Potential cytotoxic and selective effect of new benzo[b]xanthenes against oral squamous cell carcinoma

Author:

Zorzanelli Bruna C1,de Queiroz Lucas N2,Santos Raíssa MA1,Menezes Luiza M2,Gomes Fernanda C2,Ferreira Vitor F3,C da Silva Fernando de1,Robbs Bruno K2

Affiliation:

1. Departamento de Química Orgânica, Instituto de Química, Campus do Valonguinho, Universidade Federal Fluminense, CEP 24020–150, Niterói-RJ, Brazil

2. Departamento de Ciência Básica, Campus Universitário de Nova Friburgo, Universidade Federal Fluminense, CEP 28625–650, Nova Friburgo-RJ, Brazil

3. Departamento de Tecnologia Farmacêutica, Faculdade de Farmácia, Universidade Federal Fluminense, R. Dr. Mario Vianna, 523, Santa Rosa, CEP 24241–002, Niterói-RJ, Brazil

Abstract

Aim: The current work shows a new synthetic methodology to obtain 21 naphthoquinones that have been evaluated against oral cavity cancer. The compounds were obtained by a three-component reaction involving lawsone, dimedone and aromatic aldehydes catalyzed by lithium chloride under microwave irradiation to produce families of 1,4- and 1,2-naphthoquinones. Results: A clonogenic assay was performed on SCC9 cell line cultures with all compounds, revealing five very active compounds. In the 3,4,5-dimethylthiazol-2,5-diphenyltetrazolium bromide cell viability assay using three different cell lines (SCC9, SCC4 and SCC25), 8c had an average IC50 of approximately 1.45 μM capable of reducing tumor cell viability, approximately 90-times higher than carboplatin.Conclusion: Therefore, the xanthene-naphthoquinone derivatives show promising bioactivity for oral cavity cancer treatment.

Publisher

Future Science Ltd

Subject

Drug Discovery,Pharmacology,Molecular Medicine

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