A novel imidazopyridine analogue as a phosphatidylinositol 3-kinase inhibitor against human breast cancer

Abstract

Potentiation of anti-breast cancer activity of an imidazopyridine-based PI3K alpha inhibitor, HS-104, was investigated in human breast cancer cells. HS-104 shows strong inhibitory activity against recombinant PI3K alpha isoform and the PI3K signaling pathway, resulting in anti-proliferative activity in breast cancer cells. It also induced cell cycle arrest at the G(2)/M phase as well as apoptosis. Furthermore, oral administration of HS-104 significantly inhibited the growth of tumor in SkBr3 mouse xenograft models. Therefore, HS-104 could be considered as a potential candidate for the treatment of human breast cancer. Crown Copyright (C) 2011 Published by Elsevier Ireland Ltd. All rights reserved.