Výsledky vyhledávání - "L S, Gossett"

Synthesis and biological activity of 2-desamino and 4-deoxy analogs of 5,10-dideazatetrahydrofolic acid (DDATHF)

Autor: Y. Hu, Laurane G. Mendelsohn, Lillian L. Habeck, L. S. Gossett, Gerald B. Grindey, C. Shih

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 3:2657-2660

Either the 2-amino or the 4-oxo group of the potent GAR formyl-transferase inhibitor 5,10-dideazatetrahydrofolic acid (DDATHF) was replaced with a hydrogen atom and their biological activity evaluated.

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::8f76f240aaf633ac108fe79f953be2c9
https://doi.org/10.1016/s0960-894x(01)80736-8

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ChemInform Abstract: The Synthesis of N-(2-Amino-4-Substituted((pyrrolo(2,3-d)pyrimidin-5- yl)ethyl)benzoyl)-L-glu tamic Acids as Antineoplastic Agents

Autor: L. S. Gossett, Chuan Shih

Publikováno v: ChemInform. 24

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::40b345a09961e9acd308cb7b6021cda9
https://doi.org/10.1002/chin.199351296

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ChemInform Abstract: Synthesis and Biological Evaluation of a New Series of Dihydrofolate Reductase Inhibitors Based on the 4-(2,6-Diamino-5-pyrimidinyl)alkyl-L- glutamic Acid Structure

Autor: Susan B. Gates, Gerald B. Grindey, Lillian L. Habeck, Manohar Ratnam, L. S. Gossett, L. G. Mendelsohn, John F. Worzalla, Chuan Shih, Sherri L. Andis, W. Kohler, Richard M. Schultz

Publikováno v: ChemInform. 27

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::3f7dff56a54d5b566a328f424cb675e8
https://doi.org/10.1002/chin.199625202

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LY231514, a pyrrolo[2,3-d]pyrimidine-based antifolate that inhibits multiple folate-requiring enzymes

Autor: C, Shih, V J, Chen, L S, Gossett, S B, Gates, W C, MacKellar, L L, Habeck, K A, Shackelford, L G, Mendelsohn, D J, Soose, V F, Patel, S L, Andis, J R, Bewley, E A, Rayl, B A, Moroson, G P, Beardsley, W, Kohler, M, Ratnam, R M, Schultz

Publikováno v: Cancer research. 57(6)

N-[4-[2-(2-amino-3,4-dihydro-4-oxo-7H-pyrrolo[2,3-d]pyrimidin-5-yl)ethyl ]-benzoyl]-L-glutamic acid (LY231514) is a novel pyrrolo[2,3-d]pyrimidine-based antifolate currently undergoing extensive Phase II clinical trials. Previous studies have establi

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::f0225038e454981676e617741fec3d59
https://pubmed.ncbi.nlm.nih.gov/9067281

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Characterization of folate receptor from normal and neoplastic murine tissue: influence of dietary folate on folate receptor expression

Autor: S B, Gates, L G, Mendelsohn, K A, Shackelford, L L, Habeck, J D, Kursar, L S, Gossett, J F, Worzalla, C, Shih, G B, Grindey

Publikováno v: Clinical cancer research : an official journal of the American Association for Cancer Research. 2(7)

Membrane-associated folate receptors (FRs) have been detected in many mammalian species, and multiple isoforms have been identified. The pharmacological properties of FRs from murine kidney, liver, and six murine tumors were characterized. Murine kid

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::7e351458dc56644c909c826976e41a81
https://pubmed.ncbi.nlm.nih.gov/9816279

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Substrate specificity of mammalian folylpolyglutamate synthetase for 5,10-dideazatetrahydrofolate analogs

Autor: L L, Habeck, L G, Mendelsohn, C, Shih, E C, Taylor, P D, Colman, L S, Gossett, T A, Leitner, R M, Schultz, S L, Andis, R G, Moran

Publikováno v: Molecular pharmacology. 48(2)

The metabolism of 5,10-dideazatetrahydrofolate (DDATHF [lometrexol]) to polyglutamate derivatives by folylpoly-gamma-glutamate synthetase (FPGS) plays a central role in the activity of this compound as an antineoplastic agent. The availability of a s

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::9ed8e094b41fc87a70247abc4f91956c
https://pubmed.ncbi.nlm.nih.gov/7651366

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A novel class of monoglutamated antifolates exhibits tight-binding inhibition of human glycinamide ribonucleotide formyltransferase and potent activity against solid tumors

Autor: L L, Habeck, T A, Leitner, K A, Shackelford, L S, Gossett, R M, Schultz, S L, Andis, C, Shih, G B, Grindey, L G, Mendelsohn

Publikováno v: Cancer research. 54(4)

Tight-binding inhibition of recombinant human monofunctional glycinamide ribonucleotide formyltransferase by Lometrexol (6R-5,10-dideazatetrahydrofolate) requires polyglutamation. LY254155 and LY222306 differ from 5,10-dideazatetrahydrofolate in the

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::e76d346b8589dba52d6d25ffa45345e9
https://pubmed.ncbi.nlm.nih.gov/8313357

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The Synthesis of N-{2-Amino-4-substituted [(Pyrrolo[2,3-d]pyrimidin-5-yl)ethyl]benzoyl}-L-glutamic Acids as Antineoplastic Agents

Autor: L. S. Gossett, Chuan Shih

Publikováno v: HETEROCYCLES. 35:825

A series of N-{2-amino-4-substituted[(pyrrolo[2,3-d]pyrimidin-5-yl)ethyl]benzoyl}-L-glutamic acids were synthesized. In this current synthesis, compound 2-amino-4-chloro-pyrrolo[2,3-d]pyrimidine (4) was selected as an important precursor for the prep

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::285e155d657c128111f1cb8961211c9b
https://doi.org/10.3987/com-92-s(t)65

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