Chemical, pharmacological and oncostatic properties of 5-(4'-hydroxybenzylidenoimino)-4, 6-diketo-4, 5, 6, 7-tetrahydropyrimidine-[4, 5-d]-3-methyl-isothiazole (compound IP-10).
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.
D000818:Animals; D000970:Antineoplastic Agents / Q000627:therapeutic use*; D001773:Blood Cells / Q000187:drug effects; D001853:Bone Marrow / Q000187:drug effects; D002286:Carcinoma, Ehrlich Tumor / Q000188:drug therapy; D002415:Cats; D002490:Central Nervous System / Q000187:drug effects; D002642:Chick Embryo; D004285:Dogs; D005260:Female; D006168:Guinea Pigs; D006439:Hemodynamics / Q000187:drug effects; D007928:Lethal Dose 50; D007942:Leukemia, Experimental / Q000188:drug therapy; D008175:Lung Neoplasms / Q000188:drug therapy; D008297:Male; D013058:Mass Spectrometry; D008545:Melanoma / Q000188:drug therapy; D051379:Mice; D008815:Mice, Inbred Strains; D011744:Pyrimidinones / Q000032:analysis / Q000138:chemical synthesis / Q000494:pharmacology* / Q000627:therapeutic use / Q000633:toxicity; D011817:Rabbits; D051381:Rats; D011919:Rats, Inbred Strains; D012517:Sarcoma, Yoshida / Q000188:drug therapy; D013055:Spectrophotometry, Infrared; D013844:Thiazoles
D000970:Antineoplastic Agents; D011744:Pyrimidinones; D013844:Thiazoles; C041057:5(4'-hydroxybenzylidenoimino)-3-methylisothiazolo(5,4-d)pyrimidine-(7H)-4,6-dione