Tetrahedron

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

DR Appleton, AN Pearce, BR Copp

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

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Citation Number: 23

Abstract

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 ...