Preparation of Galipea officinalis Hancock type tetrahydroquinoline alkaloid analogues as anti-tumour agents

The preparation of chiral tetrahydroquinolines using Ir-catalysed asymmetric hydrogenation and their possible cytotoxic potential anti-cancer activity were reported. Both of the in vitro cytotoxicity assay on a series of human cancer cell lines including A549 small cell lung cancer, MDA-MB-231 breast cancer, SaoS2 sacroma, SKHep-1 hepatoma and Hep3B hepatocellular carcinoma as well as in vivo animal model using Hep3B hepatocellular tumour xenograft on athymic nude mice suggest that 1,2,3,4-tetrahydroquin-8-ol is a potential anti-tumour alkaloid which may be further developed as a novel cancer chemotherapeutic agent.

Graphical abstractThe preparation of enantioselective tetrahydroquinolines using Ir-catalysed asymmetric hydrogenation and their possible cytotoxic potential towards the human carcinoma cell lines were presented. Of which, 1,2,3,4-tetrahydroquin-8-ol (2l) shows its anti-cancer activity both in vitro and in vivo.Figure optionsDownload full-size imageDownload high-quality image (81 K)Download as PowerPoint slide