Preliminary biological evaluation and mechanism of action studies of selected 2-arylindoles against glioblastoma

Saurabh Prabhu; Zaheer Akbar; Frederick Harris; Katherine Karakoula; Robert Lea; Farzana Rowther; Tracy Warr; Timothy Snape

doi:10.1016/j.bmc.2013.01.032

Preliminary biological evaluation and mechanism of action studies of selected 2-arylindoles against glioblastoma

Saurabh Prabhu, Zaheer Akbar, Frederick Harris, Katherine Karakoula, Robert Lea, Farzana Rowther, Tracy Warr, Timothy Snape

School of Pharmacy

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

9 Citations (Scopus)

Abstract

A series of related 2-arylindoles have been evaluated for their anticancer activity against a range of glioblastoma cell lines using a number of different cell-based assays to determine cell viability after treatment with the compounds. The best indoles, which showed comparable activity to cisplatin against a U87MG cell line in the MTS assay, were taken forward and initial studies suggest that their mechanism of action is consistent with the generation of reactive oxygen species followed by autophagic cell death. Furthermore, activity was also observed in glioblastoma short-term cell cultures for the best lead compound and in some cases gave low micromolar IC50s.

Original language	English
Pages (from-to)	1918-1924
Number of pages	7
Journal	Bioorganic & Medicinal Chemistry
Volume	21
Issue number	7
Early online date	1 Feb 2013
DOIs	https://doi.org/10.1016/j.bmc.2013.01.032
Publication status	Published - 1 Apr 2013

Keywords

2-Arylindoles
Glioblastoma
Reactive oxygen species (ROS)
Autophagy
Cancer

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

Access to Document

10.1016/j.bmc.2013.01.032

Cite this

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title = "Preliminary biological evaluation and mechanism of action studies of selected 2-arylindoles against glioblastoma",

abstract = "A series of related 2-arylindoles have been evaluated for their anticancer activity against a range of glioblastoma cell lines using a number of different cell-based assays to determine cell viability after treatment with the compounds. The best indoles, which showed comparable activity to cisplatin against a U87MG cell line in the MTS assay, were taken forward and initial studies suggest that their mechanism of action is consistent with the generation of reactive oxygen species followed by autophagic cell death. Furthermore, activity was also observed in glioblastoma short-term cell cultures for the best lead compound and in some cases gave low micromolar IC50s.",

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Preliminary biological evaluation and mechanism of action studies of selected 2-arylindoles against glioblastoma. / Prabhu, Saurabh; Akbar, Zaheer; Harris, Frederick; Karakoula, Katherine; Lea, Robert; Rowther, Farzana; Warr, Tracy; Snape, Timothy.

In: Bioorganic & Medicinal Chemistry, Vol. 21, No. 7, 01.04.2013, p. 1918-1924.

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

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AU - Akbar, Zaheer

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AU - Rowther, Farzana

AU - Warr, Tracy

AU - Snape, Timothy

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