Synthesis of Amino Acid‐comprising Sialyltransferase Inhibitors and Their Antimetastatic Activities against Human Breast Cancer Cells

Abstract

AbstractThe amino acid‐containing lithocholic acids (LCA) represent a new class of human sialyltransferase (ST) inhibitors. In this study, we have reported their design, synthesis, and inhibitory activity against human STs. Among these derivatives, D‐Glu‐LCA 7, L‐Asp‐L‐Asp‐LCA 13, and L‐Asp‐L‐Asp‐Gly‐Gly‐LCA 22 with specific amino acid sequence were the most active ones with IC50 values of 2.3–5.6 and 4.2‐6.2 μM toward α‐2,3‐ST and α‐2,6‐ST, respectively. The current study demonstrates that the new class of ST in‐ hibitors inhibit cell migration in breast cancer cells by preventing closure of the wound rather than involv‐ ing a direct antiproliferative effect.