|
|
|
|
|
| Freire,Rachel Lima Marcelino; Marques,Maria Betânia de Freitas; Souza-Fagundes,Elaine Maria de; Oliveira,Renata Barbosa de; Alves,Ricardo José. |
| Abstract A novel series of platinum (II) complexes was synthesized and the complexes were evaluated for their in vitro cytotoxicity against four human cancer cells lines. Five platinum complexes showed activity against at least one tumor cell line. Complexes 3 and 6 were promising, being active, at micromolar concentrations, against all the assayed tumor cell lines. Compound 3 was selected for further studies in mice with Ehrlich solid tumors and it was able to reduce the rate of tumor growth significantly during the first seven days. However, at the end of the experiments, there was no significant difference between the group of animals treated with 3 and the control group. The low solubility of the compound in the assay conditions can explain, at least... |
| Tipo: Info:eu-repo/semantics/article |
Palavras-chave: /Cytotoxic activity; Platinum complexes/ Ehrlich solid tumor activity.. |
| Ano: 2017 |
URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1984-82502017000100612 |
| |
|
|
| Lavorato,Stefânia Neiva; Duarte,Mariana Costa; Andrade,Pedro Henrique Rocha De; Coelho,Eduardo Antonio Ferraz; Alves,Ricardo José. |
| ABSTRACT We describe herein the synthesis and evaluation of the antileishmanial activity against promastigote forms of Leishmania amazonensis and cytotoxicity to murine macrophages of a series of 2-chloro-N-arylacetamide derivatives. All compounds were active, except one (compound 3). Compound 5 presented the most promising results, showing good antileishmanial activity (CI50=5.39±0.67 µM) and moderate selectivity (SI=6.36), indicating that further development of this class is worthwhile. Preliminary QSAR studies, although not predictive, furnished some insights on the importance of electronic character of aryl substituent to biological activity, as well as an indirect influence of hydrophobicity on activity. |
| Tipo: Info:eu-repo/semantics/article |
Palavras-chave: Leishmaniasis/treatment; Chloroacetamides; Leishmania amazonensisChloroacetamides/QSAR.. |
| Ano: 2017 |
URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1984-82502017000100620 |
| |
|
|
| Bretas,Ana Carolina Oliveira; Souza,Thiago Belarmino de; Borelli,Beatriz; Johan,Suzana; Alves,Ricardo José. |
| Systemic fungal infections are a growing problem in contemporary medicine and few drugs are licensed for therapy of invasive fungal infections. Differences between fungi and humans, like the presence of a cell wall in fungal cells, can be explored for designing new drugs. (1,3)-β-D-glucan synthase, an enzyme that catalyzes the synthesis of (1,3)-β-D-glucan, a structural and essential component of the fungal cell wall, is absent in mammals and this makes it an excellent target for the development of new antifungal agents. Papulacandins are a family of natural antifungal agents targeting (1,3)-β-D-glucan synthase. In this study we describe the synthesis and biological evaluation of two new Papulacandin analogs as potential (1,3)-β-D-glucan synthase inhibitors. |
| Tipo: Info:eu-repo/semantics/article |
Palavras-chave: Β-(1; 3)-D-glucan synthase Antifungal activity Papulacandin D Molecular simplification. |
| Ano: 2020 |
URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1984-82502020000100509 |
| |
|
|
|
