Synthesis and anti-inflammatory evaluation of novel paclitaxel analogs

Abstract

A series of paclitaxel analogs modified at C-3′-N and C-7 positions were synthesized from baccatin III and their structures were confirmed by ¹H-NMR, ¹³C-NMR, HR-MS. Compound 7e exhibited potent ability to decrease TNFα (tumor necrosis factor α) in the LPS-activated RAW264.7 murine macrophage-like cell line. The preliminary data indicated that the anti-inflammatory effects may be related to MD-2 and Toll-like receptor 4 (TLR4), rather than Toll-like receptor 2 (TLR2).

Keywords:

• Paclitaxel
• anti-inflammatory
• tumor necrosis factor α
• lipopolysaccharide

Acknowledgments

The authors are grateful to Prof. Lei Li and Yan Tan, Research Institute of Surgery, Third Military Medical University, for their help in the activity assay. We also thank Dr H. Deng, The Instrumental Analysis & Research Center of Shanghai University, for structural analysis.