Design, synthesis, and anti-tumor activities of novel Brevinin-1BYa peptidomimetics.

In this study, a series of novel Brevinin-1BYa derivatives, including O-linked N-acetyl-glucosamine glyclopeptides and disulfide bond mimetics, were designed and synthesized. Additionally, their anti-tumor activity against human prostate cancer cell line C4-2B, human NSCLC cell line A549 (adenocarcinoma), and human hepatoma cells line HuH-7 was investigated. Among these, the thioether bridge substituted peptidomimetic Brevinin-1BYa-3 displayed improved reduction stability, more stable secondary structure, greater protease stability, and increased anti-tumor activity compared with the original peptide, rendering it a promising leading compound for drug development, particularly for applications against malignant tumors.
PMID: 33556573 [PubMed - as supplied by publisher]

Source: Bioorganic and Medicinal Chemistry Letters - February 5, 2021 Category: Chemistry Authors: Xiong S, Wang N, Liu C, Shen H, Qu Z, Zhu L, Bai X, Hu HG, Cong W, Zhao L Tags: Bioorg Med Chem Lett Source Type: research