Synthesis of taxoids 5.: Synthesis and evaluation of novel water-soluble prodrugs of a 3′-desphenyl-3′-cyclopropyl analogue of docetaxel

被引：16

作者：

Yamaguchi, T ^{[1
]}

Harada, N ^{[1
]}

Ozaki, K ^{[1
]}

Arakawa, H ^{[1
]}

Oda, K ^{[1
]}

Nakanishi, N ^{[1
]}

Tsujihara, K ^{[1
]}

Hashiyama, T ^{[1
]}

机构：

[1] Tanabe Seiyaku Co Ltd, Med Chem Res Labs, Toda, Saitama 3358505, Japan

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1999年 / 9卷 / 12期

关键词：

D O I：

10.1016/S0960-894X(99)00257-7

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A novel 3'-desphenyl-3'-cyclopropyl analogue of docetaxel was synthesized from 10-deacetylbaccatin III. The cytotoxicity of the new taxoid was evaluated against several human tumor cell lines, and it had ca. 20 times stronger activity against human colon cancer cell lines (WiDr and Colon 320) than that of docetaxel. This taxoid was converted to its water-soluble prodrugs that have 2'-substituted amino acid derivatives with spacer. The prodrugs had good solubility in saline and showed more potent antitumor activity against B16 melanoma in mice than that of docetaxel. (C) 1999 Elsevier Science Ltd. All rights reserved.

引用

页码：1639 / 1644

页数：6

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