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  • 1
    Electronic Resource
    Electronic Resource
    Synthesis and Structure-Activity Relationships of New Antitumor Taxoids. Effects of Cyclohexyl Substitution at the C-3' and/or C-2 of Taxotere (Docetaxel) (1994)
    s.l. : American Chemical Society
    Journal of medicinal chemistry 37 (1994), S. 2602-2608 
    Details
    ISSN: 1520-4804
    Source: ACS Legacy Archives
    Topics: Chemistry and Pharmacology
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1021/jm00042a013
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  • 2
    Electronic Resource
    Electronic Resource
    Synthesis and antitumor activity of 1-[[(dialkylamino)alkyl]amino]-4-methyl-5H-pyrido[4,3-b]benzo[e]- and -benzo[g])indoles. A new class of antineoplastic agents (1990)
    s.l. : American Chemical Society
    Journal of medicinal chemistry 33 (1990), S. 1519-1528 
    Details
    ISSN: 1520-4804
    Source: ACS Legacy Archives
    Topics: Chemistry and Pharmacology
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1021/jm00167a037
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  • 3
    Electronic Resource
    Electronic Resource
    Heterocyclic quinones. XVII. A new in vivo active antineoplastic drug: 6,7-bis(1-aziridinyl)-4-[[3-(N,N-dimethylamino)propyl]amino]-5,8-quinazolinedione (1991)
    s.l. : American Chemical Society
    Journal of medicinal chemistry 34 (1991), S. 38-46 
    Details
    ISSN: 1520-4804
    Source: ACS Legacy Archives
    Topics: Chemistry and Pharmacology
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1021/jm00105a007
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    Paper (German National Licenses)
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  • 4
    Electronic Resource
    Electronic Resource
    Preclinical Antitumor Activity and Pharmacokinetics of Irinotecan (CPT-11) in Tumor-bearing Mice (1996)
    Oxford, UK : Blackwell Publishing Ltd
    Annals of the New York Academy of Sciences 803 (1996), S. 0 
    Details
    ISSN: 1749-6632
    Source: Blackwell Publishing Journal Backfiles 1879-2005
    Topics: Natural Sciences in General
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1111/j.1749-6632.1996.tb26386.x
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  • 5
    Electronic Resource
    Electronic Resource
    Influence of tumor size on the main drug-metabolizing enzyme systems in mouse colon adenocarcinoma Co38 (1994)
    Springer
    Cancer chemotherapy and pharmacology 34 (1994), S. 497-502 
    Details
    ISSN: 1432-0843
    Keywords: Drug-metabolizing enzymes ; Co38 tumors
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract Mouse colon adenocarcinoma Co38 is widely used as a screening model for human colon tumors. To understand better the influence of tumor size on the main drug-metabolizing enzyme systems, we tested 15 mouse Co38 tumors at different sizes. The average weight was 917±444 mg (range, 300–1,400 mg). Cytochromes P-450 (1A1/1A2, 2B1/B2, 2C8–10, 2E1, 3A4), epoxide hydrolase (EH), and glutathione-S-transferases (GST-α,-μ, and-π) were assayed by immunoblotting. The activities of the following enzymes or cofactors were determined by spectrophotometric or fluorometric assays: 1-chloro-2,4-dinitrobenzene-GST (CDNB-GST), selenium-independent glutathione peroxidase (GPX), 3,4-dichloronitrobenzene-GST (DCNB-GST), ethacrynic acid-GST (EA-GST), total glutathione (GSH), uridine diphosphate-glucuronosyltransferase (UDP-GT), β-glucuronidase (βG), sulfotransferase (ST), and sulfatase (S). Our results showed the absence of all probed P-450s and EH in Co38 tumors. No relationship was found between the Co38 tumor weights and GPX, GST-α, and EA-GST (regression analysis). However, a significant correlation was found between the tumor weights and all other enzymes investigated. For certain enzymes or cofactors, a linear decrease (P〈0.05) was observed as a function of tumor weight (CDNB-GST, DCNB-GST, GST-μ, GST-π, GSH, and βG). Other enzymatic activities (UDP-GT, S, and ST) were found to decrease in medium-size tumors and to increase in large tumors (P〈0.05; quadratic correlation). These data demonstrate that the expression of many drug-metabolizing enzyme systems is altered during tumor growth and suggest that tumoral response to chemotherapy could be altered as a function of tumor size.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00685661
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  • 6
    Electronic Resource
    Electronic Resource
    Flavone acetic acid (LM-975; NSC-347512) activation to cytotoxic species in vivo and in vitro (1989)
    Springer
    Cancer chemotherapy and pharmacology 24 (1989), S. 273-276 
    Details
    ISSN: 1432-0843
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Summary Flavone acetic acid (FAA; LM 975; NSC 347512) is a new anticancer agent with unprecedented, broad antitumor activity in murine models. Although FAA is very effective in vivo against solid tumors, including colon 38 adenocarcinoma, it was not cytotoxic in vitro against colon 38 cells and human colon adenocarcinoma cells HCT116 at pharmacologically achievable concentrations and exposure times. For example, a concentration of 300 μg/ml for a 10-day exposure time was required to obtain 〈1log cell kill. After the administration of an effective FAA dose (180 mg/kg, i.v.) to mice, plasma cytotoxicity against HCT116 cells attained a 2 log cell kill between 0.5 and 2 h, which decreased to 1 log cell kill at 4 h. No cytotoxicity was observed 6, 12 or 21 h after drug administration. The controls used comprised mouse plasma containing FAA concentrations similar to those assayed in the above plasma samples from in-vivo-dosed mice. These apiked plasma were not cytotoxic, indicating that other cytotoxic species, formed in vivo, were responsible for the increased cytotoxicity. Mouse hepatocytes co-cultured with HCT116 cells increased FAA cytotoxicity to 1 log cell kill at 30–100 μg/ml. The addition of phenobarbital-induced mouse liver supernatant S-9000xg also markedly increased FAA cytotoxicity to a 2 log cell kill at 300 μg/ml. We conclude that FAA can be activated both in vivo and in vitro to cytotoxic species that are more active than the parent compound.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00304757
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  • 7
    Electronic Resource
    Electronic Resource
    Influence of tumor size on the main drug-metabolizing enzyme systems in mouse colon adenocarcinoma Co38 (1994)
    Springer
    Cancer chemotherapy and pharmacology 34 (1994), S. 497-502 
    Details
    ISSN: 1432-0843
    Keywords: Key words: Drug-metabolizing enzymes – Co38 tumors
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract. Mouse colon adenocarcinoma Co38 is widely used as a screening model for human colon tumors. To understand better the influence of tumor size on the main drug-metabolizing enzyme systems, we tested 15 mouse Co38 tumors at different sizes. The average weight was 917±444 mg (range, 300 – 1,400 mg). Cytochromes P-450 (1A1/1A2, 2B1/B2, 2C8-10, 2E1, 3A4), epoxide hydrolase (EH), and glutathione-S-transferases (GST-α, -μ, and -π) were assayed by immunoblotting. The activities of the following enzymes or cofactors were determined by spectrophotometric or fluorometric assays: 1-chloro-2,4-dinitrobenzene-GST (CDNB-GST), selenium-independent glutathione peroxidase (GPX), 3,4-dichloronitrobenzene-GST (DCNB-GST), ethacrynic acid-GST (EA-GST), total glutathione (GSH), uridine diphosphate-glucuronosyltransferase (UDP-GT), β-glucuronidase (βG), sulfotransferase (ST), and sulfatase (S). Our results showed the absence of all probed P-450s and EH in Co38 tumors. No relationship was found between the Co38 tumor weights and GPX, GST-α, and EA-GST (regression analysis). However, a significant correlation was found between the tumor weights and all other enzymes investigated. For certain enzymes or cofactors, a linear decrease (P 〈0.05) was observed as a function of tumor weight (CDNB-GST, DCNB-GST, GST-μ, GST-π, GSH, and βG). Other enzymatic activities (UDP-GT, S, and ST) were found to decrease in medium-size tumors and to increase in large tumors (P 〈0.05; quadratic correlation). These data demonstrate that the expression of many drug-metabolizing enzyme systems is altered during tumor growth and suggest that tumoral response to chemotherapy could be altered as a function of tumor size.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00685661
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    Paper (German National Licenses)
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  • 8
    Electronic Resource
    Electronic Resource
    Pharmacodynamics and causes of dose-dependent pharmacokinetics of flavone-8-acetic acid (LM-975; NSC-347512) in mice (1989)
    Springer
    Cancer chemotherapy and pharmacology 24 (1989), S. 15-22 
    Details
    ISSN: 1432-0843
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Summary Flavone acetic acid (FAA) is a novel antitumor agent with broad solid-tumor activity. However, this drug has shown a steep dose-response curve in preclinical trials, with a narrow sublethal window of efficacy. To investigate this threshold behavior, we studied various aspects of FAA pharmacology in mice after i.v. administration. Mice bearing advanced-stage s.c. colon 38 adenocarcinoma were treated at four dose levels (39, 65, 108, and 180 mg/kg), and only the highest dose produced significant antitumor activity, showing a steep dose-response curve. Using an HPLC assay, FAA pharmacokinetics in both plasma and tumors were found to be dose-dependent. As the dose increased, there was a decrease in both total body clearance and volume of distribution at steady state. The increase in tumor area under the curve (AUC) was more pronounced than the corresponding increase in plasma AUC, showing a better tumor exposure to FAA at high doses. The distribution of FAA in normal tissues showed a short-term retention in the liver and kidneys; low concentrations were observed in the heart, spleen, and brain, with some retention in the latter. The highest FAA concentrations were found in the gastrointestinal (GI) tract, mainly in the duodenum, suggesting an important biliary excretion of the drug. Various possible causes of FAA nonlinear pharmacokinetics were investigated. Serum protein binding was high (79%) and remained constant up to 100 μg/ml, but decreased thereafter at higher FAA concentrations, e.g., 76% at 500 μg/ml and 64% at 1,000 μg/ml. Urinary and biliary clearances were dose-dependent and decreased 5- and 9-fold, from the 39- to the 180-mg/kg dose levels, respectively. A direct assessment of FAA enterohepatic circulation using intercannulated mice showed that 27% of the plasma AUC was accounted for by enterohepatic circulation. FAA acyl glucuronide was identified as the major metabolite in mice and was found to contribute to the nonlinear pharmacokinetics due to its facile hydrolysis under physiological conditions, regenerating FAA. In conclusion, the steep FAA dose-response curve was found to be caused by dose-dependent pharmacokinetics in mice. The nonlinear pharmacokinetics of this drug was attributed to a dose-dependent decrease in both urinary and biliary clearances, concentration-dependent serum protein binding, enterohepatic circulation, and the instability of FAA acyl glucuronide under physiological conditions, forming a futile cycle. The distribution data also suggested possible tissue targets for anticancer efficacy and/or toxicity that could be useful in designing clinical studies.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00254099
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  • 9
    Electronic Resource
    Electronic Resource
    Activity of flavone acetic acid (NSC-347512) against solid tumors of mice (1986)
    Springer
    Investigational new drugs 4 (1986), S. 207-220 
    Details
    ISSN: 1573-0646
    Keywords: flavone acetic acid ; solid tumor active
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Abstract Flavone acetic acid (FAA) is a new antitumor agent that has recently entered Phase I clinical trials. In preclinical studies, we have found that FAA was broadly active against a variety of transplantable solid tumors of mice (colon #51, #07, #10, #26; pancreatic ductal adenocarcinomas #02 and #03; mammary adenocarcinoma #16/C/Adr; M5076 reticulum cell sarcoma and Glasgow's osteosarcoma). FAA was curative for colon adenocarcinoma # 10 and pancreatic ductal adenocarcinoma # 03. Thus, for the first time an agent has been identified with very broad, perhaps nearly universal solid tumor activity. FAA was also found to be orally active and stable in solution at 37 °C for 48 h. FAA was selectively cytotoxic in vitro for solid tumors over leukemias L1210 and P388 (in a soft-agar colony formation assay), thus correlating cellular selectivity in vitro with in vivo antitumor activity. The finding that FAA was active in vitro, established that the agent did not need metabolism (activation) outside the tumor cell. The main drawback of FAA was an unusual ‘threshold’ behavior in which only a narrow range of doses were active and splitting the dose markedly decreased activity.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00179586
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  • 10
    Electronic Resource
    Electronic Resource
    5-Fluorouracil containing combinations in murine tumor systems (1989)
    Springer
    Investigational new drugs 7 (1989), S. 37-49 
    Details
    ISSN: 1573-0646
    Keywords: 5-fluorouracil ; murine tumor systems
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary 5-FUra is a familiar member of a variety of clinically useful regimens. Examples include: Cytoxan-Adriamycin-5-FUra (CAP); Methotrexate-Prednisone-Vincristine-Cytoxan-5-FUra (the Cooper regimen); and CisDDPt-5-FUra. In addition to its clinical utility, over 20 different 5-FUra-combinations have been reported to be therapeutically synergistic in experimental systems (Table 1). In this report, we will attempt to evaluate the reasons behind the widespread utility of this agent in combination therapy and suggest future directions for research efforts.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00178190
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