Abstract
| - A novel series of 3-alkyl-substituted 7-phenyl-3H-pyrrolo[3,2-f]quinolin-9-ones (7-PPyQs) was synthesizedwith the aim to optimize the cytotoxic activity of recently identified PPyQs, promising inhibitors of tubulinpolymerization. All compounds inhibited the growth of 11 human tumor cell lines at submicromolarconcentrations as well as two human resistant cancer sublines, A549-T12 and A549-T24. FACS analysisindicated that all compounds caused significant arrest of the A549 cell cycle in G2/M phase at 0.1 and 1 μMand a good correlation between the cytotoxicity IC50 and their ability to block the cell cycle was observed.
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