Development and in vivo evaluation of fused benzazole analogs of anti-melanoma agent HA15


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Output type: Journal article

UM6P affiliated Publication?: Yes

Author list: Millet, Antoine; Filho, Mauro Safir; Hamouda-Tekaya, Nedra; Cavazza, Elisa; Abbe, Patricia; Rudiger, Johanna; Plaisant, Magali; Mayen, Julie; Rocchi, Stephane; Ronco, Cyril; Benhida, Rachid

Publisher: Future Science: Newlands Press

Publication year: 2021

Journal: Future Medicinal Chemistry (1756-8919)

Volume number: 13

Issue number: 14

ISSN: 1756-8919

Languages: English (EN-GB)


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Abstract

Background: In line with our recent discovery of an efficient anticancer thiazolebenzenesulfonamide framework HA15 (1) based on a remarkable endoplasmic reticulum stress inducement mode of action, we report herein a series of innovative constrained HA15 analogs, featuring four types of bicylic derivatives. Results: The structure-activity relationship analysis, using a cell line assay, led us to identify a novel version of HA15: a new benzothiazole derivative (10b) exhibiting important anti-melanoma effect against sensitive and resistant melanoma cells. Meanwhile, compound 10b induced a significant tumor growth inhibition in vivo with no apparent signs of toxicity. Conclusion: These results consistently open new directions to improve and develop more powerful anticancer therapeutics harboring this type of fused framework.


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Last updated on 2021-20-09 at 23:22