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Tetrahedron

Anti-tuberculosis natural products: synthesis and biological evaluation of pyridoacridine alkaloids related to ascididemin

DR Appleton, AN Pearce, BR Copp

文献索引:Appleton, David R.; Pearce, A. Norrie; Copp, Brent R. Tetrahedron, 2010 , vol. 66, # 27-28 p. 4977 - 4986

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被引用次数: 23

摘要

There is an urgent need for novel therapeutics possessing new modes of action to treat tuberculosis (TB) infections. In this study we report on the synthesis and biological evaluation of a series of pyrido [2, 3, 4-kl] acridin-6-one alkaloids related to the anti-TB (MIC 0.35 μM) but cytotoxic (IC50< 0.14 μM) marine natural product ascididemin (1). The most interesting compounds identified were 21 and 24, which were found to inhibit the growth ...