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基于海藻糖-6,6'-二咖啡酰基海藻酸结构-活性关系研发免疫刺激剂威他霉素。

Development of vizantin, a safe immunostimulant, based on the structure-activity relationship of trehalose-6,6'-dicorynomycolate.

机构信息

Faculty of Pharmaceutical Sciences, Tokushima Bunri University, Yamashiro-cho, Tokushima 770-8514, Japan.

出版信息

J Med Chem. 2013 Jan 10;56(1):381-5. doi: 10.1021/jm3016443. Epub 2012 Dec 19.

Abstract

Vizantin, 6,6'-bis-O-(3-nonyldodecanoyl)-α,α'-trehalose, was developed as a safe immunostimulator on the basis of a structure-activity relationship (SAR) study with trehalose 6,6'-dicorynomycolate (TDCM). It was possible to synthesize vizantin on a large scale more easily than in the case of TDCM, and the compound exhibited more potent prophylactic effect on experimental lung metastasis of B16-F0 melanoma cells. Because vizantin stimulated human macrophages, it is a promising candidate for clinical application.

摘要

Vizantin,6,6'-双-O-(3-正壬基十二烷酰基)-α,α'-海藻糖,是基于海藻糖 6,6'-二肉豆蔻酰基醚(TDCM)的构效关系(SAR)研究开发的一种安全免疫刺激剂。与 TDCM 相比,vizantin 更容易大规模合成,并且该化合物对 B16-F0 黑色素瘤细胞实验性肺转移具有更强的预防作用。由于 vizantin 能刺激人巨噬细胞,因此它是一种很有前途的临床应用候选药物。

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