Author | Hiller, Noemi de J. | |
Author | Silva, Nayane A. A. E. | |
Author | Faria, Robson X. | |
Author | Souza, André Luís A. | |
Author | Resende, Jackson A. L. C. | |
Author | Farias, André Borges | |
Author | Romeiro, Nelilma Correia | |
Author | Martins, Daniela de Luna | |
Access date | 2019-01-29T15:03:36Z | |
Available date | 2019-01-29T15:03:36Z | |
Document date | 2018 | |
Citation | HILLER, Noemi de J. et al. Synthesis and Evaluation of the Anticancer and Trypanocidal Activities of Boronic Tyrphostins. ChemMedChem, v.13,p.1395–1404, 2018. | pt_BR |
ISSN | 1860-7179 | pt_BR |
URI | https://www.arca.fiocruz.br/handle/icict/31343 | |
Language | eng | pt_BR |
Publisher | Wiley | pt_BR |
Rights | restricted access | pt_BR |
Subject in Portuguese | Anticancer | pt_BR |
Subject in Portuguese | Tirfostinas Borônicas | pt_BR |
Subject in Portuguese | Atividades Tripanocidas | pt_BR |
Subject in Portuguese | Avaliação | pt_BR |
Subject in Portuguese | Síntese | pt_BR |
Title | Synthesis and Evaluation of the Anticancer and Trypanocidal Activities of Boronic Tyrphostins | pt_BR |
Type | Article | pt_BR |
DOI | 10.1002/cmdc.201800206 | |
Abstract | Molecules containing an (cyanovinyl)arene moiety are known as tyrphostins because of their ability to inhibit proteins from the tyrosine kinase family, an interesting target for the development of anticancer and trypanocidal drugs. In the present work, (E)-(cyanovinyl)benzeneboronic acids were synthesized by Knoevenagel condensations without the use of any catalysts in water through a simple protocol that completely avoided the use of organic solvents in the synthesis and workup process. The in vitro anticancer and trypanocidal activities of the synthesized boronic acids were also evaluated, and it was discovered that the introduction of the boronic acid functionality improved the activity of the boronic tyrphostins. In silico target fishing with the use of a chemogenomic approach suggested that tyrosine-phosphorylation-regulated kinase 1a (DYRK1A) was a potential target for some of the designed compounds. | pt_BR |
Affilliation | Universidade Federal Fluminense. Instituto de Química. Campus Valonguinho. Niterói, RJ, Brasil. | pt_BR |
Affilliation | Universidade Federal Fluminense. Instituto de Química. Campus Valonguinho. Niterói, RJ, Brasil. | pt_BR |
Affilliation | Fundação Oswaldo Cruz. Instituto Oswaldo Cruz. Laboratório de Toxoplasmose e outras Protozooses. Rio de Janeiro, RJ. Brasil. | pt_BR |
Affilliation | Fundação Oswaldo Cruz. Instituto Oswaldo Cruz. Laboratório de Bioquímica de Peptídeos. Rio de Janeiro, RJ. Brasil. | pt_BR |
Affilliation | Universidade Federal do Mato Grosso. Instituto de Ciências Exatas e da Terra. Campus Universitário do Araguaia. Laboratório de Química do Estado Sólido. Barra das Garças, MT, Brasil. | pt_BR |
Affilliation | Universidade Federal do Rio de Janeiro. Núcleo de Pesquisas em Ecologia e Desenvolvimento Social. Campus de Macaé. Macaé, RJ, Brasil. | pt_BR |
Affilliation | Universidade Federal do Rio de Janeiro. Núcleo de Pesquisas em Ecologia e Desenvolvimento Social. Campus de Macaé. Macaé, RJ, Brasil. | pt_BR |
Affilliation | Universidade Federal Fluminense. Instituto de Química. Campus Valonguinho. Niterói, RJ, Brasil. | pt_BR |
Subject | Trypanocidal Activities | pt_BR |
Subject | Boronic Tyrphostins | pt_BR |
Subject | Anticancer | pt_BR |
Subject | Synthesis | pt_BR |
Subject | Evaluation | pt_BR |
e-ISSN | 1860-7187 | |
Embargo date | 2030-01-01 | |