Fuska J, Fusková A, Proksa B
Pharmazie. 1982 Jun;37(6):443-5.
The in vitro cytotoxic effect on leukemia P 388 cells of new derivatives, 7,8-dihydro-5H-isoindolo[1,2-b] [3] benzazepine-5-ones substituted at position was evaluated. The most effective were the derivatives which were substituted at position 7 by the dimethylamino, hydroxy and/or ethoxy group. These substances selectively inhibited incorporation only of 14C-uridine into P 388 cells fractions. Substance 7 which was studied more intensively stopped the proliferation of P 388 cells in vitro, but caused only a slight killing effect. The maximum inhibitory effect of this substance on P 388 cells is related to the G1/S phase of the cell cycle. In in vitro test, the substance showed synergism with the cytostatics: cycloheximide, methotrexate and vermiculin, their phase of greatest lethal activity also being G1/S or early S.
评估了在特定位置被取代的新型衍生物7,8 - 二氢 - 5H - 异吲哚并[1,2 - b][3]苯并氮杂䓬 - 5 - 酮对白血病P 388细胞的体外细胞毒性作用。最有效的是在7位被二甲氨基、羟基和/或乙氧基取代的衍生物。这些物质仅选择性地抑制14C - 尿苷掺入P 388细胞组分。对其研究更深入的物质7在体外可阻止P 388细胞的增殖，但仅产生轻微的杀伤作用。该物质对P 388细胞的最大抑制作用与细胞周期的G1/S期相关。在体外试验中，该物质与细胞抑制剂：环己酰亚胺、甲氨蝶呤和绿霉素表现出协同作用，它们最大致死活性的阶段也是G1/S或早期S期。
