Antitumor properties of selected 1,2,4-triazine derivatives.
Several new 3-thio-1,2,4-triazine derivatives were synthesized and investigated for antimicrobial and antitumor activity in in vitro and in vivo systems. Some of the investigated compounds inhibited growth of gram-positive bacteria and fungi at the concentration of 5-20 microgram/ml. Two methyl-nitro-imidazole-triazine derivatives (XI and XIII) inhibited the development of chicken fibroblast at 0.1 microgram/ml. Three out of fourteen compounds tested (V, XII and XIII) inhibited by 75% growth of sarcoma 180 when injected s.c. for 14 consecutive days in the doses of 50 and 100 mg/kg. At the same doses no effect was noted on leukemia L 1210 and P 388. Correlation between chemical structure, cytotoxic activity, antitumor effect and antimicrobial activity is discussed.
D000818:Animals; D000970:Antineoplastic Agents; D002286:Carcinoma, Ehrlich Tumor / Q000188:drug therapy; D002478:Cells, Cultured; D055598:Chemical Phenomena; D002621:Chemistry; D002642:Chick Embryo; D004353:Drug Evaluation, Preclinical; D005347:Fibroblasts / Q000187:drug effects; D066298:In Vitro Techniques; D007942:Leukemia, Experimental / Q000188:drug therapy; D008223:Lymphoma / Q000188:drug therapy; D008297:Male; D008545:Melanoma / Q000188:drug therapy; D051379:Mice; D009374:Neoplasms, Experimental / Q000188:drug therapy*; D012513:Sarcoma, Experimental / Q000188:drug therapy; D012878:Skin Neoplasms / Q000188:drug therapy; D014227:Triazines / Q000627:therapeutic use*
D000970:Antineoplastic Agents; D014227:Triazines