Novel benzylidene-9 (10 H)-anthracenones as highly active antimicrotubule agents. Synthesis, antiproliferative activity, and inhibition of tubulin polymerization

…, T Hirano, T Stoiber, JA Camacho Gomez…

Index: Prinz, Helge; Ishii, Yukihito; Hirano, Takeo; Stoiber, Thomas; Camacho Gomez, Juan A.; Schmidt, Peter; Duessmann, Heiko; Burger, Angelika M.; Prehn, Jochen H. M.; Guenther, Eckhard G.; Unger, Eberhard; Umezawa, Kazuo Journal of Medicinal Chemistry, 2003 , vol. 46, # 15 p. 3382 - 3394

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Citation Number: 61

Abstract

A novel series of 10-benzylidene-9 (10 H)-anthracenones and 10-(phenylmethyl)-9 (10 H)- anthracenones were synthesized and evaluated for antiproliferative activity in an assay based on K562 leukemia cells. The 3-hydroxy-4-methoxybenzylidene analogue 9h was found to be the most active compound (IC50 K562: 20 nM). Structure-activity relationships are also considered. The highly active compound 9h and the 2, 4-dimethoxy-3- ...