Abstract：
Fluorescent cytotoxic compounds with readout delivery are crucial in chemotherapy. The growing demands of these treatment strategies require the novel heterocyclic molecules with better selectivity alongside fluorescence marker potential. In this context, a series of nine isatin Schiff base derivatives 4a-i were synthesized, characterized and evaluated for UV-visible, fluorescence, thermal and bioanalysis in order to explore the effect of structure on their bioprofiles. The analogue 4d exhibited maximum cytotoxic activity on Hella cells with percentage inhibition of 83% at 50 µM and 100% at 150 µM concentrations while 4c showed minimum cytotoxic activity with the value of 19% at 50 µM and 22% at 150 µM concentrations. Meanwhile, 4g was found to exhibit maximum inhibition potential towards Vero Cells with the percentage inhibition values of 83 at 50 µM concentration. The overall SAR study showed that the para-fluoro-substituted isatin moieties exhibited the appreciable percentage inhibition while the least activity was delivered by the isatin derivatives with para-bromo substitution.
摘要：
具有读出递送的荧光细胞毒性化合物在化疗中是至关重要的。这些处理策略的日益增长的需求需要具有更好的选择性以及荧光标记潜力的新型杂环分子。在这种情况下，合成了一系列9种IsatinSchiff碱衍生物4a-i，表征和评估UV可见光，荧光，热和生物分析，以探索结构对其生物特征的影响。类似物4d对Hella细胞表现出最大的细胞毒性活性，在50µM浓度下的抑制百分比为83％，在150µM浓度下的抑制百分比为100％，而4c表现出最小的细胞毒性活性，在50µM浓度下的值为19％，在150µM浓度下的值为22％。同时,发现4g对Vero细胞表现出最大的抑制潜力，在50μM浓度下的抑制百分比值为83。总体SAR研究表明，对氟取代的Isatin部分表现出明显的抑制百分比，而具有对溴取代的Isatin衍生物的活性最低。
