Antitumor activity of new substituted 3-(5-imidazo[2,1-b] thiazolylmethylene)-2-indolinones and study of their effect on the cell cycle

Aldo Andreani; Massimiliano Granaiola; Alberto Leoni; Alessandra Locatelli; Rita Morigi; Mirella Rambaldi; Vida Garaliene; William Welsh; Sonia Arora; Giovanna Farruggia; Lanfranco Masotti

doi:10.1021/jm050353e

Antitumor activity of new substituted 3-(5-imidazo[2,1-b] thiazolylmethylene)-2-indolinones and study of their effect on the cell cycle

Aldo Andreani, Massimiliano Granaiola, Alberto Leoni, Alessandra Locatelli, Rita Morigi, Mirella Rambaldi, Vida Garaliene, William Welsh, Sonia Arora, Giovanna Farruggia, Lanfranco Masotti

Robert Wood Johnson Medical School (RWJMS), Pharmacology

Research output: Contribution to journal › Article › peer-review

52 Scopus citations

Abstract

This paper reports the synthesis of a new series of 3-(5-imidazo[2,1-6] thiazolylmethylene)-2-indolinones which were tested as potential antitumor agents at the National Cancer Institute. Two derivatives are now under review by BEC (Biological Evaluation Committee of NCI). To investigate the mechanism of action, the effect on cell cycle progression was studied by monitoring them in colon adenocarcinoma HT-29: both were able to block HT-29 in mitosis. 3-[(2,6-Dimethylimidazo[2,1-b]thiazol-5-yl)methylene]-5-chloro-2-indolinone was the most active compound.

Original language	English (US)
Pages (from-to)	5604-5607
Number of pages	4
Journal	Journal of medicinal chemistry
Volume	48
Issue number	17
DOIs	https://doi.org/10.1021/jm050353e
State	Published - Aug 25 2005

All Science Journal Classification (ASJC) codes

Molecular Medicine
Drug Discovery

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Andreani, A., Granaiola, M., Leoni, A., Locatelli, A., Morigi, R., Rambaldi, M., Garaliene, V., Welsh, W., Arora, S., Farruggia, G., & Masotti, L. (2005). Antitumor activity of new substituted 3-(5-imidazo[2,1-b] thiazolylmethylene)-2-indolinones and study of their effect on the cell cycle. Journal of medicinal chemistry, 48(17), 5604-5607. https://doi.org/10.1021/jm050353e

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title = "Antitumor activity of new substituted 3-(5-imidazo[2,1-b] thiazolylmethylene)-2-indolinones and study of their effect on the cell cycle",

abstract = "This paper reports the synthesis of a new series of 3-(5-imidazo[2,1-6] thiazolylmethylene)-2-indolinones which were tested as potential antitumor agents at the National Cancer Institute. Two derivatives are now under review by BEC (Biological Evaluation Committee of NCI). To investigate the mechanism of action, the effect on cell cycle progression was studied by monitoring them in colon adenocarcinoma HT-29: both were able to block HT-29 in mitosis. 3-[(2,6-Dimethylimidazo[2,1-b]thiazol-5-yl)methylene]-5-chloro-2-indolinone was the most active compound.",

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Andreani, A, Granaiola, M, Leoni, A, Locatelli, A, Morigi, R, Rambaldi, M, Garaliene, V, Welsh, W, Arora, S, Farruggia, G & Masotti, L 2005, 'Antitumor activity of new substituted 3-(5-imidazo[2,1-b] thiazolylmethylene)-2-indolinones and study of their effect on the cell cycle', Journal of medicinal chemistry, vol. 48, no. 17, pp. 5604-5607. https://doi.org/10.1021/jm050353e

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T1 - Antitumor activity of new substituted 3-(5-imidazo[2,1-b] thiazolylmethylene)-2-indolinones and study of their effect on the cell cycle

AU - Andreani, Aldo

AU - Granaiola, Massimiliano

AU - Leoni, Alberto

AU - Locatelli, Alessandra

AU - Morigi, Rita

AU - Rambaldi, Mirella

AU - Garaliene, Vida

AU - Welsh, William

AU - Arora, Sonia

AU - Farruggia, Giovanna

AU - Masotti, Lanfranco

PY - 2005/8/25

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Antitumor activity of new substituted 3-(5-imidazo[2,1-b] thiazolylmethylene)-2-indolinones and study of their effect on the cell cycle

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