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Synchrotron-based FTIR evaluation of biochemical changes in cancer and noncance...

Magalhaes, CM; Ducic, T; Pereira, RB; Gonzalez-Berdullas, P; Rodriguez Borges, JE; Pereira, DM; Joaquim C G E Esteves da Silva; Algarra, M; da Silva, LP

The mode of action toward gastric cancer cells of brominated Coelenteramine, an analogue of a metabolic product of a marine bioluminescent reaction, was investigated by synchrotron radiation-based Fourier Transform Infrared spectrocopy (FTIR). This method revealed that the anticancer activity of brominated Coelenteramine is closely connected with cellular lipids, by affecting their organization and composition....


Evaluation of the anticancer activity and chemiluminescence of a halogenated co...

Luís Pinto da Silva; José Pedro Silva; Patricia González-Berdullas; Mariana Pereira; Diana Duarte; Rodriguez Borges, JE; Nuno Vale

Chemiluminescence is a remarkable process in which light is emitted due to a chemical reaction, without the need for photoexcitation. Among some of the most well-known chemiluminescent systems is that of marine Coelenterazine. Herein, we report the synthesis of a novel halogenated Coelenterazine analog, as well as the characterization of its potential anticancer activity and chemiluminescence. We have found tha...


Discovery of the Anticancer Activity for Lung and Gastric Cancer of a Brominate...

Luís Pinto da Silva; Patricia González-Berdullas; Renato B. Pereira; Cláudia Teixeira; José Pedro Silva; Carla M. Magalhães; Rodriguez Borges, JE

Cancer is still a challenging disease to treat, both in terms of harmful side effects and therapeutic efficiency of the available treatments. Herein, to develop new therapeutic molecules, we have investigated the anticancer activity of halogenated derivatives of different components of the bioluminescent system of marine Coelenterazine: Coelenterazine (Clz) itself, Coelenteramide (Clmd), and Coelenteramine (Clm...


Photodynamic Therapy

Luís Pinto da Silva; Joaquim C G E Esteves da Silva; Nuno Vale; Patricia González-Berdullas; Rodriguez Borges, JE

This book is dedicated to a topic related to the effects of photodynamic therapy organized by Biomedicines in 2022 (https://www.mdpi.com/topics/photodynamic_therapy). In medicine, the use of photodynamic therapy for the treatment of oncological and non-oncological diseases has been widely documented and well codified. In dermatology, the use varies from oncological to the treatment of chronic wounds, as well as...


Target-Oriented Synthesis of Marine Coelenterazine Derivatives with Anticancer ...

Magalhaes, CM; Gonzalez Berdullas, P; Duarte, D; Correia, AS; Rodriguez Borges, JE; Nuno Vale; Joaquim C G E Esteves da Silva; da Silva, LP

Photodynamic therapy (PDT) is an anticancer therapeutic modality with remarkable advantages over more conventional approaches. However, PDT is greatly limited by its dependence on external light sources. Given this, PDT would benefit from new systems capable of a light-free and intracellular photodynamic effect. Herein, we evaluated the heavy-atom effect as a strategy to provide anticancer activity to derivativ...


Design, Synthesis, and Evaluation of Antineoplastic Activity of Novel Carbocycl...

Aliuska M Helguera; Rodriguez Borges, JE; Olga Caamano; Xerardo Garcia Mera; Maykel P Perez Gonzalez; Natalia N D S Cordeiro

Cancer is the leading cause of death among men and women under age 85. Every year, millions of individuals are diagnosed with cancer. But finding new drugs is a complex, expensive, and very time-consuming task. Over the past decade, the cancer research community has begun to address the in silico modeling approaches, such as Quantitative Structure-Activity Relationships (QSAR), as an important alternative tool ...


Synthesis and pharmacological evaluation of novel substituted 9-deazaxanthines ...

Isabel Nieto, MI; Carmen Balo, MC; Brea, J; Caamano, O; Fernandez, F; Garcia Mera, X; Lopez, C; Isabel Loza, MI; Rodriguez Borges, JE; Vidal, B

A new series of 9-deazaxanthine derivatives with various substituents at the heterocyclic system were synthesized and evaluated for their binding affinities for the four human recombinant adenosine receptors, A(1)-A(3) subtypes. A number of the 9-deazaxanthines derivatives 3a-m showed moderate-to-high affinity for hA(2B) receptors, with compound 3f showing a 32-fold selectivity for A(2B) over A(1) and a 2750-fo...


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