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Investigational New Drugs
Published in: Investigational New Drugs 3/2020

Open Access 01-06-2020 | Melanoma | PRECLINICAL STUDIES

Anticancer activity of a novel methylated analogue of L-mimosine against an in vitro model of human malignant melanoma

Authors: Sotiris Kyriakou, Melina Mitsiogianni, Theodora Mantso, William Cheung, Stephen Todryk, Stephany Veuger, Aglaia Pappa, David Tetard, Mihalis I. Panayiotidis

Published in: Investigational New Drugs | Issue 3/2020

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Summary

The anticancer activity of a series of novel synthesized, hydroxypyridone-based metal chelators (analogues of L-mimosine) was evaluated in an in vitro model of melanoma consisting of malignant melanoma (A375), non-melanoma epidermoid carcinoma (A431) and immortalized non-malignant keratinocyte (HaCaT) cells. More specifically, we have demonstrated that the L-enantiomer of a methylated analogue of L-mimosine (compound 22) can exert a potent anticancer effect in A375 cells when compared to either A431 or HaCaT cells. Moreover, we have demonstrated that this analogue has the ability to i) promote increased generation of reactive oxygen species (ROS), ii) activate both intrinsic and extrinsic apoptosis and iii) induce perturbations in cell cycle growth arrest. Our data highlights the potential of compound 22 to act as a promising therapeutic agent against an in vitro model of human malignant melanoma.
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Metadata
Title
Anticancer activity of a novel methylated analogue of L-mimosine against an in vitro model of human malignant melanoma
Authors
Sotiris Kyriakou
Melina Mitsiogianni
Theodora Mantso
William Cheung
Stephen Todryk
Stephany Veuger
Aglaia Pappa
David Tetard
Mihalis I. Panayiotidis
Publication date
01-06-2020
Publisher
Springer US
Published in
Investigational New Drugs / Issue 3/2020
Print ISSN: 0167-6997
Electronic ISSN: 1573-0646
DOI
https://doi.org/10.1007/s10637-019-00809-0

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