Trans-4-(aminomethyl)-cyclohexanecarboxylic acid derivs. (I) and their salts are new. In (I) R is CnH2n+n'-CO; n = 4-20; and n' = +1, -1, -3 or -5. (I) are N-acyl derivs. of tranexamic acid and are useful as antitumour agents. Their anti-tumour activity is greater than that of tranexamic acid itself (cf. JAMA 1977, 238(2), 154-155) but the freedom from side-effects is the same as that of tranexamic acid. Results of pharmacological tests are given in the specification. Thus N-linoleyl-tranexamic sodium salt (mouse LD50 4.5 g./kg. s.c., 3.0 g./kg. i.p. or 8.0 g./kg. p.o) when administered 10 times i.p. in a dosage of 30 mg./kg. or 20 times p.o. in a dosage of 150 mg./kg. gives 100% survival of mice with transplanted sarcoma 180 cells (1 x 106 cells/animal), whereas survival in control animals was only 80%.
展开▼
机译:反式-4-(氨基甲基)-环己烷羧酸的衍生物。 (I)及其盐是新的。在(I)中,R为C n H 2n + n’-CO; n = 4-20;并且n'= + 1,-1,-3或-5。 (I)是N-酰基衍生物。氨甲环酸是一种抗肿瘤药。它们的抗肿瘤活性大于氨甲环酸本身(参见JAMA 1977,238(2),154-155),但无副作用与氨甲环酸相同。说明书中给出了药理试验的结果。因此,当腹膜内给药10次时,N-亚油酰基-氨甲环肟酸钠盐(小鼠LD50为4.5g./kg s.c.,3.0g。/ kg.ip。或8.0g./kg.p.o)。剂量为30 mg./kg。或每次20次剂量为150 mg./kg。移植肉瘤180细胞(1 x 106细胞/动物)的小鼠的存活率为100%,而对照动物的存活率仅为80%。
展开▼