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Insights into the anticancer activity of chiral alkylidene-β-lactams and alkyli...

Alves, Américo J. S.; Alves, Nuno G.; Laranjo, Mafalda; Gomes, Clara S. B.; Gonçalves, Ana Cristina; Ribeiro, Ana Bela Sarmento; Botelho, M. Filomena

Chiral alkylidene-β-lactams and alkylidene-γ-lactams were synthesized and screened for their in vitro activity against four human cancer cell lines (melanoma, esophageal, lung and fibrosarcoma carcinoma). Alkylidene-β-lactams were synthesized via Wittig reaction of diverse phosphorus ylides with benzhydryl 6-oxopenicillanate, derived from 6-aminopenicillanic acid. Moreover, novel chiral alkylidene-γ-lactams wer...


Applications of Photodynamic Therapy in Endometrial Diseases

Correia-Barros, Gabriela; Serambeque, Beatriz; Carvalho, Maria João; Marto, Carlos Miguel; Pineiro, Marta; Pinho e Melo, Teresa M. V. D.

Photodynamic therapy (PDT) is a medical procedure useful for several benign conditions (such as wound healing and infections) and cancer. PDT is minimally invasive, presents few side effects, good scaring, and is able to minimal tissue destruction maintaining organ anatomy and function. Endoscopic access to the uterus puts PDT in the spotlight for endometrial disease treatment. This work systematically reviews ...


Ring-Fused meso-Tetraarylchlorins as Auspicious PDT Sensitizers: Synthesis, Str...

Laranjo, Mafalda; Pereira, Nelson A. M.; Oliveira, Andreia S. R.; Aguiar, Márcia Campos; Brites, Gonçalo Sousa; Nascimento, Bruno F. O.

Novel 4,5,6,7-tetrahydropyrazolo[1,5-a]pyridine-fused meso-tetraarylchlorins, with different degrees of hydrophilicity (with methyl ester, hydroxymethyl, and carboxylic acid moieties), have been synthesized and their photophysical characterization as well as in vitro photocytotoxicity assessment against human melanoma and esophageal and bladder carcinomas was carried out. An integrated analysis of the photosens...


Functional impairment of circulating FcεRI+ monocytes and myeloid dendritic cel...

Martín-Sierra, Carmen; Martins, Ricardo; Laranjeira, Paula; Abrantes, A. Margarida; Oliveira, R. Caetano; Tralhão, J. Guilherme; Botelho, M. Filomena

Background Hepatocellular carcinoma (HCC) and cholangiocarcinoma (CCA) represent the most common primary liver malignancies whose outcome is influenced by the immune response. Methods In this study, we have functionally characterized, by flow cytometry, circulating myeloid dendritic cells (mDCs) and FcεRI+ monocytes in a group of healthy individuals (n = 10) and in a group of patients with HCC (n = 19) and CCA ...


Tissular growth factors profile after teduglutide administration on an animal m...

Costa, Beatriz P.; Gonçalves, Ana C.; Abrantes, Ana M.; Alves, Raquel; Matafome, Paulo N.; Seiça, Raquel; Ribeiro, Ana B. Sarmento; Botelho, M. Filomena

Background: Teduglutide is an enterotrophic analogue of glucagon-like peptide-2, with an indirect and poorly understood mechanism of action, approved for the rehabilitation of short-bowel syndrome. This study aims to analyze the response of tissue growth factors to surgical injury and teduglutide administration on an animal model of intestinal anastomosis. Methods: Wistar rats (n = 59) were distributed into fou...


Platinum(II) Ring-Fused Chlorins as Near-Infrared Emitting Oxygen Sensors and P...

Pereira, Nelson A. M.; Laranjo, Mafalda; Casalta-Lopes, João; Serra, Arménio C.; Piñeiro, Marta; Pina, João; Seixas de Melo, J. Sérgio

Novel near-infrared luminescent compounds based on platinum(II) 4,5,6,7-tetrahydropyrazolo[1,5-a]pyridine-fused chlorins are described. These compounds have high photostability and display light emission, in particular simultaneous fluorescence and phosphorescence emission in solution at room temperature, in the biologically relevant 700-850 nm red and near-infrared (NIR) spectral region, making them excellent ...


Targeting triple-negative breast cancer cells with 6,7-bis(hydroxymethyl)-1H,3H...

Santos, Kathleen; Laranjo, Mafalda; Abrantes, Ana Margarida; Brito, Ana F.; Gonçalves, Cristina; Ribeiro, Ana Bela Sarmento; Botelho, M. Filomena

Further studies on 6,7-bis(hydroxymethyl)-1H,3H-pyrrolo[1,2-c]thiazoles as anticancer agents against breast cancer are reported, allowing to demonstrate the potential of these compounds for the therapy of the triple-negative breast cancer, the most challenging tumors in clinical practice. These compounds were assayed for their in vitro cytotoxicity on several human breast cancer cell lines (MCF7, HCC1954 and HC...


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