Chemokine Receptor CCR-5 Inhibitors Produced byChaetomiumglobosum
Journal of Natural Products2006Vol. 69(7), pp. 1025–1028
Citations Over TimeTop 19% of 2006 papers
Shu‐Wei Yang, Ronald Mierzwa, Joseph Terracciano, Mahesh Patel, Vincent P. Gullo, Nicole Wagner, Bahige M. Baroudy, Mohindar S. Puar, Tze‐Ming Chan, Andrew T. McPhail, Min Chu
Abstract
Two novel chemokine receptor CCR-5 inhibitors, Sch 210971 (1) and Sch 210972 (2), were isolated from the fungal fermentation broth of Chaetomium globosum by normal- and reversed-phase HPLC purifications. The structure determination of 1 and 2 was accomplished on the basis of UV, MS, and NMR spectral data analyses including COSY, NOESY, HMQC, and HMBC experiments. The structure and relative configuration of 2 were determined unequivocally by X-ray crystallographic analysis. The major component 2 demonstrated a potent inhibitory activity of IC(50) = 79 nM in the CCR-5 receptor in vitro binding assay.
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