The 2-(3,4,5-trimethoxybenzoyl)-2-aminoindole nucleus was used as the fundamental structure for the synthesis of compounds modified with respect to positions C-4 to C-7 with different moieties (chloro, methyl, or methoxy). Additional structural variations concerned the indole nitrogen, which was alkylated with small alkyl groups such as methyl or ethyl. We have identified 1-methyl-2-(3,4,5-trimethoxybenzoyl)-3-amino-7-methoxyindole as a new highly potent antiproliferative agent that targets tubulin at the colchicine binding site and leads to apoptotic cell death.

ROMAGNOLI R, BARALDI PG, SARKAR T, CARRION MD, CARA CL, CRUZ-LOPEZ O, et al. (2008). Synthesis and Biological Evaluation of 1-Methyl-2-(3',4',5'-trimethoxybenzoyl)-3-aminoindoles as a New Class of Antimitotic Agents and Tubulin Inhibitors. JOURNAL OF MEDICINAL CHEMISTRY, Mar13;51(5), 1464-1468 [10.1021/jm7011547].

Synthesis and Biological Evaluation of 1-Methyl-2-(3',4',5'-trimethoxybenzoyl)-3-aminoindoles as a New Class of Antimitotic Agents and Tubulin Inhibitors

GRIMAUDO, Stefania;DI CRISTINA, Antonietta;
2008-01-01

Abstract

The 2-(3,4,5-trimethoxybenzoyl)-2-aminoindole nucleus was used as the fundamental structure for the synthesis of compounds modified with respect to positions C-4 to C-7 with different moieties (chloro, methyl, or methoxy). Additional structural variations concerned the indole nitrogen, which was alkylated with small alkyl groups such as methyl or ethyl. We have identified 1-methyl-2-(3,4,5-trimethoxybenzoyl)-3-amino-7-methoxyindole as a new highly potent antiproliferative agent that targets tubulin at the colchicine binding site and leads to apoptotic cell death.
2008
ROMAGNOLI R, BARALDI PG, SARKAR T, CARRION MD, CARA CL, CRUZ-LOPEZ O, et al. (2008). Synthesis and Biological Evaluation of 1-Methyl-2-(3',4',5'-trimethoxybenzoyl)-3-aminoindoles as a New Class of Antimitotic Agents and Tubulin Inhibitors. JOURNAL OF MEDICINAL CHEMISTRY, Mar13;51(5), 1464-1468 [10.1021/jm7011547].
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/10447/34018
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