Issue 27, 2021
From the journal:

New Journal of Chemistry

Arylbiamidines: synthesis and structural studies en route to anticancer applications†

Oleksandr Grytsai,‡a   Leticia Christina Pires Gonçalves, ORCID logo ‡a   Rostyslav Bardovskyi,‡a   Nedra Hamouda-Tekaya,b   Stéphane Rocchi, ORCID logo b   Cyril Ronco ORCID logo *a  and  Rachid Benhida*ac  

* Corresponding authors

a Institut de Chimie de Nice CRNS UMR7272, Université Côte d’Azur, Nice, France
E-mail: cyril.ronco@univ-cotedazur.fr, rachid.benhida@univ-cotedazur.fr

b Centre Méditerranéen de Médecine Moléculaire (C3M), INSERM, U1065, Université Côte d’Azur, Nice, France

c Department of Chemical and Biochemical Sciences, Green Process Engineering, CBS, Mohamed VI Polytechnic University, UM6P, 43150 Ben Guerir, Morocco

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.

Graphical abstract: Arylbiamidines: synthesis and structural studies en route to anticancer applications

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Article information

DOI
https://doi.org/10.1039/D1NJ01943K
Article type
Communication
Submitted
21 Apr 2021
Accepted
19 May 2021
First published
27 May 2021

New J. Chem., 2021,45, 11893-11897

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Arylbiamidines: synthesis and structural studies en route to anticancer applications

O. Grytsai, L. C. P. Gonçalves, R. Bardovskyi, N. Hamouda-Tekaya, S. Rocchi, C. Ronco and R. Benhida, New J. Chem., 2021, 45, 11893 DOI: 10.1039/D1NJ01943K

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