|
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
|
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
|
|
3
|
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
|
|
4
|
Identification of Src-specific phosphorylation site on focal adhesion kinase: dissection of the role of Src SH2 and catalytic functions and their consequences for tumor cell behavior.
|
Cancer Res
|
2005
|
1.45
|
|
5
|
Antiangiogenic and antitumor effects of SRC inhibition in ovarian carcinoma.
|
Cancer Res
|
2006
|
1.38
|
|
6
|
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
|
|
7
|
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
|
|
8
|
SRC inhibitors in metastatic bone disease.
|
Clin Cancer Res
|
2006
|
0.99
|
|
9
|
SRC homology-2 inhibitors: peptidomimetic and nonpeptide.
|
Mini Rev Med Chem
|
2002
|
0.87
|
|
10
|
Future anti-catabolic therapeutic targets in bone disease.
|
Ann N Y Acad Sci
|
2006
|
0.81
|
|
11
|
In vitro and in vivo activity of ATP-based kinase inhibitors AP23464 and AP23848 against activation-loop mutants of Kit.
|
Blood
|
2005
|
0.80
|
|
12
|
Reduced pulmonary surfactant interaction of daptomycin analogs via tryptophan replacement with alternative amino acids.
|
Bioorg Med Chem Lett
|
2012
|
0.80
|
|
13
|
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
|
|
14
|
Bone-targeted Src kinase inhibitors: novel pyrrolo- and pyrazolopyrimidine analogues.
|
Bioorg Med Chem Lett
|
2003
|
0.79
|
|
15
|
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
|
|
16
|
Novel bone-targeted Src tyrosine kinase inhibitor drug discovery.
|
Curr Opin Drug Discov Devel
|
2003
|
0.78
|
|
17
|
Structure-based design of novel nonpeptide inhibitors of the Src SH2 domain:phosphotyrosine mimetics exploiting multifunctional group replacement chemistry.
|
Biopolymers
|
2003
|
0.76
|
|
18
|
Novel protein kinase inhibitors: SMART drug design technology.
|
Biotechniques
|
2003
|
0.75
|
|
19
|
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
|