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Anticancer effects of the Novel Pyrazolyl-Urea GeGe-3

Williams, Ashleigh; Cooper, Emma; Clark, Bethany; Perry, Laura; Ponassi, Marco; Iervasi, Erika; Brullo, Chiara; Greenhough, Alexander; Ladomery, Michael

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Authors

Ashleigh Williams

Emma Cooper

Bethany Clark

Laura Perry

Marco Ponassi

Erika Iervasi

Chiara Brullo



Abstract

In a screen of over 200 novel pyrazole compounds, ethyl 1-(2-hydroxypentyl)-5-(3-(3-(trifluoromethyl) phenyl)ureido)-1H-pyrazole-4-carboxylate (named GeGe-3) has emerged as a potential anticancer compound. GeGe-3 displays potent anti-angiogenic properties through the presumptive targeting of the protein kinase DMPK1 and the Ca2+-binding protein calreticulin. We further explored the anticancer potential of GeGe-3 on a range of established cancer cell lines, including PC3 (prostate adenocarcinoma), SKMEL-28 (cutaneous melanoma), SKOV-3 (ovarian adenocarcinoma), Hep-G2 (hepatocellular carcinoma), MDA-MB231, SKBR3, MCF7 (breast adenocarcinoma), A549 (lung carcinoma), and HeLa (cervix epithelioid carcinoma). At concentrations in the range of 10 μM, GeGe-3 significantly restricted cell proliferation and metabolism. GeGe-3 also reduced PC3 cell migration in a standard wound closure and trans-well assay. Together, these results confirm the anticancer potential of GeGe-3 and underline the need for more detailed pre-clinical investigations into its molecular targets and mechanisms of action.

Journal Article Type Article
Acceptance Date May 10, 2024
Online Publication Date May 15, 2024
Publication Date May 15, 2024
Deposit Date May 15, 2024
Publicly Available Date May 15, 2024
Journal International Journal of Molecular Sciences
Print ISSN 1661-6596
Electronic ISSN 1422-0067
Publisher MDPI
Peer Reviewed Peer Reviewed
Volume 25
Issue 10
Article Number 5380
DOI https://doi.org/10.3390/ijms25105380
Keywords pyrazole; novel anticancer drugs; cell proliferation; cell migration
Public URL https://uwe-repository.worktribe.com/output/11989250
Additional Information The article is part of a Special Issue entitled "ynthesis and Biological Evaluation of Pyrazole Derivatives"

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