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Joseph Fargnoli

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Articles 32
Citations 721
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Recent Articles
11.
Wong T, Lee F, Emanuel S, Fairchild C, Fargnoli J, Fink B, et al.
Clin Cancer Res . 2011 May; 17(12):4031-41. PMID: 21531814
Purpose: The extensive involvement of the HER kinases in epithelial cancer suggests that kinase inhibitors targeting this receptor family have the potential for broad spectrum antitumor activity. BMS-690514 potently inhibits...
12.
Huang F, Hurlburt W, Greer A, Reeves K, Hillerman S, Chang H, et al.
Cancer Res . 2010 Sep; 70(18):7221-31. PMID: 20807811
Agents targeting insulin-like growth factor-I receptor (IGF-IR), including antibodies and small-molecule inhibitors, are currently in clinical development for the treatment of cancers including sarcoma. However, development of resistance is a...
13.
Williams D, Chen X, Tarby C, Kaltenbach R, Cai Z, Tokarski J, et al.
Bioorg Med Chem Lett . 2010 Apr; 20(9):2998-3002. PMID: 20382527
Biarylamine-based inhibitors of Met kinase have been identified. Lead compounds demonstrate nanomolar potency in Met kinase biochemical assays and significant activity in the Met-driven GTL-16 human gastric carcinoma cell line....
14.
Patel R, Sengupta S, Kim H, Klein-Szanto A, Pyle J, Zhu F, et al.
Eur J Cancer . 2010 Mar; 46(9):1537-53. PMID: 20303261
Purpose: Tamoxifen, a selective oestrogen receptor modulator (SERM), and brivanib alaninate, a vascular endothelial growth factor receptor 2 (VEGFR-2) inhibitor, are two target specific agents that result in a substantial...
15.
Bhide R, Lombardo L, Hunt J, Cai Z, Barrish J, Galbraith S, et al.
Mol Cancer Ther . 2010 Jan; 9(2):369-78. PMID: 20103604
Tumor angiogenesis is a complex and tightly regulated network mediated by various proangiogenic factors. The fibroblast growth factor (FGF) and vascular endothelial growth factor (VEGF) family of growth factors, and...
16.
Gavai A, Fink B, Fairfax D, Martin G, Rossiter L, Holst C, et al.
J Med Chem . 2009 Oct; 52(21):6527-30. PMID: 19821562
Structure-activity relationships in a series of 4-[1H-indazol-5-ylamino]pyrrolo[2,1-f][1,2,4]triazine-6-carbamates identified dual human epidermal growth factor receptor (HER)1/HER2 kinase inhibitors with excellent biochemical potency and kinase selectivity. On the basis of its favorable...
17.
Marathe P, Kamath A, Zhang Y, DArienzo C, Bhide R, Fargnoli J
Cancer Chemother Pharmacol . 2009 Apr; 65(1):55-66. PMID: 19396600
Purpose: Brivanib alaninate is a prodrug of brivanib (BMS-540215), a potent oral VEGFR-2 inhibitor and is currently in development for the treatment of hepatocellular and colon carcinomas. In vitro and...
18.
Schroeder G, An Y, Cai Z, Chen X, Clark C, Cornelius L, et al.
J Med Chem . 2009 Mar; 52(5):1251-4. PMID: 19260711
Substituted N-(4-(2-aminopyridin-4-yloxy)-3-fluoro-phenyl)-1-(4-fluorophenyl)-2-oxo-1,2-dihydropyridine-3-carboxamides were identified as potent and selective Met kinase inhibitors. Substitution of the pyridine 3-position gave improved enzyme potency, while substitution of the pyridone 4-position led to improved aqueous...
19.
Lee F, Covello K, Castaneda S, Hawken D, Kan D, Lewin A, et al.
Clin Cancer Res . 2008 Dec; 14(24):8123-31. PMID: 19088027
Purpose: Angiogenesis is a critical step in the establishment, growth, and metastasis of solid tumors, and combination of antiangiogenic agents with chemotherapy is an attractive therapeutic option. We investigated the...
20.
Huynh H, Ngo V, Fargnoli J, Ayers M, Soo K, Koong H, et al.
Clin Cancer Res . 2008 Oct; 14(19):6146-53. PMID: 18829493
Purpose: Hepatocellular carcinoma (HCC) is the fifth most common primary neoplasm; surgery is the only curative option but 5-year survival rates are only 25% to 50%. Vascular endothelial growth factor...