Synthesis of Nitroaromatic Compounds as Potential Anticancer Agents

ISSN: 1875-5992 (Online)
ISSN: 1871-5206 (Print)


Volume 16, 12 Issues, 2016


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Anti-Cancer Agents in Medicinal Chemistry

Formerly: Current Medicinal Chemistry - Anti-Cancer Agents

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  • 27th of 59 in Chemistry, Medicinal

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Editor-in-Chief:
Michelle Prudhomme
Universite Blaise Pascal - C.N.R.S
Aubiere Cedex
France


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Synthesis of Nitroaromatic Compounds as Potential Anticancer Agents



Anti-Cancer Agents in Medicinal Chemistry, 15(2): 206-216.

Author(s): 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 and Renata Barbosa de Oliveira.

Affiliation: Department of Pharmaceutical Products, Pharmacy Faculty, Federal University of Minas Gerais, Belo Horizonte, Minas Gerais, Brazil.

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.




Keywords:

Antitumor activity, alkylating agents, bioreduction, cytotoxicity, nitrocompounds, solid tumor.



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Article Details

Volume: 15
Issue Number: 2
First Page: 206
Last Page: 216
Page Count: 11
DOI: 10.2174/1871520614666141114201749
Price: $58
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