Výsledky vyhledávání - "Robert L. Tansik"

X-ray Crystal Structures of Candida albicans Dihydrofolate Reductase: High Resolution Ternary Complexes in Which the Dihydronicotinamide Moiety of NADPH Is Displaced by an Inhibitor

Autor: Lee F. Kuyper, Karl D. Hardman, Robert L. Tansik, Jean S. Hong, David Stewart, Marc Whitlow, Joseph H. Chan, Andrew J. Howard, David P. Baccanari

Publikováno v: Journal of Medicinal Chemistry. 44:2928-2932

X-ray crystallographic analysis of 5-(4'-substituted phenyl)sulfanyl-2,4-diaminoquinazoline inhibitors in ternary complex with Candida albicans dihydrofolate reductase (DHFR) and NADPH revealed two distinct modes of binding. The two compounds with sm

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b9280f132de00963466761d27b1ea5fc
https://doi.org/10.1021/jm0101444

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Preclinical Development of Eniluracil: Enhancing the Therapeutic Index and Dosing Convenience of 5-Fluorouracil

Autor: Youcef M. Rustum, Stephen T. Davis, Shousong Cao, Thomas Spector, Robert L. Tansik, David P. Baccanari, Melanie T Paff

Publikováno v: Investigational New Drugs. 18:365-371

Eniluracil (5-ethynyluracil, GW 776, 776C85) is being developed as a novel modulator of 5-fluorouracil (5-FU) for the treatment of cancer. Eniluracil is an effective mechanism-based inactivator of dihydropyrimidine dehydrogenase (DPD), the first enzy

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::beca9352e1cfae1c06b946f4caae8da1
https://doi.org/10.1023/a:1006401432488

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α-Fluoro-β-alanine: Effects on the antitumor activity and toxicity of 5-fluorouracil

Autor: Youcef M. Rustum, Robert L Tansik, Thomas Spector, Stephen T. Davis, David P. Baccanari, Shousong Cao, David J.T. Porter

Publikováno v: Biochemical Pharmacology. 59:953-960

We have shown previously that (R)-5-fluoro-5,6-dihydrouracil (FUraH(2)) attenuates the antitumor activity of 5-fluorouracil (FUra) in rats bearing advanced colorectal carcinoma. Presently, we found that alpha-fluoro-beta-alanine (FBAL), the predomina

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c254dcd64e96c70a5b257c5e55adf06e
https://doi.org/10.1016/s0006-2952(99)00408-6

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Inhibitors of dihydrofolate reductase: Design, synthesis and antimicrobial activities of 2,4-diamino-6-methyl-5-ethynylpyrimidines

Autor: Lee F. Kuyper, Christine M. Boytos, Michael L. Jones, David P. Baccanari, Sharon K. Rudolph, Robert L. Tansik

Publikováno v: Journal of Heterocyclic Chemistry. 36:145-148

Novel 2,4-diamino-6-methyl-5-ethynylpyrimidines were prepared via palladium catalyzed coupling of 2,4-diamino-5-iodo-6-methyl-pyrimidine with terminal acetylenes. The compounds were inhibitors of dihydrofolate reductase and showed in vitro activity a

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::f6743147d4075203e5d1b2f4daa6dd69
https://doi.org/10.1002/jhet.5570360122

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X-ray Crystallographic Studies of Candida albicans Dihydrofolate Reductase

Autor: Mary E. Fling, Marc Whitlow, Karl D. Hardman, Lee F. Kuyper, David P. Baccanari, David H. Stewart, Robert L. Tansik, Andrew Howard

Publikováno v: Journal of Biological Chemistry. 272:30289-30298

The recent rise in systemic fungal infections has created a need for the development of new antifungal agents. As part of an effort to provide therapeutically effective inhibitors of fungal dihydrofolate reductase (DHFR), we have cloned, expressed, p

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::cd09531b1ded6179854d95f481b14dc4
https://doi.org/10.1074/jbc.272.48.30289

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Peptide Agonist of the Thrombopoietin Receptor as Potent as the Natural Cytokine

Autor: Steven E. Cwirla, Palaniappan Balasubramanian, Ronald W. Barrett, Nicholas C. Wrighton, Peter J. Schatz, Wagstrom Christopher R, Duffin David J, David P. Baccanari, Robert L. Tansik, Sara C. Singer, Ann M. Davis, Chris M. Boytos, Christian M. Gates, William J. Dower, Larry C. Mattheakis

Publikováno v: Science. 276:1696-1699

Two families of small peptides that bind to the human thrombopoietin receptor and compete with the binding of the natural ligand thrombopoietin (TPO) were identified from recombinant peptide libraries. The sequences of these peptides were not found i

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5c6f0144b8f6b6eb938df8eaeebb3e12
https://doi.org/10.1126/science.276.5319.1696

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Synthesis of 1,3-diamino-7,8,9,10-tetrahydropyrido[3,2-f]-quinazolines. Inhibitors ofCandida albicansdihydrofolate reductase as potential antifungal agents

Autor: Sharon K. Rudolph, Lee F. Kuyper, Christine M. Boytos, Joseph H. Chan, David P. Baccanari, Jean S. Hong, Robert L. Tansik, Andrew D. Brown, Michael L. Jones

Publikováno v: Journal of Heterocyclic Chemistry. 34:145-151

A series of novel 1,3-diamino-7,8,9,10-tetrahydropyrido[3,2-f]quinazolines were synthesized starting from 6-amino-5-cyanoquinoline (4). These compounds inhibited Candida albicans dihydrofolate reductase with Ki values of ≤0.60 aM. One analogue exhi

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::4c15aa29c9097543765be38f6904484e
https://doi.org/10.1002/jhet.5570340123

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High-Affinity Inhibitors of Dihydrofolate Reductase: Antimicrobial and Anticancer Activities of 7,8-Dialkyl-1,3-diaminopyrrolo[3,2-f]quinazolines with Small Molecular Size

Autor: Lee F. Kuyper, Robert L. Tansik, H. S. Friedman, Victoria B. Knick, Michael L. Jones, J. C. W. Comley, David P. Baccanari, H. R. Wilson, Christine M. Boytos, J. N. Stables, Robert N. Hunter, Sharon K. Rudolph, S. S. Joyner, J. M. Caddell

Publikováno v: Journal of Medicinal Chemistry. 39:892-903

A series of 7,8-dialkylpyrrolo[3,2-f]quinazolines were prepared as inhibitors of dihydrofolate reductase (DHFR). On the basis of an apparent inverse relationship between compound size and antifungal activity, the compounds were designed to be relativ

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::33923d903ff9cc597e41655d56be01f0
https://doi.org/10.1021/jm9505122

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Synthesis of 5-(4-substituted benzyl)-2,4-diaminoquinazolines as inhibitors ofcandida albicansdihydrofolate reductase

Autor: Robert L. Tansik, Sharon K. Rudolph, Christine M. Boytos, Virgil L. Styles, Joseph H. Chan, G. Erik Jagdmann

Publikováno v: Journal of Heterocyclic Chemistry. 32:1461-1465

Several 5-(4-substituted benzyl)-2,4-diaminoquinazolines were prepared as potentially selective inhibitors of Candida albicans dihydrofolate reductase. These compounds were synthesized by a novel route, which included as a key step the displacement o

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::9a57b311d2226b1046ec5d462af4ec66
https://doi.org/10.1002/jhet.5570320508

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ChemInform Abstract: Selective Inhibitors of Candida albicans Dihydrofolate Reductase: Activity and Selectivity of 5-(Arylthio)-2,4-diaminoquinazolines

Autor: Robert L. Tansik, Joseph H. Chan, David P. Baccanari, Sharon K. Rudolph, Lee F. Kuyper, Jean S. Hong, Christine M. Boytos, S. S. Joyner

Publikováno v: ChemInform. 26

The recent increase in fungal infections, especially among AIDS patients, has resulted in the need for more effective antifungal agents. In our search for such agents, we focused on developing compounds which inhibit fungal dihydrofolate reductase (D

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::1e47aa87d8d3993a0629811d7105f6a5
https://doi.org/10.1002/chin.199552156

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