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Type: Artigo
Title: Synthesis, molecular modelling and anticancer activities of new molecular hybrids containing 1,4-Naphthoquinone, 7-Chloroquinoline, 1,3,5-Triazine and morpholine cores as PI3K and AMPK Inhibitors in the metastatic melanoma cells
Author: Fiorot, Rodolfo G.
Westphal, Regina
Lemos, Barbara C.
Romagna, Rodrigo A.
Goncalves, Paola R.
Fernandes, Maruska R. N.
Ferreira, Carmen, V
Taranto, Alex G.
Greco, Sandro J.
Abstract: Three molecular hybrids containing 1,4-naphtlioquinones, 1.3,5-triazines, morpholine and 7-chloroquinoline, which have recognized contributions to the biological activity of many drugs. were synthesized in yields ranging from 43-84%. All hybrids were obtained in three steps starting from readily available reactants: lawsone, cyanuric chloride. morpholine and 4,7-dichloroquinoline. A previous docking study was carried out to identify the binding energy and pharmacophore conformation of the promising anticancer compounds with PI3K gamma (phosphoinositide 3-kinase) and AMPK (5' AMP-activated protein kinase). The cancer activity in human metastatic melanoma cells (SKMEL-103) were performed, and the synthetized compounds presented half maximal inhibitory concentration (IC50) values around 25 mu M. The expressions of PI3K and AMPK were also determined using western blotting technique, and all molecular hybrids negatively modulated both targets
Subject: Hibridação molecular
Country: Brasil
Editor: Sociedade Brasileira de Química
Rights: Aberto
Identifier DOI: 10.21577/0103-5053.20190096
Date Issue: 2019
Appears in Collections:IB - Artigos e Outros Documentos
FCM - Artigos e Outros Documentos

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