Anti-Cancer Agents in Medicinal Chemistry 2015-01-01

Synthesis of nitroaromatic compounds as potential anticancer agents.

Marcela Silva Lopes, Camila Filizzola de Andrade Sena, Bruno Leonardo Silva, Cristina Maria de Souza, Jonas Pereira Ramos, Geovanni Dantas Cassali, Elaine Maria de Souza-Fagundes, Ricardo Jose Alves, Mônica Cristina de Oliveira, Renata Barbosa de Oliveira

Index: Anticancer Agents Med. Chem. 15(2) , 206-16, (2015)

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Abstract

Twenty-seven nitrated and non-nitrated compounds have been synthesized and tested for their growth inhibitory activity on three human cancer cells lines. Fourteen compounds were able to inhibit more than 50% of the growth of at least one of the cancer cell lines and five compounds exhibited high antiproliferative activity on human cancer cell lines (IC50 < 8.5 μM). The cytotoxicity of the compounds on Vero cell line was established in vitro to evaluate the selectivity. All active compounds have a good leaving group (bromide or chloride) at the benzylic position, indicating that the mechanism of action of these compounds is related to their alkylating properties. Two compounds (3 and 24) were selected for further studies in mice with Ehrlich solid tumors and display significant antitumor effects in vivo.