a a Departament of Química Orgánica , Instituto de Química, Universidad Nacional Autónoma de México , Ciudad de México , Mexico.
b b Departament of Biología , Facultad de Química, Universidad Nacional Autónoma de México , Ciudad de México , Mexico.
Drug Dev Ind Pharm. 2019 Apr;45(4):683-688. doi: 10.1080/03639045.2019.1569036. Epub 2019 Jan 28.
A possible way of improving the activity and selectivity profile of antitumor agents is to design drug carrier systems employing soluble macromolecules. Thus, four resorcinarene-PAMAM-dendrimer conjugates of chlorambucil with different groups in the lower part of the macrocycle and different length dendritic arms showed a good stability of the chemical link between drug and spacer. Evaluation of the cytotoxicity of the resorcinarene-PAMAM-dendrimer-chlorambucil conjugate employing a sulforhodamine B (SRB) assay in K-562 (human chronic myelogenous leukemia cells) demonstrated that the conjugate was more potent as an antiproliferative agent than chlorambucil.
提高抗肿瘤药物的活性和选择性的一种可能方法是设计使用可溶性大分子的药物载体系统。因此，具有不同大环下部基团和不同长度树枝状臂的四种氯丁基-泊洛沙姆-树枝状大分子缀合物显示出药物和间隔物之间化学键的良好稳定性。采用磺基罗丹明 B（SRB）测定法在 K-562（人慢性髓性白血病细胞）中评价了杯芳烃-PAMAM-树枝状大分子-氯丁基缀合物的细胞毒性，结果表明该缀合物作为增殖抑制剂比氯丁基更有效。
