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Synthesis and Biological Evaluation of Subglutinol Analogs for Immunomodulatory Agents.
Journal of Medicinal Chemistry ( IF 7.3 ) Pub Date : 2019-12-18 , DOI: 10.1021/acs.jmedchem.9b01579
Hyeri Park 1 , Laura S Christian , Mi Jung Kim 1 , Qi-Jing Li , Jiyong Hong 1
Affiliation  

Autoimmune diseases are chronic inflammatory diseases associated with high morbidity and mortality. Treatment options for autoimmune diseases have increased over the past several decades, but they are, in general, limited in their clinical efficacy due to high toxicity and lack of selectivity. Thus, efforts must be made to identify new immunomodulatory agents that are effective through a novel mechanism to circumvent existing side effects. To define the structural requirements of subglutinols for immunomodulatory activity and to provide guiding principles on future therapeutic development, we prepared and evaluated several subglutinol analogs for their immunomodulatory activities. Our efforts identified a subglutinol analog with reduced structural complexity as a potential lead compound for future autoimmune drug development. Our study will provide an important framework for the design of potent and nontoxic immunomodulating agents derived from subglutinols.

中文翻译:

次戊二酚类似物的免疫调节剂的合成及生物学评价。

自身免疫性疾病是与高发病率和高死亡率相关的慢性炎症性疾病。在过去的几十年中,自身免疫性疾病的治疗选择有所增加,但是由于高毒性和缺乏选择性,它们的临床疗效普遍受到限制。因此,必须努力确定通过新机制有效规避现有副作用的新的免疫调节剂。为了定义亚谷蛋白的免疫调节活性的结构要求,并为将来的治疗发展提供指导原则,我们准备并评估了几种亚谷蛋白类似物的免疫调节活性。我们的努力确定了结构复杂性降低的谷胱甘肽类似物作为未来自身免疫药物开发的潜在先导化合物。
更新日期:2019-12-19
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