- High-Yielding Water-Soluble Asymmetric Cyanine Dyes for Labeling Applications
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A simple and efficient microwave-assisted synthesis of asymmetric pentamethine cyanine dyes with various functional groups was developed, which allows high-yielding results. The synthesized dyes are modifiable and suitable for single-molecule imaging in biological and medical sciences by application of click chemistry or classic esterification and amidation.
- Wolf, Natalia,Kersting, Louise,Herok, Christoph,Mihm, Cornelius,Seibel, Juergen
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- Long-chain alkyltriazoles as antitumor agents: Synthesis, physicochemical properties, and biological and computational evaluation
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A series of novel long-chain alkyltriazoles were prepared from commercial diols in a rapid process with good yields. The compounds were evaluated in vitro for their anticancer potential against two human cancer cell lines: colon carcinoma (RKO) and uterine carcinoma (HeLa). The results of colorimetric MTT assays showed that six of fourteen compounds tested decreased cell viability in these cell lines. Compounds 5e and 6a were the most active against RKO cells, with IC50 values of 16.70 and 14.57 μM, respectively. The same compounds, 5e and 6a, were the most active in HeLa cells as well, with IC50 values of 11.05 and 12.77 μM, respectively. In addition, compound 5e was found to induce apoptosis in RKO cells, as assessed by TUNEL assay. The results suggest that compound 5e may be a promising prototype anticancer agent.
- Gontijo, Vanessa Silva,Oliveira, Michael der,Resende, Rafael Jos,Fonseca, Amanda Luisa,Nunes, Renata Rachide,Jnior, Moacyr Comar,Taranto, Alex Gutterres,Torres, Natalia Machado Pereira Oliveira,Viana, Gustavo Henrique Ribeiro,Silva, Luciana Maria,Alves, Rosemeire Brondi,Varotti, Fernando Pilla,Freitas, Rossimiriam Pereira
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p. 430 - 441
(2015/03/31)
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- Leishmanicidal, antiproteolytic, and mutagenic evaluation of alkyltriazoles and alkylphosphocholines
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Abstract A series of 16 simple long-chain alkyltriazoles and two novel alkylphosphocholine derivatives containing an azide moiety were evaluated in vitro for their leishmanicidal activity against. Among the 18 compounds tested, the eight most active compounds against promastigote forms were selected for further evaluation against amastigote forms. These compounds were also evaluated for their cytotoxicity against murine macrophages and tested as inhibitors of cysteine protease rCPB2.8, an important target for development of antileishmanial drugs. The mutagenicity of some of these compounds was also evaluated in prokaryotic and eukaryotic cells to assess any genetic effects of the leishmanicidal candidates. The compound 4, an alkylphosphocholine derivative, was found to be the most potent against amastigote forms with an IC50 of 3.81 μM, comparable to that of pentamidine (IC50 = 6.62 μM) and amphotericin B (IC50 = 6.10 μM), two established leishmanicidal drugs. Compound 4 also exhibited the best selectivity index (SI) values of the series, demonstrating low toxicity against macrophages and a cLogP value higher than 5. Among the alkyltriazoles, compounds 13 and 14 were the most active against promastigote and amastigote forms. They were then evaluated for their mutagenicity in vitro; the mutagenicity index (MI) values were lower than 2, suggesting that these compounds are not mutagenic.
- Gontijo, Vanessa Silva,Espuri, Patrícia Ferreira,Alves, Rosemeire Brondi,De Camargos, Luiz Fernando,Dos Santos, Fábio Vieira,De Souza Judice, Wagner Alves,Marques, Marcos José,Freitas, Rossimiriam Pereira
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- Synthesis and Evaluation of Antimalarial Activity of Oxygenated 3-alkylpyridine Marine Alkaloid Analogues
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A series of new oxygenated analogues of marine 3-alkylpyridine alkaloids were prepared from 3-pyridinepropanol in few steps and in good yields. The key step for the synthesis of these compounds was a Williamson etherification under phase-transfer conditions. All new compounds were evaluated for their antiplasmodial activity and cytotoxicity. A significant reduction in parasitaemia was observed for some of the prepared compounds, and the majority of them exhibited a selectivity index (SI) ranging from 2.78 to 15.58, which suggests that these compounds may be a promising class of substances with antimalarial activity.
- Hilario, Flaviane F.,de Paula, Renata Cristina,Silveira, Mariana L. T.,Viana, Gustavo H. R.,Alves, Rosemeire B.,Pereira, Juliana R.C.S.,Silva, Luciana Maria,de Freitas, Rossimiriam P.,de Pilla Varotti, Fernando
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experimental part
p. 477 - 482
(2012/04/04)
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- The design and synthesis of a 5-HETE affinity chromatography ligand for 5-hydroxyeicosanoid dehydrogenase
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The first total synthesis of an ω-amino 5-HETE derivative 27 has been accomplished by a new counter-clockwise strategy, in which C-1 is constructed first and C-20 last. The ω-amino 5-HETE derivative was transformed to an affinity chromatography ligand, the biotinylated 5-HETE 30. This affinity chromatography ligand is aimed at purifying the 5-hydroxyeicosanoid dehydrogenase enzyme, which is responsible for the conversion of 5-HETE to 5- oxo-ETE, a potent eosinophil chemotactic factor. (C) 2000 Elsevier Science Ltd.
- Khanapure, Subhash P.,Saha, Goutam,Powell, William S.,Rokach, Joshua
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p. 5807 - 5811
(2007/10/03)
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