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Cancer Research
**hu Li
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Biosynthesis of 17β-oestradiol in human breast carcinoma tissue and a novel method for its characterization
Conversion of 7alpha3H-testosterone to 17beta-oestradiol by human mammary carcinoma tissue in vitro has been demonstrated. It was characterized unequivocally by conversion to 17beta-oestradiol-3-sulphate upon inc...
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Clinical, toxicological, and pharmacological studies of combination chemotherapy of adenocarcinoma with Adriamycin and Baker's Antifolate
Ten patients with disseminated adenocarcinoma were treated with combination chemotherapy employing Adriamycin and Baker's Antifolate (BAF). There were seven patients with lung adenocarcinoma, two of whom achie...
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Polymorphism in fowl serum albumin. VI. Changes in in vitro protein synthesizing activity in develo** embryonic fowl liver
Cell-free protein synthesizing systems were prepared from the livers of chick embryos at selected ages and the characteristics of individual fractions were compared. While polysomes showed decreasing size with...
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Effect of hormone manipulation on oxidation, reduction and sulphurylation of dehydroepiandrosterone and oestrone in DMBA-induced rat mammary tumours
Using the DMBA-induced mammary tumour as a model, the effect of hormone manipulation on steroid sulphurylation and on oxidative and reductive metabolism has been investigated. Oestradiol-17 beta, or oestradiol...
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The pharmacologic fate of the antitumor agent 2-amino-1,3,4-thiadiazole in the dog
Anticipating the renewed clinical trial of the antitumor agent 2-amino-1,3,4-thiadiazole (AT, NSC-4728), we have studied the pharmacologic fate of AT-5-14C in beagle dogs. The drug was only minimally metabolized ...
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Cholecystectomy has no influence on frequency of chemically induced colonic cancer in mice
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Effects of endotoxin on the pharmacology of antineoplastic agents
Patients with cancer often develop serious gram-negative bacterial infections. Since bacterial endotoxins have been shown to affect the in vitro hepatic metabolism of antineoplastic agents, significant infecti...
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Disposition and metabolism of thiopurines
The anticancer agent β-2′ deoxythioguanosine (β-TGdR, NSC-71261) has potential utility for the treatment of hematologic tumors resistant to 6-thioguanine (TG). We have studied the pharmacology and metabolism o...
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Disposition of methylglyoxal bis(guanylhydrazone) (MGBG, NSC-32946) in man
A high-pressure liquid chromatographic method was utilized to determine the concentration of the antileukemic agent methylgloxal bis(guanylhydrazone) (MGBG, NSC-32946) in tissue samples obtained at autopsy fro...
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Human growth hormone: 1974–1981
Chemical investigations of the human growth hormone (HGH) molecule were briefly reviewed for the period between 1974 and 1981. These include chemical modification, selective enzymic cleavage, the 20K HGH, synt...
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Pharmacokinetics and metabolism of β-2′-deoxythioguanosine and 6-thioguanine in man
Resistance to the antileukemic agent 6-thioguanine (TG) inevitably develops in animal tumors. However, a new agent, β-2′-deoxythioguanosine (β-TGdR) can overcome TG resistance in animal tumor models and is the...
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Pharmacology of mitoxantrone in cancer patients
Radioactive mitoxantrone was administered at doses of 1–12 mg/m2 by rapid IV infusion to 11 patients. Of the 11 patients, six had normal liver and kidney function tests while the remaining five had abnormal third...
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Human tissue distribution of platinum after cis-diamminedichloroplatinum
Using X-ray fluorescence spectrometry, platinum concentrations were determined in autopsy tissue samples from 12 patients who had received cis-diamminedichloroplatinum (DDP) 20–120 mg/m2 up to 6 months antemortem...
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Effect of RA233 alone and combined with radiation on experimental tumour metastasis. Part 1
The effect of the platelet aggregation inhibitor RA233 alone or in combination with radiation was investigated on the spontaneously metastasizing B16 melanoma and on the Lewis lung carcinoma. The effect of thi...
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Antitumour effect of RA 233 alone and combined with radiotherapy
The effect of RA233 alone or in combination with radiation was investigated in vivo on the 5180 sarcoma, the B16 melanoma and the Lewis lung carcinoma.
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Human tissue distribution of 4′-(9-acridinylamino)-methanesulfon-m-anisidide (NSC 141549, AMSA)
Concentrations of AMSA were determined by HPLC in autopsy tissue samples from five patients who had received the drug antemortem. Relative organ concentrations of AMSA varied from patient to patient; however, ...
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Effect of thymidine on the toxicity and antitumor activity of Cis-diamminedichloroplatinum (II)
The effect of thymidine (TdR) on the preclinical toxicity of cis-diamminedichloroplatinum (II) (DDP) was investigated in the BDF1 mouse and the Sprague-Dawley rat. The effect of TdR on the antitumor activity of D...
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Pharmacological disposition of 1,4-dihydroxy-5-8-bis[[2[(2-hydroxyethal)amino] ethyl]amino]-9,10-anthracenedione dihydrochloride in the dog
DHAQ, a new antitumor agent, has been selected for clinical trial on the basis of its activity against a number of transplantable rodent tumors. In anticipation of the clinical trial of this agent, the pharmac...
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Site-dependence of invasiveness of ECA109 human oesophageal carcinoma cells in nude mice
ECA109 human oesophageal carcinoma cells were injected either subcutaneously or intraperitoneally into BALB/CATc 1-nu/nu mice. After 23 weeks tumours were examined histologically and by scanning electron micro...
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Identification of anthracycline analogues with enhanced cytotoxicity and lack of cross-resistance to adriamycin using a series of mammalian cell lines in vitro
Clinical resistance to adriamycin (ADR) develops readily, and cardiotoxicity is a major dose-limiting side effect. A range of anthracycline derivatives have been synthesized recently, and a number reported to ...
