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首页> 外文期刊>Medicinal chemistry >Synthesis, cytotoxic evaluation and in silico pharmacokinetic prediction of some benzo(a)phenazine-5-sulfonic acid derivatives.
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Synthesis, cytotoxic evaluation and in silico pharmacokinetic prediction of some benzo(a)phenazine-5-sulfonic acid derivatives.

机译：一些苯并（a）吩嗪-5-磺酸衍生物的合成，细胞毒性评估和计算机模拟药物动力学。

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摘要

Cancer is one of the life threatening diseases and the development of novel anticancer molecules is limited by many reasons. In the present investigation, some novel benzo[a]phenazine-5-sulfonic acid derivatives as DNA intercalator was designed with optimized pharmacokinetic features for cancer treatment. The compounds with desired pharmacokinetic profile were synthesized and structurally characterized. Cytotoxic activity study against HL-60 tumor cell lines shows that 10-dimethyl carboxamido derivative of benzo[a]phenazine-5-sulfonic acid is found to be the most active in the series with cytotoxic activity (IC(50) = 19 microM) comparable to cisplatin (IC(50) = 7 microM). The study concluded that the novel benzo[a]phenazine-5-sulfonic acid derivatives were found to have enhanced DNA binding affinity and exhibited significant activity in vitro against HL-60 cell lines. This work will also guide for further development of effective DNA intercalators for cancer treatment.
机译：癌症是威胁生命的疾病之一，新型抗癌分子的发展受到许多原因的限制。在本研究中，设计了一些具有优化的药代动力学特征的新型苯并[a]吩嗪-5-磺酸衍生物作为DNA嵌入剂用于癌症治疗。具有所需药代动力学特征的化合物被合成并在结构上表征。对HL-60肿瘤细胞系的细胞毒活性研究表明，苯并[a]吩嗪-5-磺酸的10-二甲基羧酰胺衍生物被发现在具有细胞毒活性的系列中最活跃（IC（50）= 19 microM）相当于顺铂（IC（50）= 7 microM）。研究得出的结论是，新型苯并[a]吩嗪-5-磺酸衍生物具有增强的DNA结合亲和力，并在体外对HL-60细胞系表现出显着的活性。这项工作还将指导进一步开发用于癌症治疗的有效DNA嵌入剂。

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