www.cheminform.wiley-vch.de

AlkaloidsU 0600 Synthesis and Structure—Activity Relationships of Berberine Analogues as a

Novel Class of Low-Density-Lipoprotein Receptor Up-Regulators. — Nineteen berberine analogues with substituents on the benzene ring D are synthesized by a five-step procedure in which the intramolecular cyclization of intermediate (II) acts as the key step. The acidification of (V) using HCl affords an analogue with increased LDLR up-regulatory activity with respect to berberine. This salt is selected as a prom-ising cholesterol-lowering drug candidate for further evaluation. — (YANG, P.; SONG, D.-Q.; LI, Y.-H.; KONG, W.-J.; WANG, Y.-X.; GAO, L.-M.; LIU, S.-Y.; CAO, R.-Q.; JIANG*, J.-D.; Bioorg. Med. Chem. Lett. 18 (2008) 16, 4675-4677; Inst. Med. Biotechnol., Chin. Acad. Med. Sci., Beijing 100050, Peop. Rep. China; Eng.) — H. Hoennerscheid

02- 202

ChemInform 2009, 40, issue 02 © 2008 Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim