Cancer chemotherapy has several limitations such as often insufficient differentiation between malign tissue and benign tissue. The clinical utility of the pyrrolo[2,1-c][1,4]benzodiazepines (PBDs) are inadequate because of the lack of selectivity for tumor tissues, high reactivity of the pharmacophoric imine functionality, low water solubility, and stability. To address these limitations two new β-glucoside prodrugs of PBDs have been synthesized and evaluated for their potential use in selective therapy of solid tumors by ADEPT. The preliminary studies reveal the prodrugs are much less toxic compared to the parent moieties. These prodrugs are activated by β-glucosidase to produce the active cytotoxic moiety signifying their utility in ADEPT of cancer. The prodrugs 1a and 1b were evaluated for their cytotoxic activity in three human cancer cell lines, i.e., A375, MCF-7 and HT-29 by employing MTT assay. The results reveal that the prodrugs have shown significant cytotoxic activity in the presence of enzyme. Another important property of these molecules is their enhanced water solubility and stability, which are essential for a molecule to be an effective drug.

癌症化学疗法具有几个局限性，例如恶性组织与良性组织之间的分化往往不足。由于缺乏对肿瘤组织的选择性，药效亚胺功能性的高反应性，低水溶性和稳定性，吡咯并[2,1- c ] [1,4]苯并二氮杂（PBDs）的临床实用性不足。为了解决这些局限性，已经合成了两种新的PBDβ-葡萄糖苷前药，并通过ADEPT评估了它们在实体瘤选择性治疗中的潜在用途。初步研究表明，与母体部分相比，前药的毒性要低得多。这些前药被β-葡糖苷酶激活以产生活性细胞毒性部分，这表明它们可用于癌症的ADEPT。前药1a和通过使用MTT测定法评估1b在三种人癌细胞系，即A375，MCF-7和HT-29中的细胞毒性活性。结果表明，在存在酶的情况下，前药已显示出显着的细胞毒性活性。这些分子的另一个重要特性是其增强的水溶性和稳定性，这对于分子成为有效药物至关重要。