Citation: Qin YUE, Qi-Cheng FANG, Xiao Tian UANG. Synthesis and Biological Evaluation of Substituted 3'-N-Benzoyl Taxol Analogs[J]. Chinese Chemical Letters, ;1996, 7(11): 984-986. shu

Synthesis and Biological Evaluation of Substituted 3'-N-Benzoyl Taxol Analogs

Insititute of Materia Medica Chinese Academy of Medical Sciences & Peking Union Medical College Beijing 100050

Received Date: 22 April 1996

Fund Project: The authors wish to thank Xiao-hong Lei for performing cytotocivity tests against KB cell of compounds, Thanks are due to the Dept, of Instrumental Analysis of our institute for spectroscopic measurements.

A series of substituted 3'-N-benzoyl taxol analogs [7a~i] were synthesized by Schotten-Baumann acylation of the key intermediate,13-O-[(2'R,3'S)-3'-phenylisoserinoyl] baccatin Ⅲ[6].Evaluation of the newly prepared derivatives for cytotoxicity against KB cell line revealed that electron-donating groups at the para position(such as-CH₃,-OCH₃,etc.)have positive effect on activity,while electron-attracting groups(such as-NO₂,-Br,etc.)have negative effect.Sterically hindered substituents at the ortho position could dramatically reduce the activity.But none of the analogs had higher cytotoxicity than taxol.
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