Bioorganic & medicinal chemistry letters

Restraining the flexibility of the central linker in terameprocol results in constrained analogs with improved growth inhibitory activity

SSH Ho, ML Go

文献索引：Ho, Sherman Si Han; Go, Mei Lin Bioorganic and Medicinal Chemistry Letters, 2013 , vol. 23, # 22 p. 6127 - 6133

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被引用次数: 5

摘要

Abstract The semi-synthetic lignan terameprocol inhibits the transcription of several inflammatory and oncogenic genes and has been evaluated for its anti-cancer properties. Here we investigated the effect of restricting the flexibility of the carbon linker connecting the terminal rings of terameprocol on its growth inhibitory activity. Conformational restriction was explored by introducing unsaturation, inserting polar entities with limited flexibility and ...