Synthesis and preliminary pharmacological evaluation of new (+/-) 1,4-naphthoquinones structurally related to lapachol |
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| Authors: | da Silva Alcides J M Buarque Camilla D Brito Flávia V Aurelian Laure Macedo Luciana F Malkas Linda H Hickey Robert J Lopes Daniele V S Noël François Murakami Yugo L B Silva Noelson M V Melo Paulo A Caruso Rodrigo R B Castro Newton G Costa Paulo R R |
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| Institution: | Laboratório de Química Bioorganica (LQB), Núcleo de Pesquisas de Produtos Naturais, Centro de Ciências da Saúde, Bloco H, Universidade Federal do Rio de Janeiro, RJ 21941-590, Brazil. |
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| Abstract: | Seven new 1,4-naphthoquinones structurally related to lapachol were synthesized from lawsone and oxygenated arylmercurials. These compounds can also be seen as pterocarpan derivatives where the A-ring was substituted by the 1,4-naphthoquinone nucleus. Pharmacological screening provided evidence of significant biological activities, including effects against proliferation of the MCF-7 human breast cancer cell line, against Herpes Simplex Virus type 2 infection, and against snake poison-induced myotoxicity. One derivative displaced flunitrazepam binding and showed benzodiazepine-like activity, suggesting novel neuroactive structural motifs. |
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