Schulze W, Letsch G, Gutsche W, Jungstand W, Wohlrabe K
Pharmazie. 1979 Apr;34(4):216-21.
A series of carbonyl derivatives of tilorone was synthetized by reaction with appropriate amino compounds, mainly hydrazines and hydrazides. The condensation products obtained were tested for cancerostatic activity against the murine leucaemia L 1210 and the Walker carcinosarcoma of the rat. Only three of the substances under investigation (1a, 5, 13) proved active against the Walker carcinosarcoma, one of which (5) being comparable to tilorone. No activity against L 1210 was observed, even tilorone exerted no effect. The reduction in activity against the Walker carcinosarcoma which resulted from the carbonyl substitution might be caused by a decrease in the ability to intercalate into DNA.
通过与适当的氨基化合物（主要是肼和酰肼）反应，合成了一系列替洛隆的羰基衍生物。对所得缩合产物进行了抗小鼠白血病L 1210和大鼠沃克癌肉瘤的抑癌活性测试。在所研究的物质中，只有三种（1a、5、13）对沃克癌肉瘤有活性，其中一种（5）与替洛隆相当。未观察到对L 1210的活性，即使替洛隆也没有作用。羰基取代导致的对沃克癌肉瘤活性降低可能是由于插入DNA能力的下降。
