Category: amides-buliding-blocksOn October 1, 2021 ,《Synthesis, antitumor activity and in silico analyses of amino acid derivatives of artepillin C, drupanin and baccharin from green propolis》 was published in Bioorganic & Medicinal Chemistry. The article was written by Rodrigues, Debora Munhoz; Portapilla, Gisele Bulhoes; Silva, Guilherme Martins; Duarte, Andressa; Rotta, Cristiana Goncalez; da Silva, Carlos Henrique Tomich de Paula; de Albuquerque, Sergio; Bastos, Jairo Kenupp; Campo, Vanessa Leiria. The article contains the following contents:
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. The results came from multiple reactions, including the reaction of H-Lys(Boc)-OH(cas: 2418-95-3Category: amides-buliding-blocks)
H-Lys(Boc)-OH(cas: 2418-95-3) belongs to amino acids. These amino acids may be present in low concentrations and play a vital part as an intermediate in a biosynthetic pathway, e.g., ornithine, homoserine, or cystathionine. In contrast they may act as a major storage form of nitrogen, e.g., canavanine in the seed of Canavalia ensiformis, or may be formed in high amounts in response to an external stress, e.g., γ-aminobutyrate.Category: amides-buliding-blocks It is possible that some of these nonprotein amino acids may serve as insecticidal or fungicidal agents.
Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics