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Paper | Regular issue | Vol 53, No. 12, 2000, pp.2719-2737
Published online, 1st January, 1970
DOI: 10.3987/COM-00-9051
Synthesis and Antitumor Activity of Non-Prodrug Water-soluble Taxoid: 10-C-Aminoalkylated Docetaxel Analogs

Shin Iimura, Satoru Ohsuki, Jun Chiba, Kouichi Uoto, Michio Iwahana, Hirofumi Terasawa, and Tsunehiko Soga*

*New Product Research Laboratories IV, Daiichi Pharmaceutical Co., Ltd., 1-16-13, Kitakasai, Edogawa, Tokyo 134-8630, Japan

Abstract

To develop non-prodrugs of taxoids possessing satisfactory stability in vivo, high water solubility and potent antitumor activity, we prepared several 10-C-sec-aminoalkylated docetaxel analogs and evaluated their cytotoxicity against mouse leukemia and human tumor cell lines. These analogs were synthesized from a 10-deacetoxy-10-C-formylethyl baccatin derivative. Among these analogs, the 10-C-morpholinoethyl and 10-C-morpholinomethyl analogs exhibited cytotoxicity comparable or superior to that of docetaxel.