Braña M F, Castellano J M, Morán M, Pérez de Vega M J, Romerdahl C R, Qian X D, Bousquet P, Emling F, Schlick E, Keilhauer G
Laboratorios Knoll S. A, Madrid, Spain.
Anticancer Drug Des. 1993 Aug;8(4):257-68.
A series of bis-intercalators bearing the 1,8-naphthalimide chromophore has been synthesized and in vitro activities determined. Most compounds have higher activities in HT-29 than the leader compounds Mitonafide and Amonafide. One of them (22) was selected for in vivo studies and presents an interesting activity in MX-1 and OVCAR models. (22) also acts as antitopoisomerase II.
已合成了一系列带有1,8-萘二甲酰亚胺发色团的双嵌入剂,并测定了其体外活性。大多数化合物在HT-29细胞中的活性高于先导化合物米托萘腙和氨萘非特。其中一种化合物(22)被选用于体内研究,在MX-1和OVCAR模型中表现出有趣的活性。(22)还具有抗拓扑异构酶II的作用。