vitro and in vivo. J Clin Endocrinol Metab 2014 0.83
20 Structural requirements to obtain highly potent and selective 18 kDa Translocator Protein (TSPO) Ligands. Curr Top Med Chem 2011 0.82
21 Arylsulfonamide inhibitors of aggrecanases as potential therapeutic agents for osteoarthritis: synthesis and biological evaluation. Eur J Med Chem 2013 0.82
22 Synthesis and biological evaluation in U87MG glioma cells of (ethynylthiophene)sulfonamido-based hydroxamates as matrix metalloproteinase inhibitors. Eur J Med Chem 2011 0.82
23 CLM94, a novel cyclic amide with anti-VEGFR-2 and antiangiogenic properties, is active against primary anaplastic thyroid cancer in vitro and in vivo. J Clin Endocrinol Metab 2012 0.82
24 Synthesis and evaluation of translocator 18 kDa protein (TSPO) positron emission tomography (PET) radioligands with low binding sensitivity to human single nucleotide polymorphism rs6971. ACS Chem Neurosci 2014 0.81
25 Acetic acid aldose reductase inhibitors bearing a five-membered heterocyclic core with potent topical activity in a visual impairment rat model. J Med Chem 2008 0.80
26 New fluorescent 2-phenylindolglyoxylamide derivatives as probes targeting the peripheral-type benzodiazepine receptor: design, synthesis, and biological evaluation. J Med Chem 2007 0.80
27 3-aryl-[1,2,4]triazino[4,3-a]benzimidazol-4(10H)-one: a novel template for the design of highly selective A₂B adenosine receptor antagonists. J Med Chem 2012 0.80
28 Anxiolytic properties of a 2-phenylindolglyoxylamide TSPO ligand: Stimulation of in vitro neurosteroid production affecting GABAA receptor activity. Psychoneuroendocrinology 2010 0.80
29 2-(Benzimidazol-2-yl)quinoxalines: a novel class of selective antagonists at human A(1) and A(3) adenosine receptors designed by 3D database searching. J Med Chem 2005 0.80
30 Derivatives of 4-amino-6-hydroxy-2-mercaptopyrimidine as novel, potent, and selective A3 adenosine receptor antagonists. J Med Chem 2008 0.79
31 PIGA (N,N-Di-n-butyl-5-chloro-2-(4-chlorophenyl)indol-3-ylglyoxylamide), a new mitochondrial benzodiazepine-receptor ligand, induces apoptosis in C6 glioma cells. Chembiochem 2005 0.79
32 Benzothiopyranoindole-based antiproliferative agents: synthesis, cytotoxicity, nucleic acids interaction, and topoisomerases inhibition properties. J Med Chem 2009 0.79
33 Dialkylaminoalkylindolonaphthyridines as potential antitumour agents: synthesis, cytotoxicity and DNA binding properties. Eur J Med Chem 2002 0.79
34 Synthesis and biological evaluation of 2'-oxo-2,3-dihydro-3'H- spiro[chromene-4,5'-[1,3]oxazolidin]-3'yl]acetic acid derivatives as aldose reductase inhibitors. Arch Pharm (Weinheim) 2011 0.79
35 Structure-based optimization of tyrosine kinase inhibitor CLM3. Design, synthesis, functional evaluation, and molecular modeling studies. J Med Chem 2014 0.78
36 TSPO ligand residence time influences human glioblastoma multiforme cell death/life balance. Apoptosis 2015 0.78
37 Medicinal chemistry of indolylglyoxylamide GABAA/BzR high affinity ligands: identification of novel anxiolytic/non sedative agents. Curr Top Med Chem 2012 0.78
38 Tertiary amides with a five-membered heteroaromatic ring as new probes for the translocator protein. Eur J Med Chem 2011 0.78
39 Non-nucleoside inhibitors of human adenosine kinase: synthesis, molecular modeling, and biological studies. J Med Chem 2011 0.78
40 Evaluation of novel N1-methyl-2-phenylindol-3-ylglyoxylamides as a new chemotype of 18 kDa translocator protein-selective ligand suitable for the development of positron emission tomography radioligands. J Med Chem 2010 0.78
41 p53 functional inhibitors behaving like pifithrin-β counteract the Alzheimer peptide non-β-amyloid component effects in human SH-SY5Y cells. ACS Chem Neurosci 2014 0.77
42 A3 receptor ligands: past, present and future trends. Curr Top Med Chem 2010 0.77
43 Derivatives of benzimidazol-2-ylquinoline and benzimidazol-2-ylisoquinoline as selective A1 adenosine receptor antagonists with stimulant activity on human colon motility. ChemMedChem 2011 0.77
44 Revisiting a receptor-based pharmacophore hypothesis for human A(2A) adenosine receptor antagonists. J Chem Inf Model 2013 0.77
45 Design, synthesis and biological evaluation of new classes of thieno[3,2-d]pyrimidinone and thieno[1,2,3]triazine as inhibitor of vascular endothelial growth factor receptor-2 (VEGFR-2). Eur J Med Chem 2013 0.76
46 Antiproliferative and proapoptotic activity of CLM3, a novel multiple tyrosine kinase inhibitor, alone and in combination with SN-38 on endothelial and cancer cells. Biochem Pharmacol 2011 0.76
47 Anti-ischaemic activity of an antioxidant aldose reductase inhibitor on diabetic and non-diabetic rat hearts. J Pharm Pharmacol 2010 0.76
48 Identification of anxiolytic/nonsedative agents among indol-3-ylglyoxylamides acting as functionally selective agonists at the gamma-aminobutyric acid-A (GABAA) alpha2 benzodiazepine receptor. J Med Chem 2009 0.76
49 Medicinal chemistry of indolylglyoxylamide TSPO high affinity ligands with anxiolytic-like effects. Curr Top Med Chem 2012 0.76
50 Structure-activity relationship refinement and further assessment of 4-phenylquinazoline-2-carboxamide translocator protein ligands as antiproliferative agents in human glioblastoma tumors. J Med Chem 2014 0.76
51 Phenylpyrazolo[1,5-a]quinazolin-5(4H)-one: a suitable scaffold for the development of noncamptothecin topoisomerase I (Top1) inhibitors. J Med Chem 2013 0.75
52 3-(Fur-2-yl)-10-(2-phenylethyl)-[1,2,4]triazino[4,3-a]benzimidazol-4(10H)-one, a novel adenosine receptor antagonist with A(2A)-mediated neuroprotective effects. ACS Chem Neurosci 2011 0.75
53 Synthesis and benzodiazepine receptor affinity of derivatives of the new tricyclic heteroaromatic system pyrido[3',2':5,6]thiopyrano[4,3-c]pyridazin-3(2H,5H)-one. Arch Pharm (Weinheim) 2005 0.75
54 Novel N-substituted indol-3-ylglyoxylamides probing the LDi and L1/L2 lipophilic regions of the benzodiazepine receptor site in search for subtype-selective ligands. J Med Chem 2007 0.75
55 Novel Pyrazolopyrimidine Derivatives as Tyrosine Kinase Inhibitors with Antitumoral Activity in Vitro and in Vivo in Papillary Dedifferentiated Thyroid Cancer. Endocrinology 2011 0.75
56 Refinement of the benzodiazepine receptor site topology by structure-activity relationships of new N-(heteroarylmethyl)indol-3-ylglyoxylamides. J Med Chem 2006 0.75
57 High affinity central benzodiazepine receptor ligands: synthesis and biological evaluation of a series of phenyltriazolobenzotriazindione derivatives. J Med Chem 2005 0.75
58 The indolylglyoxylamide scaffold as an useful tool to obtain anxiolytic agents. Curr Top Med Chem 2012 0.75
59 A virtual screening study of the 18 kDa translocator protein using pharmacophore models combined with 3D-QSAR studies. ChemMedChem 2009 0.75
60 Highlighting the new advances in drug discovery and development. ChemMedChem 2008 0.75
61 Modulation of A2B adenosine receptor by 1-Benzyl-3-ketoindole derivatives. Eur J Med Chem 2013 0.75
62 Geometrically constrained analogues of N-benzylindolylglyoxylylamides: [1, 2, 4]triazino[4, 3-a]benzimidazol-4(10H)-one derivatives as potential new ligands at the benzodiazepine receptor. Arch Pharm (Weinheim) 2003 0.75