Bioorganic & Medicinal Chemistry 2002-10-01

Structure-activity relationship study at the 3'-N-position of paclitaxel: synthesis and biological evaluation of 3'-N-acyl-paclitaxel analogues.

Eun Joo Roh, Deukjoon Kim, Chong Ock Lee, Sang Un Choi, Choong Eui Song

Index: Bioorg. Med. Chem. 10(10) , 3145-51, (2002)

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Abstract

A series of 3'-N-acyl-paclitaxel analogues 1a-v were synthesized and their cytotoxicities in vitro against several human tumor cell lines examined. It has been shown that distinct correlation between activity and N-acyl-substituent. The appropriate size of N-acyl group was indispensable for cytotoxicity, and moreover, the presence of beta-substituted conjugated double and triple bond to N-carbonyl generally resulted in increase of cytotoxicities.