Synthetic 2-Aroylindole Derivatives as a New Class of Potent Tubulin-Inhibitory, Antimitotic Agents||

…, A Lyssenko, DH Paper, J Bürgermeister…

Index: Mahboobi; Pongratz; Hufsky; Hockemeyer; Frieser; Lyssenko; Paper; Buergermeister; Boehmer; Fiebig; Burger; Baasner; Beckers Journal of Medicinal Chemistry, 2001 , vol. 44, # 26 p. 4535 - 4553

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Citation Number: 57

Abstract

A new class of simple synthetic antimitotic compounds based on 2-aroylindoles was discovered.(5-Methoxy-1 H-2-indolyl)-phenylmethanone (1) as well as analogous 3- fluorophenyl-(36) and 3-methoxyphenyl (3) derivatives displayed high cytotoxicity of IC50= 20 to 75 nM against the human HeLa/KB cervical, SK-OV-3 ovarian, and U373 astrocytoma carcinoma cell lines. The inhibition of proliferation correlated with the arrest in the G2/M ...