Výsledky vyhledávání

Potential antitumor agents. 61. Structure-activity relationships for in vivo colon 38 activity among disubstituted 9-oxo-9H-xanthene-4-acetic acids

Autor: Gordon W. Rewcastle, Z A Li, Bruce C. Baguley, William A. Denny, G. J. Atwell

Publikováno v: Journal of Medicinal Chemistry. 34:217-222

Analogues of 9-oxo-9H-xanthene-4-acetic acid (XAA) bearing small, lipophilic 5-substituents are among the most dose-potent compounds yet reported with the capability of causing hemorrhagic necrosis of implanted colon 38 tumors in mice. To further ext

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ff70722d20e6e5c75723d902217d9ace
https://doi.org/10.1021/jm00105a034

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Inhibition of the action of the topoisomerase II poison amsacrine by simple aniline derivatives: evidence for drug-protein interactions

Autor: G J, Finlay, G J, Atwell, B C, Baguley

Publikováno v: Oncology research. 11(6)

The action of the anticancer drug amsacrine appears to involve molecular interactions with both DNA and topoisomerase II. It has been shown previously that DNA intercalators can inhibit the action of amsacrine and several other topoisomerase II poiso

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::927f13a9c0020e05e14a2476cf5d3ed2
https://pubmed.ncbi.nlm.nih.gov/10691026

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Dimeric analogues of non-cationic tricyclic aromatic carboxamides are a new class of cytotoxic agents

Autor: J A, Spicer, S A, Gamage, G J, Atwell, G J, Finlay, B C, Baguley, W A, Denny

Publikováno v: Anti-cancer drug design. 14(3)

A series of tricyclic aromatic carboxamides, and their corresponding dimeric analogues, were prepared and their growth-inhibitory properties were evaluated in a series of cell lines. The dimeric compounds were prepared by reaction of the appropriate

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::174ac09f86e7d3da9cf3c13b7333bb86
https://pubmed.ncbi.nlm.nih.gov/10500503

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Synthesis and evaluation of 4-substituted analogues of 5-[N,N-bis (2-chloroethyl)amino]-2-nitrobenzamide as bioreductively activated prodrugs using an Escherichia coli nitroreductase

Autor: G J, Atwell, M, Boyd, B D, Palmer, R F, Anderson, S M, Pullen, W R, Wilson, W A, Denny

Publikováno v: Anti-cancer drug design. 11(7)

2,4-Dinitrobenzamide mustards, exemplified by the parent compound SN 23862 (2) are activated under aerobic conditions by an Escherichia coli nitroreductase enzyme (NR2) via selective reduction of the 2-nitro group, and are thus of interest as prodrug

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::164b89df8fc6ea3d8790dc1c707e3114
https://pubmed.ncbi.nlm.nih.gov/8921936

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Metabolic and radiolytic reduction of 4-alkylamino-5-nitroquinoline bioreductive drugs. Relationship to hypoxia-selective cytotoxicity

Autor: B G, Siim, G J, Atwell, W R, Wilson

Publikováno v: Biochemical pharmacology. 48(8)

The 4-alkylamino-5-nitroquinolines (5NQs) are a new series of bioreductive drugs that exhibit varying degrees of selective toxicity (up to 60-fold) under hypoxic conditions in cell culture. This study tested the hypothesis that differences in hypoxia

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::167373e60441a5ea78a457e5612a9bf6
https://pubmed.ncbi.nlm.nih.gov/7980625

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Oxygen dependence of the cytotoxicity and metabolic activation of 4-alkylamino-5-nitroquinoline bioreductive drugs

Autor: William R. Wilson, Bronwyn G. Siim, G. J. Atwell

Publikováno v: British Journal of Cancer

The cytotoxic potency of 4-alkylamino-5-nitroquinoline drugs in AA8 cell cultures is enhanced up to 60-fold under hypoxia, with wide variations in selectivity for hypoxic cells observed for different members of this series. This study uses three repr

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9d91294f5e12b3ffdec60e38a3bc518a
https://pubmed.ncbi.nlm.nih.gov/7917903

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