PubRank

Saul H Rosenberg

Author PubWeight™ 119.53‹?›

Top papers

Rank Title Journal Year PubWeight™‹?›
1 An inhibitor of Bcl-2 family proteins induces regression of solid tumours. Nature 2005 22.40
2 ABT-263: a potent and orally bioavailable Bcl-2 family inhibitor. Cancer Res 2008 9.65
3 ABT-199, a potent and selective BCL-2 inhibitor, achieves antitumor activity while sparing platelets. Nat Med 2013 8.89
4 ABT-888, an orally active poly(ADP-ribose) polymerase inhibitor that potentiates DNA-damaging agents in preclinical tumor models. Clin Cancer Res 2007 5.75
5 Navitoclax, a targeted high-affinity inhibitor of BCL-2, in lymphoid malignancies: a phase 1 dose-escalation study of safety, pharmacokinetics, pharmacodynamics, and antitumour activity. Lancet Oncol 2010 3.76
6 Influence of Bcl-2 family members on the cellular response of small-cell lung cancer cell lines to ABT-737. Cancer Res 2007 3.24
7 Chk1 mediates S and G2 arrests through Cdc25A degradation in response to DNA-damaging agents. J Biol Chem 2003 2.18
8 Potent and selective inhibitors of Akt kinases slow the progress of tumors in vivo. Mol Cancer Ther 2005 2.15
9 Activity of the Bcl-2 family inhibitor ABT-263 in a panel of small cell lung cancer xenograft models. Clin Cancer Res 2008 2.10
10 Studies leading to potent, dual inhibitors of Bcl-2 and Bcl-xL. J Med Chem 2007 2.09
11 Discovery of potent antagonists of the antiapoptotic protein XIAP for the treatment of cancer. J Med Chem 2004 2.05
12 Discovery of an orally bioavailable small molecule inhibitor of prosurvival B-cell lymphoma 2 proteins. J Med Chem 2008 1.85
13 A small-molecule inhibitor of Bcl-XL potentiates the activity of cytotoxic drugs in vitro and in vivo. Cancer Res 2006 1.67
14 Discovery of a potent inhibitor of the antiapoptotic protein Bcl-xL from NMR and parallel synthesis. J Med Chem 2006 1.64
15 Potent, orally active heterocycle-based combretastatin A-4 analogues: synthesis, structure-activity relationship, pharmacokinetics, and in vivo antitumor activity evaluation. J Med Chem 2002 1.55
16 Selective Chk1 inhibitors differentially sensitize p53-deficient cancer cells to cancer therapeutics. Int J Cancer 2006 1.53
17 The Bcl-2 inhibitor ABT-263 enhances the response of multiple chemotherapeutic regimens in hematologic tumors in vivo. Cancer Chemother Pharmacol 2010 1.47
18 Identification of expression signatures predictive of sensitivity to the Bcl-2 family member inhibitor ABT-263 in small cell lung carcinoma and leukemia/lymphoma cell lines. Mol Cancer Ther 2010 1.41
19 Development of a high-throughput fluorescence polarization assay for Bcl-x(L). Anal Biochem 2002 1.38
20 The Bcl-2/Bcl-X(L)/Bcl-w inhibitor, navitoclax, enhances the activity of chemotherapeutic agents in vitro and in vivo. Mol Cancer Ther 2011 1.36
21 ABT-888 confers broad in vivo activity in combination with temozolomide in diverse tumors. Clin Cancer Res 2009 1.36
22 Survivin enhances Aurora-B kinase activity and localizes Aurora-B in human cells. J Biol Chem 2002 1.35
23 ABT-263 and rapamycin act cooperatively to kill lymphoma cells in vitro and in vivo. Mol Cancer Ther 2008 1.34
24 Discovery and structure-activity relationship of antagonists of B-cell lymphoma 2 family proteins with chemopotentiation activity in vitro and in vivo. J Med Chem 2006 1.33
25 A novel mechanism of checkpoint abrogation conferred by Chk1 downregulation. Oncogene 2005 1.32
26 Potentiation of temozolomide cytotoxicity by poly(ADP)ribose polymerase inhibitor ABT-888 requires a conversion of single-stranded DNA damages to double-stranded DNA breaks. Mol Cancer Res 2008 1.27
27 Structure-guided design of a series of MCL-1 inhibitors with high affinity and selectivity. J Med Chem 2015 1.22
28 The PARP inhibitor, ABT-888 potentiates temozolomide: correlation with drug levels and reduction in PARP activity in vivo. Anticancer Res 2008 1.12
29 Discovery of a novel small molecule binding site of human survivin. Bioorg Med Chem Lett 2007 1.11
30 Syntheses of potent, selective, and orally bioavailable indazole-pyridine series of protein kinase B/Akt inhibitors with reduced hypotension. J Med Chem 2007 1.06
31 The Bcl-2 family antagonist ABT-737 significantly inhibits multiple animal models of autoimmunity. J Immunol 2009 1.03
32 Discovery of a potent and selective Bcl-2 inhibitor using SAR by NMR. Bioorg Med Chem Lett 2010 1.02
33 Synthesis and SAR of indazole-pyridine based protein kinase B/Akt inhibitors. Bioorg Med Chem 2006 0.99
34 Discovery of 3H-benzo[4,5]thieno[3,2-d]pyrimidin-4-ones as potent, highly selective, and orally bioavailable inhibitors of the human protooncogene proviral insertion site in moloney murine leukemia virus (PIM) kinases. J Med Chem 2009 0.95
35 Akt inhibitor a-443654 interferes with mitotic progression by regulating aurora a kinase expression. Neoplasia 2008 0.95
36 Aryl tetrahydropyridine inhibitors of farnesyltransferase: bioavailable analogues with improved cellular potency. Bioorg Med Chem Lett 2003 0.93
37 Pseudosubstrate peptides inhibit Akt and induce cell growth inhibition. Biochemistry 2004 0.93
38 Optimal classes of chemotherapeutic agents sensitized by specific small-molecule inhibitors of akt in vitro and in vivo. Neoplasia 2005 0.91
39 Novel indication for cancer therapy: Chk1 inhibition sensitizes tumor cells to antimitotics. Int J Cancer 2005 0.91
40 Discovery and SAR of oxindole-pyridine-based protein kinase B/Akt inhibitors for treating cancers. Bioorg Med Chem Lett 2006 0.87
41 Tumor selective antivascular effects of the novel antimitotic compound ABT-751: an in vivo rat regional hemodynamic study. Cancer Chemother Pharmacol 2004 0.86
42 N-aryl-benzimidazolones as novel small molecule HSP90 inhibitors. Bioorg Med Chem Lett 2010 0.86
43 Design, synthesis, and biological activity of 4-[(4-cyano-2-arylbenzyloxy)-(3-methyl-3H-imidazol-4-yl)methyl]benzonitriles as potent and selective farnesyltransferase inhibitors. J Med Chem 2004 0.83
44 Biological activity of A-289099: an orally active tubulin-binding indolyloxazoline derivative. Mol Cancer Ther 2003 0.83
45 1-(5-Chloro-2-alkoxyphenyl)-3-(5-cyanopyrazin-2-yl)ureas [correction of cyanopyrazi] as potent and selective inhibitors of Chk1 kinase: synthesis, preliminary SAR, and biological activities. J Med Chem 2005 0.83
46 Synthesis and biological evaluation of 4'-(6,7-disubstituted-2,4-dihydro-indeno[1,2-c]pyrazol-3-yl)-biphenyl-4-ol as potent Chk1 inhibitors. Bioorg Med Chem Lett 2007 0.82
47 Design, synthesis, and activity of achiral analogs of 2-quinolones and indoles as non-thiol farnesyltransferase inhibitors. Bioorg Med Chem Lett 2005 0.82
48 Synthesis and structure-activity relationship of 3,4'-bispyridinylethylenes: discovery of a potent 3-isoquinolinylpyridine inhibitor of protein kinase B (PKB/Akt) for the treatment of cancer. Bioorg Med Chem Lett 2006 0.82
49 Isoquinoline-pyridine-based protein kinase B/Akt antagonists: SAR and in vivo antitumor activity. Bioorg Med Chem Lett 2006 0.82
50 ABT-751, a novel tubulin-binding agent, decreases tumor perfusion and disrupts tumor vasculature. Anticancer Drugs 2009 0.82
51 Discovery and SAR of 2-(1-propylpiperidin-4-yl)-1H-benzimidazole-4-carboxamide: A potent inhibitor of poly(ADP-ribose) polymerase (PARP) for the treatment of cancer. Bioorg Med Chem 2008 0.82
52 Synthesis and SAR of novel, potent and orally bioavailable benzimidazole inhibitors of poly(ADP-ribose) polymerase (PARP) with a quaternary methylene-amino substituent. Bioorg Med Chem Lett 2008 0.81
53 Synthesis and biological evaluation of 3-ethylidene-1,3-dihydro-indol-2-ones as novel checkpoint 1 inhibitors. Bioorg Med Chem Lett 2005 0.81
54 Discovery of novel inhibitors of Bcl-xL using multiple high-throughput screening platforms. Anal Biochem 2004 0.80
55 Design, synthesis, and biological activity of 5,10-dihydro-dibenzo[b,e][1,4]diazepin-11-one-based potent and selective Chk-1 inhibitors. J Med Chem 2007 0.80
56 Investigation of novel 7,8-disubstituted-5,10-dihydro-dibenzo[b,e][1,4]diazepin-11-ones as potent Chk1 inhibitors. Bioorg Med Chem Lett 2008 0.80
57 Corrigendum: The promise and peril of chemical probes. Nat Chem Biol 2015 0.79
58 Design and synthesis of pyridine-pyrazolopyridine-based inhibitors of protein kinase B/Akt. Bioorg Med Chem 2007 0.79
59 A highly potent and selective farnesyltransferase inhibitor ABT-100 in preclinical studies. Anticancer Drugs 2005 0.79
60 Synthesis and biological evaluation of 1-(2,4,5-trisubstituted phenyl)-3-(5-cyanopyrazin-2-yl)ureas as potent Chk1 kinase inhibitors. Bioorg Med Chem Lett 2006 0.79
61 Discovery of 1,4-dihydroindeno[1,2-c]pyrazoles as a novel class of potent and selective checkpoint kinase 1 inhibitors. Bioorg Med Chem 2007 0.79
62 Discovery of trans-3,4'-bispyridinylethylenes as potent and novel inhibitors of protein kinase B (PKB/Akt) for the treatment of cancer: Synthesis and biological evaluation. Bioorg Med Chem Lett 2006 0.79
63 Discovery of 4'-(1,4-dihydro-indeno[1,2-c]pyrazol-3-yl)-benzonitriles and 4'-(1,4-dihydro-indeno[1,2-c]pyrazol-3-yl)-pyridine-2'-carbonitriles as potent checkpoint kinase 1 (Chk1) inhibitors. Bioorg Med Chem Lett 2007 0.78
64 Design, synthesis, and activity of 4-quinolone and pyridone compounds as nonthiol-containing farnesyltransferase inhibitors. Bioorg Med Chem Lett 2004 0.78
65 Aryl tetrahydropyridine inhibitors of farnesyltransferase: glycine, phenylalanine and histidine derivatives. Bioorg Med Chem Lett 2003 0.78
66 Tumour-selective antivascular effects of the novel anti-mitotic compound A-318315: An in vivo rat regional haemodynamic study. Clin Exp Pharmacol Physiol 2010 0.78
67 Benzimidazolones and indoles as non-thiol farnesyltransferase inhibitors based on tipifarnib scaffold: synthesis and activity. Bioorg Med Chem Lett 2005 0.77
68 Identification of a novel 3,5-disubstituted pyridine as a potent, selective, and orally active inhibitor of Akt1 kinase. Bioorg Med Chem Lett 2006 0.77
69 Correction to Structure-Guided Design of a Series of MCL-1 Inhibitors with High Affinity and Selectivity. J Med Chem 2015 0.76
70 1,4-Dihydroindeno[1,2-c]pyrazoles as potent checkpoint kinase 1 inhibitors: extended exploration on phenyl ring substitutions and preliminary ADME/PK studies. Bioorg Med Chem Lett 2007 0.75
71 Cyanopyridyl containing 1,4-dihydroindeno[1,2-c]pyrazoles as potent checkpoint kinase 1 inhibitors: improving oral biovailability. Bioorg Med Chem Lett 2007 0.75
72 Synthesis of 1H-pyridin-2-one derivatives as potent and selective farnesyltransferase inhibitors. Bioorg Med Chem Lett 2004 0.75
73 Synthesis and biological evaluation of 1-benzyl-5-(3-biphenyl-2-yl-propyl)-1H-imidazole as novel farnesyltransferase inhibitor. Bioorg Med Chem Lett 2004 0.75
74 Discovery of potent imidazole and cyanophenyl containing farnesyltransferase inhibitors with improved oral bioavailability. Bioorg Med Chem Lett 2003 0.75
75 Design and synthesis of o-trifluoromethylbiphenyl substituted 2-amino-nicotinonitriles as inhibitors of farnesyltransferase. Bioorg Med Chem Lett 2005 0.75
76 Synthesis and in-vitro biological activity of macrocyclic urea Chk1 inhibitors. Bioorg Med Chem Lett 2007 0.75
77 Synthesis and activity of 1-aryl-1'-imidazolyl methyl ethers as non-thiol farnesyltransferase inhibitors. Bioorg Med Chem Lett 2004 0.75