引用本文:
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.
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.
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.
Synthesis and Biological Evaluation of Substituted 3'-N-Benzoyl Taxol Analogs
摘要:
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.
English
Synthesis and Biological Evaluation of Substituted 3'-N-Benzoyl Taxol Analogs
Abstract:
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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