PubRank

William C Shakespeare

Author PubWeight™ 37.85‹?›

Top papers

Rank Title Journal Year PubWeight™‹?›
1 AP24534, a pan-BCR-ABL inhibitor for chronic myeloid leukemia, potently inhibits the T315I mutant and overcomes mutation-based resistance. Cancer Cell 2009 6.97
2 Therapeutic strategies to overcome crizotinib resistance in non-small cell lung cancers harboring the fusion oncogene EML4-ALK. Proc Natl Acad Sci U S A 2011 3.97
3 Inhibition of wild-type and mutant Bcr-Abl by AP23464, a potent ATP-based oncogenic protein kinase inhibitor: implications for CML. Blood 2004 2.61
4 Structural mechanism of the Pan-BCR-ABL inhibitor ponatinib (AP24534): lessons for overcoming kinase inhibitor resistance. Chem Biol Drug Des 2010 2.19
5 Ponatinib (AP24534), a multitargeted pan-FGFR inhibitor with activity in multiple FGFR-amplified or mutated cancer models. Mol Cancer Ther 2012 2.05
6 Discovery of 3-[2-(imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide (AP24534), a potent, orally active pan-inhibitor of breakpoint cluster region-abelson (BCR-ABL) kinase including the T315I gatekeeper mutant. J Med Chem 2010 1.82
7 Crizotinib-resistant mutants of EML4-ALK identified through an accelerated mutagenesis screen. Chem Biol Drug Des 2011 1.68
8 Potent activity of ponatinib (AP24534) in models of FLT3-driven acute myeloid leukemia and other hematologic malignancies. Mol Cancer Ther 2011 1.51
9 Antiangiogenic and antitumor effects of SRC inhibition in ovarian carcinoma. Cancer Res 2006 1.38
10 Activity of dual SRC-ABL inhibitors highlights the role of BCR/ABL kinase dynamics in drug resistance. Proc Natl Acad Sci U S A 2006 1.30
11 AP23846, a novel and highly potent Src family kinase inhibitor, reduces vascular endothelial growth factor and interleukin-8 expression in human solid tumor cell lines and abrogates downstream angiogenic processes. Mol Cancer Ther 2005 1.13
12 9-(Arenethenyl)purines as dual Src/Abl kinase inhibitors targeting the inactive conformation: design, synthesis, and biological evaluation. J Med Chem 2009 1.10
13 Src activation of Stat3 is an independent requirement from NF-kappaB activation for constitutive IL-8 expression in human pancreatic adenocarcinoma cells. Angiogenesis 2006 1.03
14 Fragment growing and linking lead to novel nanomolar lactate dehydrogenase inhibitors. J Med Chem 2013 1.01
15 Novel N9-arenethenyl purines as potent dual Src/Abl tyrosine kinase inhibitors. Bioorg Med Chem Lett 2008 1.00
16 SRC inhibitors in metastatic bone disease. Clin Cancer Res 2006 0.99
17 SRC homology-2 inhibitors: peptidomimetic and nonpeptide. Mini Rev Med Chem 2002 0.87
18 Structural analysis of DFG-in and DFG-out dual Src-Abl inhibitors sharing a common vinyl purine template. Chem Biol Drug Des 2009 0.82
19 Future anti-catabolic therapeutic targets in bone disease. Ann N Y Acad Sci 2006 0.81
20 AP24163 inhibits the gatekeeper mutant of BCR-ABL and suppresses in vitro resistance. Chem Biol Drug Des 2009 0.81
21 In vitro and in vivo activity of ATP-based kinase inhibitors AP23464 and AP23848 against activation-loop mutants of Kit. Blood 2005 0.80
22 Discovery of 5-(arenethynyl) hetero-monocyclic derivatives as potent inhibitors of BCR-ABL including the T315I gatekeeper mutant. Bioorg Med Chem Lett 2011 0.79
23 Bone-targeted 2,6,9-trisubstituted purines: novel inhibitors of Src tyrosine kinase for the treatment of bone diseases. Bioorg Med Chem Lett 2003 0.79
24 Bone-targeted Src kinase inhibitors: novel pyrrolo- and pyrazolopyrimidine analogues. Bioorg Med Chem Lett 2003 0.79
25 Structure-based design of novel nonpeptide inhibitors of the Src SH2 domain:phosphotyrosine mimetics exploiting multifunctional group replacement chemistry. Biopolymers 2003 0.76
26 Novel protein kinase inhibitors: SMART drug design technology. Biotechniques 2003 0.75
27 Bone-targeted pyrido[2,3-d]pyrimidin-7-ones: potent inhibitors of Src tyrosine kinase as novel antiresorptive agents. Bioorg Med Chem Lett 2003 0.75