899588-25-1Relevant articles and documents
Synthesis of Novel Chalcone-Based L-Homoserine Lactones and Their Quorum Sensing Inhibitory Activity Evaluation
Chunying, Luo,Feng, Pengxia,Li, Jieming,Li, Pan,Liu, Haoyue,Wu, Chun-Li,Zhao, Liutao
, p. 139 - 148 (2020/05/04)
Abstract: Two novel series of chalcone-based homoserine lactones were synthesized and their quorum sensing (QS) inhibitory activity was evaluated against Pseudomonas aeruginosa in vitro. Furthermore these compounds’ capacity for modulation of the LasR-dependent quorum sensing system of P. aeruginosa was identified. Among these compounds, (S)-2-((4-(3-(4-bromo-2-fluorophenyl) acryloyl) phenyl) amino)-N-(2-oxotetrahydrofuran-3-yl)acetamide exerted the inhibition of LasR-dependent QS system of P. aeruginosa in contrast to brominated furanone C30. Worthy of particular note, this research has delivered novel potent quorum sensing inhibitors (QSIs), which strongly inhibit the production of virulence factors in a wild type strain of this pathogenic bacterium.
Antiproliferative activity and p53 upregulation effects of chalcones on human breast cancer cells
dos Santos, Mariana Bastos,Bertholin Anselmo, Daiane,de Oliveira, Jéssica Gisleine,Jardim-Perassi, Bruna V.,Alves Monteiro, Diego,Silva, Gabriel,Gomes, Eleni,Lucia Fachin, Ana,Marins, Mozart,de Campos Zuccari, Débora Aparecida Pires,Octavio Regasini, Luis
, p. 1093 - 1099 (2019/06/06)
Chalcones are valuable structures for drug discovery due to their broad bioactivity spectrum. In this study, we evaluated 20 synthetic chalcones against estrogen-receptor-positive breast cancer cells (MCF-7 line) and triple-negative breast cancer (TNBC) cells (MDA-MB-231 line). Antiproliferative screening by MTT assay resulted in two most active compounds: 2-fluoro-4’-aminochalcone (11) and 3-pyridyl-4’-aminochalcone (17). Their IC50 values ranged from 13.2 to 34.7?μM against both cell lines. Selected chalcones are weak basic compounds and maintained their antiproliferative activity under acidosis conditions (pH 6.7), indicating their resistance to ion-trapping effect. The mode of breast cancer cells death was investigated and chalcones 11 and 17 were able to induce apoptosis rather than necrosis in both lines. Antiproliferative target investigations with MCF-7 cells suggested 11 and 17 upregulated p53 protein expression and did not affect Sp1 protein expression. Future studies on chalcones 11 and 17 can define their in vivo therapeutic potential.
Naphthoquinone-based chalcone hybrids and derivatives: Synthesis and potent activity against cancer cell lines
Jardim, Guilherme A. M.,Guimares, Tiago T.,Pinto, Maria Do Carmo F.R.,Cavalcanti, Bruno C.,De Farias, Kaio M.,Pessoa, Claudia,Gatto, Claudia C.,Nair, Divya K.,Namboothiri, Irishi N. N.,Da Silva Jnior, Eufrnio N.
, p. 120 - 150 (2015/02/02)
Novel naphthoquinone-based chalcones were prepared from the reaction between 3-bromo-nor-β-lapachone and amino-chalcones. Lapachone derivatives are also described here. All the substances were evaluated against cancer and normal cell lines and several compounds demonstrated potent antitumor activity. This journal is