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

Stefania Grimaudo; Carlota Lopez Cara; Olga Cruz-Lopez; Nicola Zonta; Taradas Sarkar; Ernest Hamel; Mojgan Aghazadeh Tabrizi; Jan Balzarini; Andrea Brancale; Delia Preti; Maria Dora Carrion; Pier Giovanni Baraldi; Romeo Romagnoli; Hsing-Pang Hsieh; Antonietta Di Cristina

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

Stefania Grimaudo, Carlota Lopez Cara, Olga Cruz-Lopez, Nicola Zonta, Taradas Sarkar, Ernest Hamel, Mojgan Aghazadeh Tabrizi, Jan Balzarini, Andrea Brancale, Delia Preti, Maria Dora Carrion, Pier Giovanni Baraldi, Romeo Romagnoli, Hsing-Pang Hsieh, Antonietta Di Cristina

Promozione della Salute, Materno-Infantile, di Medicina Interna e Specialistica di Eccellenza “G. D’Alessandro”

Risultato della ricerca: Article › peer review

82 Citazioni (Scopus)

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.

Lingua originale	English
pagine (da-a)	1464-1468
Rivista	Journal of Medicinal Chemistry
Volume	Mar13;51(5)
Stato di pubblicazione	Published - 2008

All Science Journal Classification (ASJC) codes

Molecular Medicine
Drug Discovery

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Cita questo

Grimaudo, S., Cara, C. L., Cruz-Lopez, O., Zonta, N., Sarkar, T., Hamel, E., Tabrizi, M. A., Balzarini, J., Brancale, A., Preti, D., Carrion, M. D., Baraldi, P. G., Romagnoli, R., Hsieh, H-P., & Di Cristina, A. (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.

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; Cara, Carlota Lopez; Cruz-Lopez, Olga; Zonta, Nicola; Sarkar, Taradas; Hamel, Ernest; Tabrizi, Mojgan Aghazadeh; Balzarini, Jan; Brancale, Andrea; Preti, Delia; Carrion, Maria Dora; Baraldi, Pier Giovanni; Romagnoli, Romeo; Hsieh, Hsing-Pang; Di Cristina, Antonietta.

In: Journal of Medicinal Chemistry, Vol. Mar13;51(5), 2008, pag. 1464-1468.

Risultato della ricerca: Article › peer review

Grimaudo, S, Cara, CL, Cruz-Lopez, O, Zonta, N, Sarkar, T, Hamel, E, Tabrizi, MA, Balzarini, J, Brancale, A, Preti, D, Carrion, MD, Baraldi, PG, Romagnoli, R, Hsieh, H-P & Di Cristina, A 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, vol. Mar13;51(5), pagg. 1464-1468.

Grimaudo, Stefania ; Cara, Carlota Lopez ; Cruz-Lopez, Olga ; Zonta, Nicola ; Sarkar, Taradas ; Hamel, Ernest ; Tabrizi, Mojgan Aghazadeh ; Balzarini, Jan ; Brancale, Andrea ; Preti, Delia ; Carrion, Maria Dora ; Baraldi, Pier Giovanni ; Romagnoli, Romeo ; Hsieh, Hsing-Pang ; Di Cristina, Antonietta. / Synthesis and Biological Evaluation of 1-Methyl-2-(3',4',5'-trimethoxybenzoyl)-3-aminoindoles as a New Class of Antimitotic Agents and Tubulin Inhibitors. In: Journal of Medicinal Chemistry. 2008 ; Vol. Mar13;51(5). pagg. 1464-1468.

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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.",

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AU - Cruz-Lopez, Olga

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AU - Sarkar, Taradas

AU - Hamel, Ernest

AU - Tabrizi, Mojgan Aghazadeh

AU - Balzarini, Jan

AU - Brancale, Andrea

AU - Preti, Delia

AU - Carrion, Maria Dora

AU - Baraldi, Pier Giovanni

AU - Romagnoli, Romeo

AU - Hsieh, Hsing-Pang

AU - Di Cristina, Antonietta

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AB - 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.

UR - http://hdl.handle.net/10447/34018

M3 - Article

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