Arylbiamidines: synthesis and structural studies en route to anticancer applications


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Output type: Journal article

UM6P affiliated Publication?: Yes

Author list: Grytsai, Oleksandr; Goncalves, Leticia Christina Pires; Bardovskyi, Rostyslav; Hamouda-Tekaya, Nedra; Rocchi, Stephane; Ronco, Cyril; Benhida, Rachid

Publisher: Royal Society of Chemistry

Publication year: 2021

Journal: New Journal of Chemistry (1144-0546)

Volume number: 45

Issue number: 27

ISSN: 1144-0546

eISSN: 1369-9261

Languages: English (EN-GB)


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Abstract

Biamidines are a unique and poorly studied class of nitrogenous compounds prone to tautomerization and H-bonding. Four series of heteroaryl diarylbiamidines were synthesized and the antimelanoma activity and physicochemical properties of the resulting 37 new compounds were evaluated. The dimethylthiazolyl 3-bromophenyl biamidine derivative B6 inhibits the growth of six different melanoma cell lines, having higher activity than the positive control drug, the B-RAF inhibitor PLX4032. This study introduces diarylbiamidines as promising frameworks for drug discovery.


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Last updated on 2021-12-09 at 23:21