作者:Christiane Contino-Pépin、Audrey Parat、Cindy Patinote、Wendi A. Roscoe、Stephen J. Karlik、Bernard Pucci
DOI:10.1002/cmdc.201000326
日期:2010.12.3
mechanism‐of‐action of thalidomide remains uncertain and might differ between diseases and under different clinical condition. With implications in the treatment of a variety of inflammatory and autoimmune diseases, as well as for use as an anticancer agent, alone or in combination with established therapeutics, it is clear that thalidomide and its derivatives deserve further scrutiny. In particular, thalidomide was
沙利度胺的确切作用机制仍不确定,并且在疾病之间以及在不同的临床条件下可能会有所不同。单独或与已确立的疗法联合用于治疗多种炎性和自身免疫性疾病,以及用作抗癌剂,显然沙利度胺及其衍生物值得进一步研究。特别地,沙利度胺在多发性硬化症(MS)的小鼠模型中是有效的,MS是一种自身免疫性炎性疾病,称为实验性自身免疫性脑脊髓炎(EAE)。在这里,我们描述了在邻苯二甲酰亚胺环上带有氨基烷基的沙利度胺的新大分子前药的合成和初步生物学评估。研究了这些化合物限制EAE的有效性,结果表明,-1沙利度胺等效剂量,他们废除了EAE的临床和病理特征。