Klayman D L, Scovill J P, Mason C J, Bartosevich J F, Bruce J, Lin A J
Arzneimittelforschung. 1983;33(7):909-12. doi: 10.1002/chin.198344210.
N4-Monosubstituted and N4,N4-disubstituted thiosemicarbazones derived from 2-acetylpyridine, 2-acetyl-6-methylpyridine and 2-butyrylpyridine, and N4,N4-disubstituted selenosemicarbazones derived from 2-acetylpyridine were evaluated against leukemia P388 in the mouse. Significant antitumor activity (T/C greater than 125%) was observed for members of each class. Enhancement of antitumor activity resulted from increasing the size of the N4-substituent of the thiosemicarbazone moiety. Selenosemicarbazones were less active than the corresponding thiosemicarbazones.
对源自2-乙酰基吡啶、2-乙酰基-6-甲基吡啶和2-丁酰基吡啶的N4-单取代和N4,N4-二取代硫代氨基脲,以及源自2-乙酰基吡啶的N4,N4-二取代硒代氨基脲进行了小鼠白血病P388实验评估。每类化合物的成员均表现出显著的抗肿瘤活性(T/C大于125%)。硫代氨基脲部分N4-取代基尺寸的增大导致了抗肿瘤活性的增强。硒代氨基脲的活性低于相应的硫代氨基脲。