50 documents found, page 1 of 5
Liposomal formulations for efficient delivery of a novel, highly potent pyrimid...
Teixeira, Sofia; Ferreira, Débora Carina Gonçalves Abreu; Rodrigues, Ana Rita Oliveira; Rodrigues, L. R.; Castanheira, Elisabete M. S.Background/Objectives: Cancer is one of the deadliest diseases worldwide. Despite the existing treatments, the adverse side effects and the increasing drug resistance to the current therapies lead to a reduced quality of life for patients and poor prognosis. The pyrimido[5,4-d]pyrimidine compound (PP) was identified as a promising new anticancer drug due to its potent activity against colorectal and triple-nega...
Hydrazides as powerful tools in medicinal chemistry: synthesis, reactivity, and...
Teixeira, Sofia; Castanheira, Elisabete M. S.; Carvalho, M. AliceThe increase in drug resistance and the high toxicity of current drugs have inspired the scientific community to develop new drugs for various diseases. Hydrazides have become an attractive functional group to easily obtain a plethora of novel compounds with a broad range of biological activities. This review, which contains studies in the literature from the previous five years, focuses on the synthesis method...
Albumin/Hyaluronic acid gel nanoparticles loaded with a pyrimidine-based drug f...
Teixeira, Sofia; Ferreira, Débora Carina Gonçalves Abreu; Rodrigues, L. R.; Carvalho, M. Alice; Castanheira, Elisabete M. S.A pyrimidine-based compound (PP) was recently found to be a promising anticancer agent for colorectal and breast cancers. However, this compound exhibited low selectivity and poor water solubility. To address these challenges, albumin gel nanoparticles were used, where the gel matrix is formed by cross-linking of BSA molecules, allowing for a high concentration of this hydrophobic drug to be carried with no cyt...
Nanoformulações de um novo composto muito promissor para terapia do cancro da m...
Teixeira, Marta Sofia Vilela Barreira; Ferreira, Débora Carina Gonçalves Abreu; Rodrigues, L. R.; Castanheira, Elisabete M. S.; Carvalho, M. AliceNo presente estudo pretendeu-se desenvolver, caracterizar e avaliar o efeito antitumoral de nanoformulações carregadas com o composto Hit. As formulações carregadas com o composto hit foram caracterizadas por DLS (tamanho hidrodinâmico, índice de polidispersividade e potencial zeta), e a cinética de libertação do composto. Adicionalmente, os efeitos antitumorais das nanoformulações foram determinados na linha c...
Development and characterization of liposomal and albumin nanoformulations for ...
Teixeira, Marta Sofia Vilela Barreira; Castanheira, Elisabete M. S.; Carvalho, M. AliceCancer is a threat for humankind [1], and the scientific community has been fighting against this disease, developing new strategies and new potential chemotherapeutic agents.[2,3] Many of the drugs already used in chemotherapy (or under development) have poor water solubility and, therefore, cannot reach the targets efficiently.[4] The development of nanoformulations is a strategy followed to solve solubility ...
Discovery of 2,9-diaryl-6-carbamoylpurines as a novel class of antitubercular a...
Correia, Carla; Leite, Ana Claúdia; Fraga, Alexandra G.; Proença, M. Fernanda R. P.; Pedrosa, Jorge; Carvalho, M. AliceA series of novel 9-alkyl/aryl-2-aryl-6-carbamoylpurines were synthesized, and their activity against $\text{Mycobacterium tuberculosis}$ strain $\text{H}37\text{Rv}$ was assessed. The $\text{SAR}$ analysis on the first set of derivatives, with an alkyl or aryl unit at $\text{N}$-$9$ and a phenolic unit at $\text{C}$-$2$, showed that the activity depends on the purine ring substituents at $\text{N}$-$9$ and $\t...
2-Aryladenine derivatives as a potent scaffold for adenosine receptor antagonis...
Areias, Filipe; Correia, Carla; Rocha, Ashly; Teixeira, Sofia; Castro, Marián; Brea, Jose; Hu, Huabin; Carlsson, Jens; Loza, Maria I.A set of 2-aryl-9-H or methyl-6-morpholinopurine derivatives were synthesized and assayed through radioligand binding tests at human A<inf>1</inf>, A<inf>2A</inf>, A<inf>2B</inf>, and A<inf>3</inf> adenosine receptor subtypes. Eleven purines showed potent antagonism at A<inf>1</inf>, A<inf>3</inf>, dual A<inf>1</inf>/A<inf>2A</inf>, A<inf>1</inf>/A<inf>2B</inf>, or A<inf>1</inf>/A<inf>3</inf> adenosine receptor...
SAR study of 4,8-disubstituted Pyrimido[5,4-d]pyrimidines exhibiting antitrypan...
Lopes, André; Teixeira, Sofia; Santarém, Nuno; Greco, Alessandro; Pagliaro, Angela; Keminer, Oliver; Gul, Sheraz; Cordeiro-Da-Silva, AnabelaA set of new derivatives of 4,8-disubstituted pyrimido[5,4-d]pyrimidines were efficiently synthesized and in vitro evaluated against Trypanosoma brucei and Leishmania infantum promastigotes and intramacrophage amastigotes. The in vitro cytotoxicity was determined using the THP-1 cell line, and early in vitro ADME-Tox was carried out using in vitro assays for cytotoxicity (A549 and HEK293 cell lines) and CYP3A4 ...
Synthesis of novel 2,9-disubstituted-6-morpholino purine derivatives assisted b...
Lobo, Vítor; Rocha, Ashly; Castro, Tarsila Gabriel; Carvalho, M. AliceThe phosphatidylinositol-3 kinase (PI3K) pathway is one of the most frequently activated pathogenic signalling cascades in a wide variety of cancers. In the last 15 years, there has been an increase in the search for selective inhibitors of the four class I isoforms of PI3K, as they demonstrate better specificity and reduced toxicity in comparison to existing inhibitors. A ligand-based and target-based rational...
A tandem reaction in the synthesis of new 4,8-disubstituted-pyrimido[5,4-d]pyri...
Rocha, Ashly; Lopes, André; Teixeira, Sofia; Carvalho, M. AlicePyrimido[5,4-d]pyrimidines are biologically important compounds with diverse activity depending on the substituent groups around the heterocycle. The 3,4-dihydropyrimido[5,4-d]pyrimidines are efficiently converted to the aromatic derivatives by Dimroth rearrangement promoted by reaction with piperidine, in a very slow process. Subsequently, the aromatic derivatives are converted to new 4,8-disubstituted-pyrimid...