pyrimidinones and Carcinoma--Ehrlich-Tumor

A new series of 3-(1,3-disubstituted-1H-pyrazole-4-carbonyl)-1,7-diphenyl-[1,2,4]triazolo[4,3-a]pyrimidin-5(1H)-ones 4 was prepared by reaction of the enaminone 2 with hydrazonoyl halides 3. The preliminary screening for antitumor activity of the synthesized compounds was carried out against Ehrlich Ascites Carcinoma tumor cells. The results revealed that the studied compounds 4 have low or no antitumor activity towards EAC tumor cells.

Topics: Animals; Antibiotics, Antineoplastic; Antineoplastic Agents; Carcinoma, Ehrlich Tumor; Cell Line, Tumor; Doxorubicin; Drug Screening Assays, Antitumor; Indicators and Reagents; Magnetic Resonance Spectroscopy; Mass Spectrometry; Mice; Pyrimidinones; Spectrophotometry, Infrared; Triazoles

Two selenium compounds have a strong antitumor effect on Ehrlich ascites tumor; 6-phenyl-7(6H)-isoselenazolo[4,3-d]pyrimidone (ISP) especially, markedly inhibited the growth of tumor inoculated i.p. in mice, inducing almost complete regression of tumors at doses of 100 micrograms/mouse per day X 10 with no sign of toxicity. The antitumor activity of 4,5-dihydro-4-methyl-6-oxo-5-phenyl-6H-pyrazolo [4,5-c]isoselenazole(PIS) was weaker than that of ISP. The total lipid and phospholipid contents in the tumor cells treated with ISP were significantly decreased. In addition, the fatty acid pattern of cholesterol esters, phosphatidyl choline and phosphatidyl ethanolamine from the ISP-treated Ehrlich ascites tumor cells differed markedly from that of the corresponding lipids from the control tumor cells.

Topics: Animals; Antineoplastic Agents; Carcinoma, Ehrlich Tumor; Fatty Acids; Female; Lipids; Mice; Mice, Inbred ICR; Organometallic Compounds; Phospholipids; Pyrimidinones; Selenium

Advanced preclinical studies on IP-10 preparation (4,6-diketo-4, 5, 6, 7-tetrahydropyrimidine-[4, 5-d]-3-methyl-isothiazole) were carried out. The drug was shown to be devoid of the irritating local effect, mildly toxic and hardly absorbing when administered per os. The toxic effect showed tendency toward cumulation. In the long-term exposure it did not affect either the elements of peripheral blood or parenchymatous organs. It exerted slight hypotensive effect on the circulatory system but only after intravenous administration. In relation to the smooth muscle organs and central nervous system, IP-10 was only slightly active. Weak effect of the compound was observed with bacteria and fungi. In the case of transplantable tumors, its activity was differentiated. It exerted a significant effect in relation to leukemia, melanoma B-16, Ehrlich carcinoma and Nemeth-Kellner lymphoma. As other isothiasole derivatives, IP-10 exhibits an interesting pharmacological, easy to render activity; particular attention should be paid to its oncostatis activity.

Topics: Animals; Antineoplastic Agents; Blood Cells; Bone Marrow; Carcinoma, Ehrlich Tumor; Cats; Central Nervous System; Chick Embryo; Dogs; Female; Guinea Pigs; Hemodynamics; Lethal Dose 50; Leukemia, Experimental; Lung Neoplasms; Male; Mass Spectrometry; Melanoma; Mice; Mice, Inbred Strains; Pyrimidinones; Rabbits; Rats; Rats, Inbred Strains; Sarcoma, Yoshida; Spectrophotometry, Infrared; Thiazoles

Topics: Animals; Carcinoma, Ehrlich Tumor; Cell Cycle; Cells, Cultured; DNA, Neoplasm; HeLa Cells; Metaphase; Mice; Puromycin; Pyrimidinones; Time Factors

Topics: Adenosine Triphosphatases; Animals; Anti-Bacterial Agents; Antimycin A; Candida; Carcinoma, Ehrlich Tumor; Cyanides; Electron Transport; Hydrogen-Ion Concentration; Ketoglutaric Acids; Malonates; Mitochondria; Mitochondria, Liver; NAD; Oxidation-Reduction; Oxygen Consumption; Phenylhydrazines; Polarography; Potentiometry; Pyrimidinones; Rats; Rotenone; Species Specificity; Spectrometry, Fluorescence; Succinates; Triazines

Topics: Animals; Carcinoma, Ehrlich Tumor; Female; Injections, Intraperitoneal; Male; Mice; Neoplasm Transplantation; Pyrimidinones; Radiation-Sensitizing Agents; Radiotherapy Dosage

Topics: Animals; Carbon Isotopes; Carcinoma, Ehrlich Tumor; Cell-Free System; Chemical Phenomena; Chemistry; Floxuridine; Kinetics; Mice; N-Glycosyl Hydrolases; Pyrimidinones; Thymidine Kinase; Transferases; Tritium