Mordarski M, Wieczorek J, Fiszer L, Nantka-Namirski P, Rykowski A
Arch Immunol Ther Exp (Warsz). 1980;28(5):717-25.
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.
合成了几种新型3-硫代-1,2,4-三嗪衍生物，并在体外和体内系统中对其抗菌和抗肿瘤活性进行了研究。一些被研究的化合物在5-20微克/毫升的浓度下可抑制革兰氏阳性菌和真菌的生长。两种甲基-硝基-咪唑-三嗪衍生物（XI和XIII）在0.1微克/毫升时可抑制鸡成纤维细胞的生长。在14种受试化合物中，有3种（V、XII和XIII）以50和100毫克/千克的剂量连续14天皮下注射时，可抑制肉瘤180生长75%。在相同剂量下，未观察到对白血病L 1210和P 388有影响。讨论了化学结构、细胞毒性活性、抗肿瘤作用和抗菌活性之间的相关性。
