Design, synthesis and cytotoxicity of novel 3′-N-alkoxycarbonyl docetaxel analogs

J Chang, XD Hao, YP Hao, HF Lu, JM Yu…

Index: Chang, Jun; Hao, Xiao-Dong; Hao, Yun-Peng; Lu, Hong-Fu; Yu, Jian-Ming; Sun, Xun Bioorganic and Medicinal Chemistry Letters, 2013 , vol. 23, # 24 p. 6834 - 6837

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Abstract

Abstract By-product 9a exhibited potent cytotoxicity against both SK-OV-3 and A549 cell lines. The structure of 9a was characterized using 1D and 2D NMR experiments and confirmed by synthesis to afford a diastereomeric mixture (16a) that was identical to 9a, as well as a pair of diastereomers (R)-16b and (S)-16c. The preliminary SAR study demonstrated that analogs with an (R)-configuration were slightly more potent than ...