33640-67-4Relevant articles and documents
Synthesis, experimental and theoretical photophysical study of proton transfer based oxazoline fluorophores. Potential tailor made optical sensors for enantiomeric detection in solution
Santos, Fabiano S.,Zanotto, Gabriel M.,Argomedo, Luis M.Z.,Darbem, Mariana P.,Gon?alves, Paulo F.B.,Stefani, Helio A.,Rodembusch, Fabiano S.
, p. 372 - 382 (2019)
A series of oxazoline based compounds was obtained via amidation formation from salicylic acid derivatives and benzyl-protected L-threonine with good yields (50–90%). These compounds present absorption in the UV region (～300 nm) and fluorescence emission
Synthesis, antitumor activity and in silico analyses of amino acid derivatives of artepillin C, drupanin and baccharin from green propolis
Rodrigues, Débora Munhoz,Portapilla, Gisele Bulh?es,Silva, Guilherme Martins,Duarte, Andressa,Rotta, Cristiana Gon?alez,da Silva, Carlos Henrique Tomich de Paula,de Albuquerque, Sérgio,Bastos, Jairo Kenupp,Campo, Vanessa Leiria
, (2021/08/30)
Breast cancer has the highest incidence and mortality in females, while prostate cancer has the second-highest incidence in males. Studies have shown that compounds from Brazilian green propolis have antitumor activities and can selectively inhibit the AKR1C3 enzyme, overexpressed in hormone-dependent prostate and breast tumors. Thus, in an attempt to develop new cytotoxic inhibitors against these cancers, three prenylated compounds, artepillin C, drupanin and baccharin, were isolated from green propolis to synthesize new derivatives via coupling reactions with different amino acids. All obtained derivatives were submitted to antiproliferative assays against four cancer cells (MCF-7, MDA MB-231, PC-3, and DU145) and two normal cell lines (MCF-10A and PNT-2) to evaluate their cytotoxicity. In general, the best activity was observed for compound 6e, derived from drupanin, which exhibited half-maximal inhibitory concentration (IC50) of 9.6 ± 3 μM and selectivity index (SI) of 5.5 against MCF-7 cells. In silico studies demonstrated that these derivatives present coherent docking interactions and binding modes against AKR1C3, which might represent a possible mechanism of inhibition in MCF-7 cells.
Concise synthesis of α-methylene-β-hydroxy-γ-carboxy- γ-lactams
Tekkam, Srinivas,Johnson, Joseph L.,Jonnalagadda, Subash C.,Mereddy, Venkatram R.
, p. 955 - 958 (2013/08/23)
A concise protocol for the synthesis of α-methylene-β-hydroxy- γ-carboxy-γ-lactams has been described via alkylation of amino acid derived iminoesters with α-bromomethylmethacrylate, followed by allylic hydroxylation. All the synthesized compounds have been evaluated for their cytotoxicity on multiple myeloma cancer cell lines.
