The 2-(3,4,5-trimethoxybenzoyl)-2-aminoindole nucleus was used as the fundamental structure for the synthesis of compds. modified with respect to positions C-4 to C-7 with different moieties (chloro, Me, or methoxy). Addnl. structural variations concerned the indole nitrogen, which was alkylated with small alkyl groups such as Me or Et. 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.

Synthesis and Biological Evaluation of 1-Methyl-2-(3’,4’,5’-Trimethoxybenzoyl)-3-Amino Indoles as a New Class of Antimitotic Agents and Tubulin Inhibitors

ROMAGNOLI, Romeo;BARALDI, Pier Giovanni;PRETI, Delia;AGHAZADEH TABRIZI, Mojgan;
2008

Abstract

The 2-(3,4,5-trimethoxybenzoyl)-2-aminoindole nucleus was used as the fundamental structure for the synthesis of compds. modified with respect to positions C-4 to C-7 with different moieties (chloro, Me, or methoxy). Addnl. structural variations concerned the indole nitrogen, which was alkylated with small alkyl groups such as Me or Et. 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, Romeo; Baraldi, Pier Giovanni; Sarkar, T.; Carrion, M. D.; Lopez Cara, C.; Cruz Lopez, O.; Preti, Delia; AGHAZADEH TABRIZI, Mojgan; Tolomeo, M.; Grimaudo, S.; Di Cristina, A.; Zonta, N.; Balzarini, J.; Brancale, A.; Hsieh, H. P.; Hamel, E.
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11392/530085
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