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

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Original languageEnglish
Pages (from-to)621-633
JournalInvestigational New Drugs
Volume38
Issue number3
Early online date26 Jun 2019
DOIs
Publication statusPublished - 1 Jun 2020
Publication type

Research output: Contribution to journalArticle

Abstract

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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