5(4--hydroxybenzylidenoimino)-3-methylisothiazolo(5-4-d)pyrimidine-(7h)-4-6-dione and Melanoma

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