Výsledky vyhledávání - "Brian G, Hartl"

3-(3,5-Dimethoxyphenyl)-1,6-naphthyridine-2,7-diamines and Related 2-Urea Derivatives Are Potent and Selective Inhibitors of the FGF Receptor-1 Tyrosine Kinase

Autor: Wayne Klohs, Denise L. Driscoll, Aneesa M. Amar, Wilbur R. Leopold, H. D. Hollis Showalter, Brian G. Hartl, William L. Elliott, Bill J. Roberts, Stacey L. Boushelle, Andrew M. Thompson, Randall W. Steinkampf, Connolly Cleo, Patrick W. Vincent, William A. Denny, James M. Hamby, Sandra J. Patmore, Alan J. Kraker

Publikováno v: Journal of Medicinal Chemistry. 43:4200-4211

A series of 3-aryl-1,6-naphthyridine-2,7-diamines and related 2-ureas were prepared and evaluated as inhibitors of the FGF receptor-1 tyrosine kinase. Condensation of 4,6-diaminonicotinaldehyde and substituted phenylacetonitriles gave intermediate na

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b07718491fc8ec80795a8cc02f1071ca
https://doi.org/10.1021/jm000161d

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Biochemical and cellular effects of c-Src kinase-selective pyrido[2,3-d]pyrimidine tyrosine kinase inhibitors

Autor: Alan J. Kraker, Charles W. Moore, Barvian Mark Robert, Brian G. Hartl, H. D. Hollis Showalter, Aneesa Amar

Publikováno v: Biochemical Pharmacology. 60:885-898

Increased expression or activity of c-Src tyrosine kinase has been associated with the transformed phenotype in tumor cells and with progression of neoplastic disease. A number of pyrido[2, 3-d]pyrimidines have been characterized biochemically and in

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9124c7855e894eaa5e692f9de06815b7
https://doi.org/10.1016/s0006-2952(00)00405-6

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Synthesis and Tyrosine Kinase Inhibitory Activity of a Series of 2-Amino-8H-pyrido[2,3-d]pyrimidines: Identification of Potent, Selective Platelet-Derived Growth Factor Receptor Tyrosine Kinase Inhibitors

Publikováno v: Journal of Medicinal Chemistry. 41:4365-4377

Screening of a compound library led to the identification of 2-amino-6-(2,6-dichlorophenyl)-8-methylpyrido[2,3-d]pyrimidine (1) as a inhibitor of the platelet-derived growth factor receptor (PDGFr), fibroblast growth factor receptor (FGFr), and c-src

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fc761f1e47ac7d9db7f59488360a5bd4
https://doi.org/10.1021/jm980398y

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1-Oxo-3-aryl-1H-indene-2-carboxylic acid derivatives as selective inhibitors of fibroblast growth factor receptor-1 tyrosine kinase

Autor: Aneesa Amar, Gina H. Lu, Alan J. Kraker, H. D. Hollis Showalter, James Marino Hamby, Barvian Mark Robert, Brian G. Hartl, Robert L. Panek

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 7:2903-2908

Fibroblast growth factor receptor (FGFr) mediated signal transduction is implicated in vascular proliferative diseases and some cancers. We have identified methyl 1-oxo-3-phenyl-1H-indene-2-carboxylic ester as a small molecule inhibitor of the tyrosi

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::25cbbf66eab9272afd6be54069fec679
https://doi.org/10.1016/s0960-894x(97)10110-x

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ChemInform Abstract: 1-Oxo-3-aryl-1H-indene-2-carboxylic Acid Derivatives as Selective Inhibitors of Fibroblast Growth Factor Receptor-1 Tyrosine Kinase

Autor: Alan J. Kraker, Brian G. Hartl, Gina H. Lu, James Marino Hamby, H. D. Hollis Showalter, Aneesa Amar, Robert L. Panek, Barvian Mark Robert

Publikováno v: ChemInform. 29

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::1f0f7e7cd5355b6b23e6ee67041af8b7
https://doi.org/10.1002/chin.199810112

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Modulation of histone acetylation by [4-(acetylamino)-N-(2-amino-phenyl) benzamide] in HCT-8 colon carcinoma

Autor: Alan J, Kraker, Craig A, Mizzen, Brian G, Hartl, Johnson, Miin, C David, Allis, Ronald L, Merriman

Publikováno v: Molecular cancer therapeutics. 2(4)

CI-994 or N-acetyldinaline [4-(acetylamino)-N-(2-amino-phenyl) benzamide] is an antitumor cytostatic agent currently undergoing clinical trial. Although several changes in cellular metabolism induced by the drug have been characterized, the primary m

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::fbdb6d16baa0902ba8b6650110814e92
https://pubmed.ncbi.nlm.nih.gov/12700284

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Synthesis and structure-activity relationships of 7-substituted 3-(2, 6-dichlorophenyl)-1,6-naphthyridin-2(1H)-ones as selective inhibitors of pp60(c-src)

Autor: William A. Denny, Robert L. Panek, Brian L. Batley, Andrew M. Thompson, Stacey L. Boushelle, Gina H. Lu, H. D. Hollis Showalter, Gordon W. Rewcastle, Brian G. Hartl, Alan J. Kraker

Publikováno v: Journal of medicinal chemistry. 43(16)

7-substituted 3-(2,6-dichlorophenyl)-1,6-naphthyridin-2(1H)-ones are potent inhibitors of protein tyrosine kinases, with some selectivity for c-Src. The compounds were prepared by condensing 4, 6-diaminonicotinaldehyde with 2,6-dichlorophenylacetonit

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5cbf98d01a162b8164e45598fd724727
https://pubmed.ncbi.nlm.nih.gov/10956222

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Structure-activity relationships for 5-substituted 1-phenylbenzimidazoles as selective inhibitors of the platelet-derived growth factor receptor

Autor: Alan J. Kraker, William A. Denny, Brian D. Palmer, Robert L. Panek, Brian G. Hartl, Gina H. Lu, H. D. Hollis Showalter, Susanne Trumpp-Kallmeyer, Athanasia D. Panopoulos, Brian L. Batley

Publikováno v: Journal of medicinal chemistry. 42(13)

Following an earlier discovery of 1-phenylbenzimidazoles as ATP-site inhibitors of the platelet-derived growth factor receptor (PDGFR), further structure-activity relationships for analogues (particularly 5-substituted derivatives) are reported. The

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ff02ae32c84e2f6c614152ed6cc7f36a
https://pubmed.ncbi.nlm.nih.gov/10395478

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2-Substituted aminopyrido[2,3-d]pyrimidin-7(8H)-ones. structure-activity relationships against selected tyrosine kinases and in vitro and in vivo anticancer activity

Publikováno v: Journal of medicinal chemistry. 41(17)

While engaged in therapeutic intervention against a number of proliferative diseases, we have discovered the 2-aminopyrido[2, 3-d]pyrimidin-7(8H)-ones as a novel class of potent, broadly active tyrosine kinase (TK) inhibitors. An efficient route was

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a96247a3000b371a6bbb1cbb03279775
https://pubmed.ncbi.nlm.nih.gov/9703473

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