Total Synthesis of Prostaglandin 15d-PGJ2 and Investigation of its Effect on the Secretion of IL-6 and IL-12

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• 作者：Julian Egger ; Stefan Fischer ; Peter Bretscher ; Stefan Freigang ; Manfred Kopf ; Erick M. Carreira
• 刊名：Organic Letters
• 出版年：2015
• 出版时间：September 4, 2015
• 年：2015
• 卷：17
• 期：17
• 页码：4340-4343
• 全文大小：362K
• ISSN：1523-7052

文摘

An efficient synthesis of 15-deoxy-螖12,14-prostaglandin J₂ (15d-PGJ₂, 1) is reported. The route described allows for diversification of the parent structure to prepare seven analogues of 1 in which the positioning of electrophilic sites is varied. These analogues were tested in SAR studies for their ability to reduce the secretion of proinflammatory cytokines. It was shown that the endocyclic enone is crucial for the bioactivity investigated and that the conjugated 蠅-side chain serves in a reinforcing manner.