Instituto de Investigaciones en Materiales, Universidad Nacional Autónoma de México, Apartado Postal 70-360, CU, Coyoacán, Mexico, DF, 04510, Mexico.
Molecules. 2010 Nov 9;15(11):8082-97. doi: 10.3390/molecules15118082.
This study describes the synthesis of two new families of dendrimers based on the esterification of N-alkylated 3-amine-1-propanol with two different cores, adipic acid (1st and 2nd generations) and ethylenediamine (generation 1.5), both with carboxylic acid end groups, offering a wide variety of further modifications at the periphery. According to the cytotoxic evaluation of the dendrimers and their possible degradation products within cell lines, these materials could be considered as innocuous. In preliminary studies, the synthesized dendrimers proved to be potential enhancers of solubility of highly hydrophobic drugs, like methotrexate, widely used in chemotherapy.
本研究描述了基于 N-烷基化 3-胺-1-丙醇与两种不同核心（己二酸（第一代和第二代）和乙二胺（第一代半代））的酯化反应合成的两种新型树状大分子，这两种核心都具有羧酸末端基团，为外围提供了多种进一步修饰的可能性。根据树状大分子及其在细胞系中可能的降解产物的细胞毒性评估，这些材料可被视为无害。在初步研究中，合成的树状大分子被证明是提高高度疏水性药物（如广泛用于化疗的甲氨蝶呤）溶解度的潜在增溶剂。
